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Template residues during the preparation of hydroxyapatite (HA) microspheres with hollow structures limit their biological applications to some extent. In this study, the nanosheet-assembled porous-wall hollow HA microspheres were successfully synthesized by a template-free hydrothermal method. SEM and TEM observations revealed that the prepared hollow HA microspheres were about 3–7 μm in diameter and were composed of an interior cavity and a porous shell assembled by nanosheets (consisting of radial nanorods arranged side-by-side). A possible mechanism for the formation of the hollow HA microspheres was proposed based on the time-gradient experiments. Furthermore, the hollow HA microspheres exhibited excellent vancomycin loading capacity (101.3 mg/g) and pH-responsive release properties. This study provides new inspiration for the design and various applications of hollow materials. [ABSTRACT FROM AUTHOR]

In situ forming implants (ISFIs) composed of biodegradable polymers and biocompatible solvents are generally designed for sustained drug release. In this study, a non-invasive computed tomography (CT) imaging approach is used to achieve real time imaging of ISFIs in vivo and in vitro using leuprolide acetate in situ forming implant as a model drug product. The process of implant formation, inner structure change and their impact on drug release were elucidated. Real-time drug distribution was unveiled by the CT contrast agent, iohexol, where it shows a core-shell structure of the deposition. The incorporation of leuprolide acetate (LA) led to a reduced extent of burst release, prolongated release profile, and extended implant size expansion. LA was found to interact with the solvent and slowed down the polymer phase inversion, thus significantly changed the drug distribution in the implant and reduced the drug release. The implant inner structure identified through SEM, implant size change, and polymer degradation along with the CT real time imaging all consistently support the implant formation differences and their implant on the drug release. Similar patterns of implant size expansion and iohexol distribution in the implants were observed both in vitro and in vivo for the implants with and without LA. The comprehensive understanding of the impact of implant formation on drug release through real time CT imaging facilitates the ISFI product development and evaluation. [Display omitted] [ABSTRACT FROM AUTHOR]

A tri-layer scaffold was fabricated according to functionally graded materials (FGM) theory from poly(glycerol sebcate)/poly(L-lactic acid) blend by the increasing polylactic acid ratio from the inner to the outer layer. Heparin and platelet-rich plasma were loaded in separate layers to achieve proper remodeling and patency. The scaffold showed a linear degradation trend. The elastic modulus was 13.8 ± 1.11 Mpa that was in the favorable range for constructing artificial vessels. The integrity of the layers was preserved due to its FGM structure. The scaffold showed full blood compatibility by minimal platelet adhesion and hemolysis due to relatively slow release of Heparin. [ABSTRACT FROM AUTHOR]

Porous nickel-titanium (NiTi) manufactured using metal injection molding (MIM) has emerged as an innovative generation of drug-loaded stent materials. However, an increase in NiTi porosity may compromise its mechanical properties and cytocompatibility. This study aims to explore the potential of porous NiTi as a vascular drug delivery material and evaluate the impact of porosity on its drug loading and release, mechanical properties, and cytocompatibility. MIM, combined with the powder space-holder method, was used to fabricate porous NiTi alloys with three porosity levels. The mechanical properties of porous NiTi were assessed, as well as the surface cell growth capability. Furthermore, by loading rapamycin nanoparticles onto the surface and within the pores of porous NiTi, we evaluated the in vitro drug release behavior, inhibitory effect on cell proliferation, and inhibition of neointimal hyperplasia in vivo. The results demonstrated that an increase in porosity led to a decrease in the mechanical properties of porous NiTi, including hardness, tensile strength, and elastic modulus, and a decrease in the surface cell growth capability, affecting both cell proliferation and morphology. Concurrently, the loading capacity and release duration of rapamycin were extended with increasing porosity, resulting in enhanced inhibitory effects on cell proliferation in vitro and inhibition of neointimal hyperplasia in vivo. In conclusion, porous NiTi holds promise as a desirable vascular drug delivery material, but a balanced consideration of the influence of porosity on both mechanical properties and cytocompatibility is necessary to achieve an optimal balance among drug-loading and release performance, mechanical properties, and cytocompatibility. [ABSTRACT FROM AUTHOR]

In this study, ZnO quantum dots (ZnO@QDs) were synthesized and functionalized with 2nd generation poly amido amine (2GPD) using 3-amino-propyl tri-methoxy silane as the initiator core, facilitated by tetramethylammonium hydroxide (TMAH) to enhance stability against oleate coating. Concurrently, a mesoporous substrate with a unique morphology was developed as a drug reservoir for doxorubicin loading. ZnO quantum dots displayed photoluminescence radiation, with dimensions ranging from 5 to 7 nm and exhibiting spherical morphology. The cubic structure of the synthesized mesoporous nanocatalysts was also confirmed. Brunauer-Emmett-Teller analysis indicated a multidimensional porous structure of the nanocarriers, while zeta potential analysis showed a stable system (approximately −9.6 mV). Fourier transform infrared spectroscopy, X-ray diffraction, and energy dispersive spectroscopy corroborated these findings. Drug release studies demonstrated sustained release under acidic conditions (pH 5.5), with an efficiency of approximately 94 %. These results highlight the potential applications of this nanosystem for controlled drug delivery, underscoring its practical implications in the field of nanotechnology. [ABSTRACT FROM AUTHOR]

In recent years, the understanding of the role of the immune system in tumor progression and metastasis is paving the way for the development of antitumoral strategies based on the delivery of immunotherapeutic agents. The engineering of stimuli‐responsive nanocarriers able to release their payload in a controlled manner being able to boost potent and sustained immune responses against tumors has provided a powerful tool to eradicate tumors with extreme precision. Paramount advantages to trigger the immune system against tumors are the high selectivity and memory effect of immune response, which allows not only to eradicate primary and metastatic malignancies but also to avoid their relapse. In this review, the recent advances carried out in the development of smart nanocarriers for immunotherapy are presented. [ABSTRACT FROM AUTHOR]

A series of hybrid hydrogels of poly(ethylene glycol) (PEG) were synthesized using gelatin as a crosslinker and investigated for controlled delivery of the first-generation cephalosporin antibiotic, Cefazedone sodium (CFD). A commercially available 4-arm-PEG–OH was first modified to obtain four-arm-PEG–succinimidyl glutarate (4-arm-PEG–SG), which formed the gelatin–PEG composite hydrogels (SnNm) through crosslinking with gelatin. To regulate the drug delivery, SnNm hydrogels with various solid contents and crosslinking degrees were prepared. The effect of solid contents and crosslinking degrees on the thermal, mechanical, swelling, degradation, and drug release properties of the hydrogels were intensively investigated. The results revealed that increasing the crosslinking degree and solid content of SnNm could not only enhance the thermal stability, swelling ratio (SR), and compression resistance capacity of SnNm but also prolong the degradation and drug release times. The release kinetics of the SnNm hydrogels were found to follow the first-order model, suggesting that the transport rate of CFD within the matrix of hydrogels is proportional to the concentration of the drug where it is located. Specifically, S1N1-III showed 90% mass loss after 60 h of degradation and a sustained release duration of 72 h. The cytotoxicity assay using the MTT method revealed that cell viability rates of S1N1 were higher than 95%, indicating excellent cytocompatibility. This study offers new insights and methodologies for the development of hydrogels as biomedical composite materials. [ABSTRACT FROM AUTHOR]

The purpose of the current work was to develop and characterize ethosomes of vitamin D3 gel that could more effectively work against psoriasis. Psoriasis is a chronic immune-mediated inflammatory skin disease. Due to vitamin D3 role in proliferation and maturation of keratinocytes, it has become an important local therapeutic option in the treatment of psoriasis. In this research we have initiated worked on ethosomes gels containing vitamin D3 to treat psoriasis. Soya lecithin 1–8% (w/v), propylene glycol and ethanol were used to create the formulations, which were then tested for vesicle size, shape, surface morphology, entrapment effectiveness, and in vitro drug permeation. The drug encapsulation efficiency of ethosomes was 96.25% ± 0.3. The particle sizes of the optimized ethosomes was 148 and 657 nm, and the PDI value was 0.770 ± 0.12 along with negative charge − 14 ± 3. Fourier transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC) along with thermogravimetric analysis (TGA) studies confirmed the absence of interactions between vitamin D3 and other ingredients. It was determined that the total amount of medication that penetrated the membrane was 95.34% ± 3. Percentage lysis was very negligible for all strengths which were found less than 15%. Based on our research, ethosomes appear to be safe for use. The vitamin D3 ethosomal gel order, description, pH, and viscosity were all within the specified ranges, according to the findings of a 6-month investigation into the stability profile of the completed system. In this research, we successfully prepared ethosomes loaded with vitamin D3 and then converted it into gel for patients' easy applications. [ABSTRACT FROM AUTHOR]

This work combines experimental and computational modeling studies for the preparation of a composite of metformin and an organoclay, examining the advantages of a Tunisian clay used for drug delivery applications. The clay mineral studied is a montmorillonite-like smectite (Sm-Na), and the organoclay derivative (HDTMA-Sm) was used as a drug carrier for metformin hydrochloride (MET). In order to assess the MET loading into the clays, these materials were characterized by means of cation exchange capacity assessment, specific surface area measurement, and with the techniques of X-ray diffraction (XRD), differential scanning calorimetry, X-ray fluorescence spectroscopy, and Fourier-transformed infrared spectroscopy. Computational molecular modeling studies showed the surface adsorption process, identifying the clay–drug interactions through hydrogen bonds, and assessing electrostatic interactions for the hybrid MET/Sm-Na and hydrophobic interactions and cation exchange for the hybrid MET/HDTMA-Sm. The results show that the clays (Sm-Na and HDTMA-Sm) are capable of adsorbing MET, reaching a maximum load of 12.42 and 21.97 %, respectively. The adsorption isotherms were fitted by the Freundlich model, indicating heterogeneous adsorption of the studied adsorbate–adsorbent system, and they followed pseudo-second-order kinetics. The calculations of ΔGº indicate the spontaneous and reversible nature of the adsorption. The calculation of ΔH° indicates physical adsorption for the purified clay (Sm-Na) and chemical adsorption for the modified clay (HDTMA-Sm). The release of intercalated MET was studied in media simulating gastric and intestinal fluids, revealing that the purified clay (Sm-Na) and the modified organoclay (HDTMA-Sm) can be used as carriers in controlled drug delivery in future clinical applications. The molecular modeling studies confirmed the experimental phenomena, showing that the main adsorption mechanism is the cation exchange process between proton and MET cations into the interlayer space. [ABSTRACT FROM AUTHOR]

• Four candesartan cilexetil-loaded mesoporous silica dispersions were prepared through solvent immersion. • Dissolution in vitro of four formulations were evaluated using flow-through cell dissolution method. • Pore size and surface area of carriers played key roles in drug loading and release. • CC-XDP 3150 exhibited a 1.88-fold larger release of CC as compared to crystalline drug. • The relative bioavailability of CC-XDP3150 in rats was enhanced 326 % in comparison with CC. Candesartan cilexetil (CC) is one of well-tolerated antihypertensive drugs, while its poor solubility and low bioavailability limit its use. Herein, two mesoporous silica (Syloid XDP 3150 and Syloid AL-1 FP) and the corresponding amino-modified products (N-XDP 3150 and N-AL-1 FP) have been selected as the carriers of Candesartan cilexetil to prepare solid dispersion through solvent immersion, and characterized through using powder X-ray diffraction analysis, infrared spectroscopy, differential scanning calorimetry, scanning electron microscopy, and solid-state nuclear magnetic resonance spectroscopy, etc. The state of CC changed from crystalline to amorphous after loading onto the silica carriers, in which no interactions between CC and silica existed. Then, the dissolution behaviors in vitro were studied through using flow-through cell dissolution method. CC-XDP 3150 sample exhibited the most extensive dissolution, and the cumulative release of CC from it was 1.88-fold larger than that of CC. Moreover, the pharmacokinetic results in rats revealed that the relative bioavailability of CC-XDP 3150 and CC-N-XDP 3150 solid dispersions were estimated to be 326 % % and 238 % % in comparison with CC, respectively. Clearly, pore size, pore volume, and surface properties of silica carrier have remarkable effect on loading, dissolution and bioavailability of CC. In brief, this work will provide valuable information in construction of mesoporous silica-based delivery system toward poorly water-soluble drugs. [Display omitted] [ABSTRACT FROM AUTHOR]

In this study, a novel bio-composite material that allow sustained release of plant derived antimicrobial compound was developed for the biomedical applications to prevent the infections caused by microorganisms resistant to commercial antimicrobials agents. With this aim, bacterial cellulose (BC)-p(HEMA) nanocomposite film that imprinted with eugenol (EU) via metal chelated monomer, MAH was prepared. Firstly, characterization studies were utilized by FTIR, SEM and BET analysis. Then antimicrobial assays, drug release studies and in vitro cytotoxicity test were performed. A significant antimicrobial effect against both Gram (+) Staphylococcus aureus and Gram (-) Escherichia coli bacteria and a yeast Candida albicans were observed even in low exposure time periods. When antimicrobial effect of EU compared with commercially used agents, both antifungal and antibacterial activity of EU were found to be higher. Then, sustained drug release studies showed that approximately 55% of EU was released up to 50 h. This result proved the achievement of the molecular imprinting for an immobilization of molecules that desired to release on an area in a long-time interval. Finally, the in vitro cytotoxicity experiment performed with the mouse L929 cell line determined that the synthesized EU-imprinted BC nanocomposite was biocompatible. [ABSTRACT FROM AUTHOR]

Molecularly imprinted polymers (MIPs) have garnered the interest of researchers in the drug delivery due to their advantages, such as exceptional durability, stability, and selectivity. In this study, a biocompatible MIP drug adsorption and delivery system with high loading capacity and controlled release, was prepared based on chitosan (CS) and graphene quantum dots (GQDs) as the matrix, and the anticancer drug oxaliplatin (OXAL) as the template. Additionally, samples without the drug (non-imprinted polymers, NIPs) were created for comparison. GQDs were produced using the hydrothermal method, and samples underwent characterization through FTIR, XRD, FESEM, and TGA. Various experiments were conducted to determine the optimal pH for drug adsorption, along with kinetic and isotherm studies, selectivity assessments, in vitro drug release and kinetic evaluations. The highest drug binding capacity was observed at pH 6.5. The results indicated the Lagergren-first-order kinetic model (with rate constant of 0.038 min−1) and the Langmuir isotherm (with maximum adsorption capacity of 17.15 mg g−1) exhibited better alignment with the experimental data. The developed MIPs displayed significant selectivity towards OXAL, by an imprinting factor of 2.88, in comparison to two similar drugs (cisplatin and carboplatin). Furthermore, the analysis of the drug release profile showed a burst release for CS-Drug (87% within 3 h) at pH 7.4, where the release from the CS-GQD-Drug did not occur at pH 7.4 and 10; instead, the release was observed at pH 1.2 in a controlled manner (100% within 28 h). Consequently, this specific OXAL adsorption and delivery system holds promise for cancer treatment. [ABSTRACT FROM AUTHOR]

Lurasidone hydrochloride (LRS HCl), an antipsychotic drug with low aqueous solubility, was dispersed in a matrix of polyethylene glycol (PEG) using the green solvent evaporation method. The green solvents used were water and ethanol. Solid dispersions and physical mixtures were prepared at various drug-to-polymer ratios, characterized by XRPD, FTIR, and DSC analyzes, and then used for the preparation of fast disintegrating tablets (FDTs). The tablets were analyzed for hardness, disintegration, and in vitro dissolution of LRS HCl. In vitro release profiles showed a significant improvement in the release rate of LRS HCl from tablets prepared with solid dispersions compared to those containing untreated LRS HCl or the physical mixture. The presented results confirm that the use of solid dispersions prepared by the green solvent evaporation method is a promising approach to enhance the in vitro dissolution of poorly soluble drugs such as LRS HCl. The applicability of mathematical models was tested to describe the release profiles of LRS HCl from FDTs. The diffusion process, following Fick's law for drug release, appears to be the predominant release mechanism for this specific drug in FDTs. [ABSTRACT FROM AUTHOR]

Copyright of Afyon Kocatepe University Journal of Science & Engineering / Afyon Kocatepe Üniversitesi Fen Ve Mühendislik Bilimleri Dergisi is the property of Afyon Kocatepe University, Faculty of Science & Literature and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

This study aims to develop contact lenses with improved drug-release duration time by layer-by-layer (LBL) coating with natural polymers on contact lenses containing the drug gatifloxacin. LBL coating was performed in single and double layers on contact lenses containing gatifloxaxin using natural polymers carrageenan and polylysine. The performance of contact lenses was evaluated based on various physical properties and antibacterial properties. As a result, contact lenses containing gatifloxacin have reduced physical properties compared to lenses without gatifloxacin. As the concentration of gatifloxacin increased, oxygen permeability and wettability decreased, and antibacterial properties increased. LBL coating improved the wettability and antibacterial properties of contact lenses and increased the drug-release duration. Double-layers coated lenses increased the duration of drug release more than single-coated lenses. Double layer-coating with poly-L-lysine and carrageenan on contact lenses [ABSTRACT FROM AUTHOR]

Copyright of Acta Materiae Compositae Sinica is the property of Acta Materiea Compositae Sinica Editorial Department and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Current transdermal drug delivery technologies, like patches and ointments, effectively deliver low molecular weight drugs through the skin. However, delivering larger, hydrophilic drugs and macromolecules remains a challenge. In the present study, we developed novel transdermal nanoneedle patches containing levofloxacin-loaded modified chitosan nanoparticles. Chitosan was chemically modified with transcutol in three ratios (1/1, 1/2, 1/3, w/w), and the optimum ratio was used for nanoparticle fabrication via the ionic gelation method. The successful modification was confirmed using ATR-FTIR spectroscopy, while DLS results revealed that only the 1/3 ratio afforded suitably sized particles of 220 nm. After drug encapsulation, the particle size increased to 435 nm, and the final formulations were examined via XRD and an in vitro dissolution test, which suggested that the nanoparticles reach 60% release in a monophasic pattern at 380 h. We then prepared transdermal patches with pyramidal geometry nanoneedles using different poly(lactic acid)/poly(ethylene adipate) (PLA/PEAd) polymer blends of varying ratios, which were characterized in terms of morphology and mechanical compressive strength. The 90/10 blend exhibited the best mechanical properties and was selected for further testing. Ex vivo permeation studies proved that the nanoneedle patches containing drug-loaded nanoparticles achieved the highest levofloxacin permeation (88.1%). [ABSTRACT FROM AUTHOR]

Therapeutic options for addressing inflammatory bowel disease (IBD) include the administration of an enema to reduce intestinal inflammation and alleviate associated symptoms. However, uncontrollable retention of enemas in the intestinal tract has posed a long-term challenge for improving their therapeutic efficacy and safety. Herein we have developed a protease-labile hydrogel system as an on-demand enema vehicle with tunable degradation and drug release rates in response to varying matrix metalloproteinase-9 (MMP-9) expression. The system, composed of three tailored hydrogel networks, is crosslinked by poly (ethylene glycol) (PEG) with 2-, 4- and 8-arms through dynamic hydrazone bonds to confer injectability and generate varying network connectivity. The retention time of the hydrogels can be tuned from 12 to 36 h in the intestine due to their different degradation behaviors induced by MMP-9. The drug-releasing rate of the hydrogels can be controlled from 0.0003 mg/h to 0.278 mg/h. In addition, injection of such hydrogels in vivo resulted in significant differences in therapeutic effects including MMP-9 consumption, colon tissue repair, reduced collagen deposition, and decreased macrophage cells, for treating a mouse model of acute colitis. Among them, GP-8/5-ASA exhibits the best performance. This study validates the effectiveness of the tailored design of hydrogel architecture in response to pathological microenvironment cues, representing a promising strategy for on-demand therapy of IBD. The uncontrollable retention of enemas at the delivery site poses a long-term challenge for improving therapeutic efficacy in IBD patients. MMP-9 is highly expressed in IBD and correlates with disease severity. Therefore, an MMP-9-responsive GP hydrogel system was developed as an enema by linking multi-armed PEG and gelatin through hydrazone bonds. This forms a dynamic hydrogel characterized by in situ gelation, injectability, enhanced bio-adhesion, biocompatibility, controlled retention time, and regulated drug release. GP hydrogels encapsulating 5-ASA significantly improved the intestinal phenotype of acute IBD and demonstrated notable therapeutic differences with increasing PEG arms. This method represents a promising on-demand IBD therapy strategy and provides insights into treating diseases of varying severities using endogenous stimulus-responsive drug delivery systems. [Display omitted] [ABSTRACT FROM AUTHOR]

This work focused on synthesizing novel chrysophanol‐loaded composites with varied ratios of polycaprolactone/xanthan gum to enhance the release of chrysophanol. The characteristics of the obtained composites were analyzed by infrared spectroscopy, scanning electron microscopy, transmission electron microscopy, differential scanning calorimetry, rhermogravimetric analysis and dynamic light scattering methods. The xanthan gum/polycaprolactone/chrysophanol (XPC) composites were obtained in the powdery form with particle sizes ranging from 80–100 nm. The results of hydrophilic and hydrophobic tests of the composites were discussed. Chrysophanol, polycaprolactone and xanthan gum can interact and are compatible to each other. XPC composites exhibit high stability and don't cause the negative effect on cells. Additionally, the chrysophanol release and kinetic model of chrysophanol release from the XPC composites in different pH buffer solutions were investigated and evaluated. Using drug carriers such as xanthan gum and polycaprolactone can enhance the release of chrysophanol in both pH 2.0 and pH 7.4 buffer solutions. In the presence of biopolymers, the distribution ability of chrysophanol in aqueous solutions such as pH 2.0 buffer, pH 7.4 buffer solutions, and 0.9 % NaCl solution was enhanced significantly. This will be favorable for an increase in the absorption of chrysophanol in the human body. [ABSTRACT FROM AUTHOR]

Temperature‐responsive hydrogels, or thermogels, have emerged as a leading platform for sustained delivery of both small molecule drugs and macromolecular biologic therapeutics. Although thermogel properties can be modulated by varying the polymer's hydrophilic‐hydrophobic balance, molecular weight and degree of branching, varying the supramolecular donor‐acceptor interactions on the polymer remains surprisingly overlooked. Herein, to study the influence of enhanced hydrogen bonding on thermogelation, we synthesized a family of amphiphilic polymers containing urea and urethane linkages using quinuclidine as an organocatalyst. Our findings showed that the presence of strongly hydrogen bonding urea linkages significantly enhanced polymer hydration in water, in turn affecting hierarchical polymer self‐assembly and macroscopic gel properties such as sol‐gel phase transition temperature and gel stiffness. Additionally, analysis of the sustained release profiles of Aflibercept, an FDA‐approved protein biologic for anti‐angiogenic treatment, showed that urea bonds on the thermogel were able to significantly alter the drug release mechanism and kinetics compared to usage of polyurethane gels of similar composition and molecular weight. Our findings demonstrate the unrealized possibility of modulating gel properties and outcomes of sustained drug delivery through judicious variation of hydrogen bonding motifs on the polymer structure. [ABSTRACT FROM AUTHOR]

Background and Purpose: Designing and manufacturing controlled drug release systems can be highly beneficial in improving drug treatment methods. The aim of this study is to synthesize SBA-16 nanosilica and evaluate its use as a drug carrier for carbamazepine. Additionally, this research aims to assess the effects of pH, contact time, temperature, initial drug concentration, and adsorbent amount on the performance efficiency of the drug carrier. Materials and Methods: In this study, carbamazepine (obtained from the Food and Drug Organization of Iran), double-distilled water, 1-butanol, hydrochloric acid, pluronic copolymer F127, tetraethyl orthosilicate, and sodium hydroxide were used. All chemicals were sourced from Sigma-Aldrich and Merck. A dialysis bag manufactured by Sigma-Aldrich (14000 MWCO, 99.99% retention) was used for drug release experiments. The equipment used in this research includes a digital scale (EJ 303), pH meter (ST 2100), oven (Memmert), magnetic stirrer (HOTPLATE STIRRER 81), electric furnace (Shimaz), FT-IR device (Magna-IR Spectrometer 550 Nicolet), X-ray diffraction device (STADIP), scanning electron microscope (MIRA3-LMU), UV-Vis spectrophotometer (DB20-UV), and BET analyzer (NanoSORD92). SBA-16 was synthesized using the sol-gel method. XRD, FTIR, SEM, and EDX analyses were employed to identify and characterize the synthesized adsorbent. The effects of pH, adsorbent amount (nanocarrier), drug concentration, temperature, and contact time were evaluated using the response surface method (RSM) with the central composite design (CCD) in the Design of Experiments software (DOE) to determine optimal conditions and maximum drug loading capacity. Langmuir, Freundlich, and Temkin adsorption isotherms were used for adsorption studies, and thermodynamic and kinetic studies were also conducted. The dialysis method was applied for drug release experiments, providing physical separation and allowing easy sampling at different time intervals Results: In this study, SBA-16 nanosilica was successfully synthesized, and scanning electron microscope (SEM) images of the SBA-16 surface demonstrated that it had a spherical and homogeneous morphology with particle sizes ranging from 2 to 50 nm. Additionally, the XRD spectrum showed that SBA-16 had a regular structure. Experiment design was used to investigate the effects of key parameters. After conducting the tests, the results were input into the software to generate the best model for evaluating and describing the data. Of the four models (linear, interaction, quadratic, and cubic), the software proposed the quadratic model as the most consistent with the responses. According to the software output, the nanocarrier was able to adsorb 99.87% of carbamazepine under optimal conditions (pH=2, initial drug concentration=20 ppm, drug carrier amount=0.05 g, temperature = 30°C, and contact time=12 minutes). The adsorption data fit the Langmuir isotherm most closely (R²=0.9996). Thermodynamic studies revealed that the adsorption process is spontaneous, exothermic, and physical, following first-order kinetics. The drug release data corresponded with the theoretical kinetic model presented by Zeng et al. (2012) for drug release from mesoporous silica nanoparticles, which assumes an initial burst release in the early hours followed by a slow and steady release. Conclusion: The nanocarrier introduced in this research is a water-insoluble, non-toxic, and highly effective adsorbent for loading the drug carbamazepine. The results demonstrated that, under optimal conditions, the drug loading efficiency reached 99.87%. Additionally, the study showed controlled drug release. The adsorption process followed the Langmuir isotherm with a regression coefficient of 0.9991, while drug release followed the first-order kinetic model with a regression coefficient of 0.9996. Thermodynamic results indicated that the drug loading process is exothermic and spontaneous [ABSTRACT FROM AUTHOR]

Disease's severity, mortality rates, and common failures to achieve clinical improvement during the unprecedented COVID-19 pandemic exposed the emergency need for new antiviral therapeutics with higher efficacy and fewer adverse effects. This study explores the potential to encapsulate multi-component plant extracts in liposomes as optimized delivery systems and to verify if they exert inhibitory effects against human seasonal betacoronavirus OC43 (HCoV-OC43) in vitro. The selection of Sambucus nigra, Potentilla reptans, Allium sativum, Aesculus hippocastanum, and Glycyrrhiza glabra L. plant extracts was based on their established pharmacological and antiviral properties. The physicochemical characterization of extract-loaded liposomes was conducted by DLS and electrokinetics. Encapsulated amounts of the extract were evaluated based on the total flavonoid content (TFC) and total polyphenol content (TPC) by colorimetric methods. The BALB 3T3 neutral red uptake (NRU) phototoxicity/cytotoxicity assay was used to estimate compounds' safety. Photo irritation factors (PIFs) of the liposomes containing extracts were <2 which assigned them as non-phototoxic substances. The antiviral capacities of liposomes containing medicinal plant extracts against HCoV-OC43 were measured by the cytopathic effect inhibition test in susceptible HCT-8 cells. The antiviral activity increased by several times compared to "naked" extracts' activity reported previously. A. hippocastanum extract showed 16 times higher inhibitory properties reaching a selectivity index (SI) of 58.96. Virucidal and virus-adsorption effects were investigated using the endpoint dilution method and ∆lgs comparison with infected and untreated controls. The results confirmed that nanoparticles do not directly affect the viral surface or cell membrane, but only serve as carriers of the active substances and the observed protection is due solely to the intracellular action of the extracts. [ABSTRACT FROM AUTHOR]

Samples of bacterial cellulose with different contents of carboxyl groups have been obtained. The exchange capacity and degree of swelling of these samples were determined. A procedure was developed for the quantitative spectrophotometric determination of CeO2 nanoparticles. The immobilization of CeO2 nanoparticles on oxidized bacterial cellulose was studied. A semi-empirical kinetic model describing the release of nanoparticles from the matrix was formulated. [ABSTRACT FROM AUTHOR]

Starches from underutilized sources such as Bambara nut (BAM) and pigeon pea (PP) can serve as new sources of starch. Starch nanoparticles (SNP) of BAM (BAMnp) and PP (PPnp) are prepared by nanoprecipitation. The physicochemical and pasting properties of the native and SNP are evaluated. The scanning electron microscopy, fourier transform infrared spectroscopy (FTIR), X‐ray diffraction (XRD), drug loading, and release studies of curcumin‐loaded starches and SNP are carried out. The flow, swelling, and solubility of the native starches improve with nanoparticle fabrication. Setback viscosities of the starches are in the order PPnp < BAMnp < PP < BAM. The integrity of the starch granules is maintained after modification. The FTIR of loaded starches shows no interaction between the entities. Reduction in crystallinity of the SNP is observed in the XRD diffractogram. The drug loading efficiency of BAM, PP, BAMnp, and PPnp are 48.55 ± 0.11, 49.00 ± 0.11, 55.44 ± 0.40, and 54.72 ± 0.11, respectively. The drug release is improved when curcumin is loaded on the SNP. The release after 6 h is 33%, 25%, and 2% for BAMnp, PPnp, and pure curcumin, respectively. The properties of the SNP showed that they are potential candidates for the delivery of curcumin, a poorly water soluble drug. [ABSTRACT FROM AUTHOR]

The electrospinning process is an effective technique for creating micro- and nanofibers from synthetic and natural polymers, with significant potential for biomedical applications and drug delivery systems due to their high drug-loading capacity, large surface area, and tunable release times. Poly(L-lactic acid) (PLLA) stands out for its excellent thermo-mechanical properties, biodegradability, and bioabsorbability. Electrospun PLLA nanofibrous structures have been extensively investigated as wound dressings, sutures, drug delivery carriers, and tissue engineering scaffolds. This study aims to create and characterize electrospun PLLA membranes loaded with spironolactone (SP), mimicking active compounds of Ganoderma lucidum (GL), to develop a biodegradable patch for topical wound-healing applications. GL, a medicinal mushroom, enhances dermal wound healing with its bioactive compounds, such as polysaccharides and ganoderic acids. Focusing on GL extracts—obtained through green extraction methods—and innovative drug delivery, we created new fibers for wound-healing potential applications. To integrate complex mixtures of bioactive compounds into the fibers, we developed a prototype using a single pure substance representing the extract mixture. This painstaking work presents the results of the fabricating, wetting, moisture properties, material resilience, and full characterization of the product, providing a robust rationale for the fabrication of fibers imbued with more complex extracts. [ABSTRACT FROM AUTHOR]

3D printing technologies confer an unparalleled degree of control over the material distribution on the structures they produce, which has led them to become an extremely attractive research topic in pharmaceutical dosage form development, especially for the design of personalized treatments. With fine tuning in material selection and careful design, these technologies allow to tailor not only the amount of drug administered but the biopharmaceutical behaviour of the dosage forms as well. While fused deposition modelling (FDM) is still the most studied 3D printing technology in this area, others are gaining more relevance, which has led to many new and exciting dosage forms developed during 2022 and 2023. Considering that these technologies, in time, will join the current manufacturing methods and with the ever-increasing knowledge on this topic, our review aims to explore the advantages and limitations of 3D printing technologies employed in the design and development of pharmaceutical oral dosage forms, giving special focus to the most important aspects governing the resulting drug release profiles. [Display omitted] [ABSTRACT FROM AUTHOR]

Here, a novel kind of composite scaffold was fabricated by loading vascular endothelial growth factor (VEGF) and gastrodin liposome (GAS-LP) into electrospun silk fibroin/graphene oxide(SF/GO)nanofibrous and silk fibroin sponge-filled, respectively. Our results demonstrated that VEGF and GAS exhibited different release patterns in vitro which VEGF showed rapid release rate in the first few days while GAS was released slowly and continuously as encapsulated in liposomes. The scaffolds realized the combination of intraneural vascularization drugs and electrical stimulation effectively, leading to enhanced growth of RSC96 cells. Furthermore, the scaffolds could protect RSC96 cells in an inflammatory environment. [ABSTRACT FROM AUTHOR]

Recently, polymeric multi-layer capsules have gained a great deal of attention from the life science community. Furthermore, myriad interesting systems have appeared in the literature with biodegradable components and biospecific functionalities. In the present work, we presented a mathematical model of drug release from a multi-layer capsule into a target tissue. The diffusion problem was described by a system of coupled partial differential equations, Fickian and non-Fickian, which we solved numerically via nonuniform finite differences method. Energy estimates were further established for the coupled system and also, the convergence properties of the proposed numerical method were justified. We ultimately demonstrated the qualitative behavior of the system. [ABSTRACT FROM AUTHOR]

Drug delivery is the process of introducing bio-active medicinal components into the body of a patient. It is possible to use a variety of natural resources and synthetic materials made from natural resources as the building blocks for creating drug delivery systems (DDs). Liposomal systems are such kinds of DDs consisting of a phospholipid membrane with a hydrophobic tail and a hydrophilic head. Liposomes are lipid-rich spherical or multilayered spherical structures with variations in their size (starting from 2 to > 5000 nm), production techniques, processing, and drug loading. Many advantages of liposomal drug delivery systems over conventional liposomes or free drug treatment of cancer have been discovered as modern drug delivery formulations. Because of their outstanding performance in targeted delivery, liposome nanocarriers have recently displayed excellent drug loading capacity, drug protection, higher bioavailability, enhanced intracellular delivery, and greater therapeutic impact. In this approach, the multifunctional and stimulus-responsive nanocarriers for the drug delivery of cancer treatments improve the effectiveness of treatment, by sustained release of the drug that combats metastases while limiting the systemic negative effects on healthy tissues and organs. This review summarizes the mechanism of liposomal encapsulation of different anticancer drugs, the mechanism of interaction of liposomal anticancer drugs with cancer cells, and also the mechanism of release of drugs from liposomes. The possible disadvantages and future scope of the technique have also been accounted for. [ABSTRACT FROM AUTHOR]

Background and Purpose: Designing and manufacturing controlled drug release systems can be highly beneficial in improving drug treatment methods. The aim of this study is to synthesize SBA-16 nanosilica and evaluate its use as a drug carrier for carbamazepine. Additionally, this research aims to assess the effects of pH, contact time, temperature, initial drug concentration, and adsorbent amount on the performance efficiency of the drug carrier. Materials and Methods: In this study, carbamazepine (obtained from the Food and Drug Organization of Iran), double-distilled water, 1-butanol, hydrochloric acid, pluronic copolymer F127, tetraethyl orthosilicate, and sodium hydroxide were used. All chemicals were sourced from Sigma-Aldrich and Merck. A dialysis bag manufactured by Sigma-Aldrich (14000 MWCO, 99.99% retention) was used for drug release experiments. The equipment used in this research includes a digital scale (EJ 303), pH meter (ST 2100), oven (Memmert), magnetic stirrer (HOTPLATE STIRRER 81), electric furnace (Shimaz), FT-IR device (Magna-IR Spectrometer 550 Nicolet), X-ray diffraction device (STADIP), scanning electron microscope (MIRA3-LMU), UV-Vis spectrophotometer (DB20-UV), and BET analyzer (NanoSORD92). SBA-16 was synthesized using the sol-gel method. XRD, FTIR, SEM, and EDX analyses were employed to identify and characterize the synthesized adsorbent. The effects of pH, adsorbent amount (nanocarrier), drug concentration, temperature, and contact time were evaluated using the response surface method (RSM) with the central composite design (CCD) in the Design of Experiments software (DOE) to determine optimal conditions and maximum drug loading capacity. Langmuir, Freundlich, and Temkin adsorption isotherms were used for adsorption studies, and thermodynamic and kinetic studies were also conducted. The dialysis method was applied for drug release experiments, providing physical separation and allowing easy sampling at different time intervals. Results: In this study, SBA-16 nanosilica was successfully synthesized, and scanning electron microscope (SEM) images of the SBA-16 surface demonstrated that it had a spherical and homogeneous morphology with particle sizes ranging from 2 to 50 nm. Additionally, the XRD spectrum showed that SBA-16 had a regular structure. Experiment design was used to investigate the effects of key parameters. After conducting the tests, the results were input into the software to generate the best model for evaluating and describing the data. Of the four models (linear, interaction, quadratic, and cubic), the software proposed the quadratic model as the most consistent with the responses. According to the software output, the nanocarrier was able to adsorb 99.87% of carbamazepine under optimal conditions (pH=2, initial drug concentration=20 ppm, drug carrier amount=0.05 g, temperature = 30°C, and contact time=12 minutes). The adsorption data fit the Langmuir isotherm most closely (R²=0.9996). Thermodynamic studies revealed that the adsorption process is spontaneous, exothermic, and physical, following first-order kinetics. The drug release data corresponded with the theoretical kinetic model presented by Zeng et al. (2012) for drug release from mesoporous silica nanoparticles, which assumes an initial burst release in the early hours followed by a slow and steady release. Conclusion: The nanocarrier introduced in this research is a water-insoluble, non-toxic, and highly effective adsorbent for loading the drug carbamazepine. The results demonstrated that, under optimal conditions, the drug loading efficiency reached 99.87%. Additionally, the study showed controlled drug release. The adsorption process followed the Langmuir isotherm with a regression coefficient of 0.9991, while drug release followed the first-order kinetic model with a regression coefficient of 0.9996. Thermodynamic results indicated that the drug loading process is exothermic and spontaneous

Abstract The purpose of the current work was to develop and characterize ethosomes of vitamin D3 gel that could more effectively work against psoriasis. Psoriasis is a chronic immune-mediated inflammatory skin disease. Due to vitamin D3 role in proliferation and maturation of keratinocytes, it has become an important local therapeutic option in the treatment of psoriasis. In this research we have initiated worked on ethosomes gels containing vitamin D3 to treat psoriasis. Soya lecithin 1–8% (w/v), propylene glycol and ethanol were used to create the formulations, which were then tested for vesicle size, shape, surface morphology, entrapment effectiveness, and in vitro drug permeation. The drug encapsulation efficiency of ethosomes was 96.25% ± 0.3. The particle sizes of the optimized ethosomes was 148 and 657 nm, and the PDI value was 0.770 ± 0.12 along with negative charge − 14 ± 3. Fourier transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC) along with thermogravimetric analysis (TGA) studies confirmed the absence of interactions between vitamin D3 and other ingredients. It was determined that the total amount of medication that penetrated the membrane was 95.34% ± 3. Percentage lysis was very negligible for all strengths which were found less than 15%. Based on our research, ethosomes appear to be safe for use. The vitamin D3 ethosomal gel order, description, pH, and viscosity were all within the specified ranges, according to the findings of a 6-month investigation into the stability profile of the completed system. In this research, we successfully prepared ethosomes loaded with vitamin D3 and then converted it into gel for patients’ easy applications.

Polypropylene (PP) rapidly gains scientific attention as fatigue-resistant and lightweight tissue repair and implant material, while emerging laser-sintering based methods for PP processing further allow unlimited versatility of PP specimens and often reduced numbers of process steps, substituting traditional manufacturing approaches. Generally, PP is considered biocompatible for a variety of medical applications while showing superior long-term stability, however, thermoplastic processing of polypropylene may induce the formation of cytotoxic degradation products, necessitating its cytotoxicological assessment. In the present study, PP specimens have been fabricated using warm, quasi-isothermal and complementary cold, non-isothermal powder bed fusion (PBF), allowing processing PP at ambient powder bed temperature of 25 °C for minimizing thermal exposure and the formation of decomposition products. The surface of manufactured specimens has been modified with hybrid coatings consisting of mesoporous inorganic microcrystals of vaterite laden with model biomacromolecules, i.e., fluorescently labelled dextran, demonstrating the stable coating and attachment of dextran-loaded vaterite crystals independent of the applied PBF processing regime. Vaterite coating is degradable and enables the opportunity to endow the surface of PP with sustained release functionalities. Both coated and uncoated specimens demonstrated excellent biocompatibility independent of the applied processing regime, as evaluated in an ex ovo shell-less hen's egg model.

Intramolecular bonds in small organic molecules, macromolecules, and organic-inorganic hybrids are broken or formed by ultrasound-activated mechanical force that can be applied with spatial and temporal precision for contactless external control of mechanochemical reactions. Ultrasound featuring non-invasiveness, high tissue penetration, and spatiotemporal controllability has shown great potential in controlling the activation of mechanochemical reactions such as chemical bond scission, natural enzyme activation, and catalytic radical generation for targeted drug or gene therapy. Here, we comprehensively summarize the latest research and future trends in ultrasound-activated mechanochemical reactions for smart biomedical applications. First, the mechanism of ultrasound-activated mechanochemical reactions will be outlined. Then, the types of mechanochemical reactions will be carefully discussed. After that, the representative biomedical applications have been summarized from a unique perspective. Finally, we systematically emphasize the current challenges and future outlooks to guide the rational design of ultrasound-activated drug release over conventional drug-loaded therapies. We believe that this review will substantially facilitate the progression and widespread utilization of ultrasound-activated mechanochemical reactions in biomedical applications.

Recent research is based on biocompatible drug delivery systems due to the need for bioavailability, route of administration, dose dumping, and first-pass metabolism. Despite its excellent mechanical strength, elasticity, and stability, polyurethane has associated risk factors such as high hydrophobic nature and long-term degradability. This review focuses on providing insight into polyurethane as a drug delivery system. The key objective of the review is to signify the importance of polyurethane in biomedical, the essential compounds to synthesize polyurethane, and the types of polyurethane. The review has highlighted polyurethane's drug loading and release capacity and its composites in various forms. The essential biological studies such as polyurethane's antibacterial, antiinflammatory, and anticancer activity were also discussed. Herein, polyurethane and its hybrid composites can be a potential material for future implantable drug delivery systems. [ABSTRACT FROM AUTHOR]

الملخص: أهداف البحث: داساتينيب هو مثبط تيروزين كيناز من الجيل الثاني. إنه يعمل كدواء جزيء صغير متعدد الأهداف من خلال استهداف كينازات التيروزين المختلفة التي تشارك في نمو الخلايا الورمية. وقد وجدت التحقيقات الأخيرة أنه يمنع تكاثر الخلايا السرطانية، والهجرة، ويحفز موت الخلايا المبرمج في مجموعة متنوعة من الأورام الصلبة. ومع ذلك، فهو ضعيف الذوبان في الماء تحت ظروف الرقم الهيدروجيني المختلفة، بالإضافة إلى نصف عمره القصير. لذلك، فإن تطوير نظام توصيل الدواء المحتوي على داساتينيب، ذاتي الاستحلاب يمكن أن يساعد في التغلب على هذه المشكلات في علاج الخلايا السرطانية. طريقة البحث: تم تطوير تركيبات مختلفة لنظام توصيل الدواء ذاتي الاستحلاب ومحملة بداساتينيب باستخدام آيزوبروبيل ميريستات (مرحلة الزيت)، ولابرافيل (الخافض للتوتر السطحي)، والبولي إيثيلين جلايكول (الخافض للتوتر السطحي المشترك). تم تقييم الخواص الفيزيائية والكيميائية للتركيبات من حيث حجم القطرات، وكفاءة التغليف، وإطلاق الدواء في المختبر. تم أيضا تقييم السمية الخلوية للتركيبات على ثلاثة خطوط من الخلايا السرطانية، وسرطان القولون والمستقيم البشري وسرطان الثدي الغدي البشري، بالإضافة إلى خلايا الليفية الرئوية الجنينية البشرية الطبيعية من أجل الانتقائية. النتائج: داساتينيب-تركيبة نظام توصيل الدواء ذاتي الاستحلاب، تتميز بحجم جسيم جيد، وكفاءة تغليف، وإطلاق دواء في المختبر. في فهمنا، أظهرت هذه الدراسة أن فعالية داساتينيب المضادة للسرطان - نظام الاستحلاب الذاتي، ونظام توصيل الدواء كان لها تأثيرات أفضل على السمية الخلوية على خطوط الخلايا السرطانية الثلاثة، وسرطان الثدي الغدي البشري، وسرطان القولون والمستقيم البشري، مقارنة مع داساتينيب النقي. الاستنتاجات: من المحتمل أن تكون تركيبات نظام توصيل الدواء داساتينيب-الاستحلاب الذاتي، فعالة كطريقة مستدامة لتوصيل الدواء لعلاج السرطان. Abstract: Background/Aim: Dasatinib (DS), a second-generation tyrosine kinase inhibitor, functions as a multi-target small-molecule drug via targeting various tyrosine kinases involved in neoplastic cell growth. DS inhibits cancer cell replication and migration, and induces tumor cell apoptosis in a variety of solid tumors. However, it is poorly soluble in water under some pH values. Therefore, the development of a DS-containing, self-emulsifying, drug delivery system (SeDDs) could help overcome these problems in treating cancer cells. Methods: Various SeDD formulations loaded with DS were developed with isopropyl myristate (oil phase), Labrafil (surfactant), and polyethylene glycol (co-surfactant). The physicochemical properties of the formulations were assessed according to droplet size, encapsulation efficiency, and in vitro drug release. The cytotoxicity of the formulations on the cancer cell lines HT29 and SW420 (human colorectal carcinoma), and MCF7 (human breast adenocarcinoma), in addition to MRC5 normal human fetal lung fibroblasts, was evaluated to assess selectivity. Results: The DS-SeDD formulation showed favorable particle size, encapsulation efficiency, and in vitro drug release. The anti-cancer potency of DS-SeDDs had greater cytotoxicity effects than pure DA on the three cancer cell lines, MCF7, HT29, and SW420l. Conclusion: The developed DS-SeDD formulations may potentially be an effective sustained drug delivery method for cancer therapy.

Abstract β-glucans are polysaccharides found in the cell walls of various fungi, bacteria and cereals. β-glucan have been found to show various kinds of anti-inflammatory, antimicrobial, antidiabetic antioxidant and anticancerous activities. In the present study, we have isolated β-glucan from the baker’s yeast Saccharomyces cerevisiae and white button mushroom Agaricus bisporus and tested their antioxidant potential and anticancerous activity against prostate cancer cell line PC3. Particles were characterized with zeta sizer and further with FTIR that confirmed that the isolated particles are β-glucan and alginate sealing made slow and sustained release of the Quercetin from the β-glucan particles. Morphological analysis of the hollow and Quercetin loaded β-glucan was performed with the SEM analysis and stability was analyzed with TGA and DSC analysis that showed the higher stability of the alginate sealed particles. Assessments of the antioxidant potential showed that Quercetin loaded particles were having higher antioxidant activity than hollow β-glucan particles. Cell viability of the PC3 cells was examined with MTT assay and it was found that Quercetin loaded alginate sealed Agaricus bisporus derived β-glucan particles were having lowest IC50. Further ROS generation was found to increase in a dose dependent manner. Apoptosis detection was carried out with Propidium iodide and AO/EtBr staining dye which showed significant death in the cells treated with higher concentration of the particles. Study showed that particles derived from both of the sources were having efficient anticancer activity and showing a dose dependent increase in cell death in PC3 cells upon treatment.

Abstract Nanogels offer hope for precise drug delivery, while addressing drug delivery hurdles is vital for effective prostate cancer (PCa) management. We developed an injectable elastin nanogels (ENG) for efficient drug delivery system to overcome castration-resistant prostate cancer (CRPC) by delivering Decursin, a small molecule inhibitor that blocks Wnt/βcatenin pathways for PCa. The ENG exhibited favourable characteristics such as biocompatibility, flexibility, and low toxicity. In this study, size, shape, surface charge, chemical composition, thermal stability, and other properties of ENG were used to confirm the successful synthesis and incorporation of Decursin (DEC) into elastin nanogels (ENG) for prostate cancer therapy. In vitro studies demonstrated sustained release of DEC from the ENG over 120 h, with a pH-dependent release pattern. DU145 cell line induces moderate cytotoxicity of DEC-ENG indicates that nanomedicine has an impact on cell viability and helps strike a balance between therapeutics efficacy and safety while the EPR effect enables targeted drug delivery to prostate tumor sites compared to free DEC. Morphological analysis further supported the effectiveness of DEC-ENG in inducing cell death. Overall, these findings highlight the promising role of ENG-encapsulated decursin as a targeted drug delivery system for CRPC.

The purpose of this in vitro study was to develop calcium sulfate (CS)-based disks infused with an antimicrobial drug, which can be used as a post-surgical treatment modality for osteomyelitis. CS powder was embedded with 10% antibiotic, amoxicillin (AMX) or moxifloxacin (MFX), to form composite disks 11 mm in diameter that were tested for their degradation and antibiotic release profiles. For the disk degradation study portion, the single drug-loaded disks were placed in individual meshes, subsequently submerged in phosphate-buffered saline (PBS), and incubated at 37 °C. The disks were weighed once every seven days and analyzed via Fourier-transform infrared spectroscopy, X-ray diffraction, energy dispersive X-ray spectroscopy, and scanning electron microscopy. During the antibiotic release analysis, composite disks were placed in PBS solution, which was changed every 3 days, and analyzed for antibiotic activity and efficacy. The antibacterial effects of these sustained-release composites were tested by agar diffusion assay using Streptococcus mutans (S. mutans) UA 159 as an indicator strain. The degradation data showed significant increases in the degradation of all disks with the addition of antibiotics. Following PBS incubation, there were significant increases in the amount of phosphate and decreases in the amount of sulfate. The agar diffusion assay demonstrated that the released concentrations of the respective antibiotics from the disks were significantly higher than the minimum inhibitory concentration exhibited against S. mutans over a 2–3-week period. In conclusion, CS-antibiotic composite disks can potentially serve as a resorbable, osteoconductive, and antibacterial therapy in the treatment of bone defects and osteomyelitis. [ABSTRACT FROM AUTHOR]

Silybin is a natural flavonolignan with potential anticancer, antioxidant, and hepatoprotective properties. In the present study, various loadings of silybin (1, 3, and 5 wt%) were encapsulated in poly-ε-caprolactone (PCL) fibers by electrospinning, in order to produce new pharmaceutical composites with improved bioactive and drug delivery properties. The morphological characteristics of the composite fibrous structures were evaluated by scanning electron microscopy (SEM), and the encapsulation efficiency and the release rate of silybin were quantified using a UV-Vis spectrophotometer. The analysis of the membranes' thermal behavior by differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) revealed the existence of interaction between PCL and silybin. An investigation of the cytocompatibility of the composite membranes revealed that normal cells displayed an unimpeded proliferation in the respective silybin concentrations; however, tumor cell growth demonstrated a dose-dependent inhibition. Furthermore, an effective antioxidant activity against hydrogen peroxide-induced oxidative stress in HEK-293 cells was observed for the prepared electrospun fibrous mats. [ABSTRACT FROM AUTHOR]

Introduction: In recent years, the development of drug-eluting embolization beads that can be imaged has become a hot research topic in regard to meeting clinical needs. In our previous study, we successfully developed nano-assembled microspheres (NAMs) for multimodal imaging purposes. NAMs can not only be visualized under CT/MR/Raman imaging but can also load clinically required doses of doxorubicin. It is important to systematically compare the pharmacokinetics of NAMs with those of commercially available DC Beads and CalliSpheres to evaluate the clinical application potential of NAMs. Methods: In our study, we compared NAMs with two types of drug-eluting beads (DEBs) in terms of irinotecan, drug-loading capacity, release profiles, microsphere diameter variation, and morphological characteristics. Results: Our results indicate that NAMs had an irinotecan loading capacity similar to those of DC Beads and CalliSpheres but exhibited better sustained release in vitro. Conclusion: NAMs have great potential for application in transcatheter arterial chemoembolization for the treatment of colorectal cancer liver metastases. [ABSTRACT FROM AUTHOR]

Light‐activated drug delivery systems allow precise spatiotemporal control of a drug release process. However, safe and efficient drug release activation needs a low‐power nonpulsed red/near‐infrared light with high tissue penetration depth. Nevertheless, such systems remain a challenge. Herein, a self‐assembled nanovehicle made of 2,6‐diiodo‐B‐dimethyl‐boron dipyrromethene (BODIPY)‐based photocleavable trigonal molecules bearing Pt(II) meso‐tetraphenyltetranaphthoporhyrin photosensitizer and a fluorescent release marker Nile Red in hydrophobic core is introduced. The system employs endothermic triplet–triplet energy transfer between the photosensitizer and the trigonal molecule, leading to the cleavage of the trigonal molecule followed by cargo release. This allows to engage 730 nm light to cleave BODIPY photoremovable protecting groups (PPGs) instead of 530 nm light that would be needed for direct photocage excitation. Therefore, the approach unleashes the desired activation of drug release via photocleavage with longer wavelengths (within the phototherapeutic window) without any chemical modification of the PPGs. Cell studies demonstrate fast intracellular uptake of the nanovehices by PC3 human prostate cancer cells with accumulation in lysosomes in 2 h. Light irradiation at 730 nm on nanovehicles dispersed in cell media leads to payload release. Remarkably, the system exhibits higher release efficiency at low oxygen concentration than at ambient thus allowing to tackle aggressive hypoxic solid tumors. [ABSTRACT FROM AUTHOR]

A strategy for the preparation of a hybrid chitosan/silica nanohydrogel is reported, which combines the gelation of chitosan in a nanoemulsion system with a sol–gel process to produce silica. Chitosan is used as a biopolymer matrix, while silica acts as a structuring additive. Hydrogel nanocapsules are obtained through the ionic interaction of the cationic groups of chitosan with the anionic groups of sodium triphosphate (STP), which is used as a physical cross‐linker. Two alternative preparation methods are compared in this work: in the first one, STP is added to the continuous phase of an inverse emulsion of chitosan; in the second one, the fusion of droplets of two emulsions containing separate chitosan and STP takes place. The size of the obtained nanocapsules ranges from 50 to 200 nm. The efficiency of the formed hydrogel for entrapping a hydrophilic model substance (erioglaucine disodium salt) is investigated for the two systems by studying the release in a neutral aqueous medium. The results indicate that the hydrophilic cargo is efficiently encapsulated by both preparation methods, although the droplet‐fusion method yields more stable suspensions. As a general observation, the release behavior of erioglaucine is systematically retarded when silica is present in the systems. [ABSTRACT FROM AUTHOR]

Hydrogel films with a polymer base of corn starch and poly(vinyl alcohol) (50:50 wt%), citric acid as a crosslinking agent, and glycerin as a plasticizer were synthesized. Their physical and mechanical characteristics corresponded to the performance level of commercial wound dressings of the same type. The degree of swelling increased by ~30%, whereas the elastic modulus and water-vapor permeability decreased by ~60% when ethonium was introduced into the polymer matrix (from 1 to 5 wt% of the polymer weight). Drug release from the polymer matrix occurred within 90-105 min at drug contents of 2.5-5 wt%. The developed films inhibited the growth of the microorganisms E. coli and P. aeruginosa. [ABSTRACT FROM AUTHOR]

OBJECTIVES Our objective was to explore the safety and efficacy of a graphene oxide-loaded rapamycin-coated self-expandable metallic airway stent (GO@RAPA-SEMS) in a rabbit model. METHODS The dip coating method was used to develop a GO@RAPA-SEMS and a poly(lactic-co-glycolic)-acid loaded rapamycin-coated self-expandable metallic airway stent (PLGA@RAPA-SEMS). The surface structure was evaluated using a scanning electronic microscope. The in vitro drug-release profiles of the 2 stents were explored and compared. In the animal study, a total of 45 rabbits were randomly divided into 3 groups and underwent 3 kinds of stent placements. Computed tomography was performed to evaluate the degree of stenosis at 1, 2 and 3 months after the stent operation. Five rabbits in each group were sacrificed after the computed tomography scan. The stented trachea and blood were collected for further pathological analysis and laboratory testing. RESULTS The in vitro drug-release study revealed that GO@RAPA-SEMS exhibited a sudden release on the first day and maintained a certain release rate on the 14th day. The PLGA@RAPA-SEMS exhibited a longer sustained release time. All 45 rabbits underwent successful stent placement. Pathological results indicated that the granulation tissue thickness in the GO@RAPA-SEMS group was less than that in the PLGA@RAPA-SEMS group. The TUNEL and hypoxia-inducible factor-1α staining results support the fact that the granulation inhibition effect in the GO@RAPA-SEMS group was greater than that in the PLGA@RAPA-SEMS group. CONCLUSIONS GO@RAPA-SEMS effectively inhibited stent-related granulation tissue hyperplasia. [ABSTRACT FROM AUTHOR]

The ultrasound (US)‐induced activation of mechanophores embedded in linear polymers (LPs) is the most widely employed technique to realize chemical function by polymer mechanochemistry. However, the commonly used US frequency in this context is around 20 kHz, producing strong inertial cavitation limiting biomedical applicability. Herein, 20 kHz US and 1.5 MHz high‐intensity focused US (HIFU) are investigated to drive disulfide mechanophore activation and mechanochemical polymer chain scission in network core‐structured star polymers (NCSPs). It is found that the efficiency of activating disulfide mechanophores in NCSPs using 1.5 MHz HIFU irradiation is similar to the efficiency achieved with 20 kHz sonication. This is quantified by 'turn on' sensor molecules leveraging the Michael addition of the mechanochemically generated thiol groups and subsequent retro Diels–Alder reaction to release a fluorophore. Moreover, the anticancer drug doxorubicin (Dox) covalently loaded into NCSPs is efficiently released by 1.5 MHz HIFU. Finally, an in vitro study of drug release from NCSPs is performed, demonstrating the potential of HIFU‐activated polymer mechanochemistry for sonopharmacology. [ABSTRACT FROM AUTHOR]

Fiber-based technologies are widely used in various industries, but their use in pharmaceuticals remains limited. While melt extrusion is a standard method for producing medical fibers such as sutures, it is rarely used for pharmaceutical fiber-based dosage forms. The EsoCap system is a notable exception, using a melt-extruded water-soluble filament as the drug release trigger mechanism. The challenge of producing drug-loaded fibers, particularly due to the use of spinning oils, and the processing of the fibers are addressed in this work using other approaches. The aim of this study was to develop processes for the production and processing of pharmaceutical fibers for targeted drug delivery. Fibers loaded with polyvinyl alcohol and fluorescein sodium as a model drug were successfully prepared by a continuous melt extrusion process and directly spun. These fibers exhibited uniform surface smoothness and consistent tensile strength. In addition, the fibers were further processed into tubular dosage forms using a modified knitting machine and demonstrated rapid drug release in a flow cell. [ABSTRACT FROM AUTHOR]

Chitosan nanoparticles (CSNPs) are promising vehicles for targeted and controlled drug release. Recognized for their biodegradability, biocompatibility, low toxicity, and ease of production, CSNPs represent an effective approach to drug delivery. Encapsulating drugs within nanoparticles (NPs) provides numerous benefits compared to free drugs, such as increased bioavailability, minimized toxic side effects, improved delivery, and the incorporation of additional features like controlled release, imaging agents, targeted delivery, and combination therapies with multiple drugs. Keys parameters in nanomedicines are drug loading content and drug loading efficiency. Most current NP systems struggle with low drug loading, presenting a significant challenge to the field. This review summarizes recent research on developing CSNPs with high drug loading capacity, focusing on various synthesis strategies. It examines CSNP systems using different materials and drugs, providing details on their synthesis methods, drug loadings, encapsulation efficiencies, release profiles, stability, and applications in drug delivery. Additionally, the review discusses factors affecting drug loading, providing valuable guidelines for future CSNPs' development. [ABSTRACT FROM AUTHOR]

Accurately measuring drug and its release kinetics in both in vitro and in vivo environments is crucial for enhancing therapeutic effectiveness while minimizing potential side effects. Nevertheless, the real-time visualization of drug release from microspheres to monitor potential overdoses remains a challenge. The primary objective of this investigation was to employ fluorescence imaging for the real-time monitoring of drug release from microspheres in vitro, thereby simplifying the laborious analysis associated with the detection of drug release. Two distinct varieties of microspheres were fabricated, each encapsulating different drugs within PLGA polymers. Cy5 was selected as the donor, and Cy7 was selected as the acceptor for visualization and quantification of the facilitated microsphere drug release through the application of the fluorescence resonance energy transfer (FRET) principle. The findings from the in vitro experiments indicate a correlation between the FRET fluorescence alterations and the drug release profiles of the microspheres. [ABSTRACT FROM AUTHOR]

Compared to other forms of drug administration, the use of Transdermal Drug Delivery Systems (TDDSs) offers significant advantages, including uniform drug release profiles that contribute to lower side effects and higher tolerability, avoidance of direct exposure to the gastrointestinal tract, better patient compliance due to their non-invasive means of application and others. Mesoporous silica membranes are of particular interest in this regard, due to their chemical stability and their tunable porous system, with adjustable pore sizes, pore volumes and surface chemistries. While this allows for fine-tuning and, thus, the development of optimized TDDSs with high loading capacities and the desired release profile of a given drug, its systemic availability also relies on skin penetration. In this paper, using a TDDS based on mesoporous silica membranes in Franz cell experiments on porcine skin, we demonstrate surprisingly substantial drug loss during skin penetration. Drug passage through porcine skin was found to be dependent on the age and pre-treatment of the skin. pH and temperature were major determinants of drug recovery rates as well, indicating drug loss in the skin by enzymatic metabolization. Regarding the TDDS, higher loading obtained by SO3H surface modification of the mesoporous silica membranes reduced drug loss. Still, high loss rates in the skin were determined for different drugs, including anastrozole, xylazine and imiquimod. We conclude that, beyond the fine-tuned drug release profiles from the mesoporous silica membrane TDDS, remarkably high drug loss in the skin is a major issue for achieving desired skin penetration and, thus, the systemic availability of drugs. This also poses critical requirements for defining an optimal TDDS based on mesoporous silica membranes. [ABSTRACT FROM AUTHOR]

The present study aimed to create a more sustainable and controlled delivery system based on natural biopolymer bacterial nanocellulose (BNC) and bacterial natural product actinomycin (Act), with the applicative potential in the biomedical field. In order to provide improved interaction between BNC and the active compound, and thus to modulate the release kinetics, the TEMPO oxidation of BNC support was carried out. A mix of actinomycins from bacterial fermentation (ActX) were used as natural antimicrobial agents with an established bioactivity profile and clinical use. BNC and TEMPO-oxidized BNC films with incorporated active compounds were obtained and analyzed by FTIR, SEM, XPS, and XRD. The ActX release profiles were determined in phosphate-buffer solution, PBS, at 37 °C over time. FTIR analysis confirmed the improved incorporation and efficiency of ActX adsorption on oxidized BNC due to the availability of more active sites provided by oxidation. SEM analysis indicated the incorporation of ActX into the less-dense morphology of the TEMPO-oxidized BNC in comparison to pure BNC. The release kinetics of ActX were significantly affected by the BNC structure, and the activated BNC sample indicated the sustained release of active compounds over time, corresponding to the Fickian diffusion mechanism. Antimicrobial tests using Staphylococcus aureus NCTC 6571 confirmed the potency of this BNC-based system for biomedical applications, taking advantage of the capacity of modified BNC to control and modulate the release of bioactive compounds. [ABSTRACT FROM AUTHOR]