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The development of chitosan-coated nanoliposomes has emerged as a promising strategy for enhancing the intranasal delivery of therapeutic agents targeting the central nervous system. In this study, optimized Levetiracetam-loaded nanoliposomes (Opt-LEV-NLs) were coated with 0.1% and 0.3% chitosan to improve nasal uptake and mucoadhesion. The formulations were evaluated for vesicle size, entrapment efficiency, invitro release, surface morphology, zeta potential, and pH to select the best formulation for brain targeting. Results demonstrated that 0.1% chitosan-coated nanoliposomes (Chit-NLs) retained an optimal particle size (151.72 ± 1.37 nm), suitable for nasal delivery, with a satisfactory entrapment efficiency (64.56 ± 1.03%) and effective drug release (82.51 ± 2.15%). In contrast, 0.3% Chit-NLs exhibited larger particle sizes (> 300 nm), lower release rates, and reduced suitability for intranasal delivery. TEM and zeta potential analyses confirmed the successful chitosan coating and improved mucoadhesive properties. Based on these findings, 0.1% Chit-NLs were selected as the optimized formulation for further studies. This research supports the potential of chitosan-coated nanoliposomes for enhancing the bioavailability of Levetiracetam via the intranasal route. [ABSTRACT FROM AUTHOR]

Background: Oral thrush, caused by Candida albicans, is currently treated under guidelines by using topical antifungal pharmaceutical formulations such as lozenges and liquid gargles. Using these drugs may cause irritation and adverse reactions. Moreover, there is a short exposure time to reach the lesion, which may result in low effectiveness of the treatment. Therefore, the research group aimed to develop mouthwash solutions that can form gel at oral temperature containing Zingiber zerumbet rhizome extracts, which work as an active substance inhibiting fungi. Methods: The development process began with the extraction of substances from Zingiber zerumbet rhizome using hexane and the analysis of the active substance by HPLC. Antifungal and anti-inflammatory activities of the extracts were evaluated. Hydrogel mouthwash was prepared by varying the type and concentration of polymer, solvent, and mucoadhesive agent. The optimized formulation was then evaluated for its properties. Results: Zingiber zerumbet rhizome extracts, containing 16.29±0.39 % zerumbone, demonstrated both antifungal and anti-inflammatory activities against Candida albicans. The extract also had anti-inflammatory activity when tested by the proteinase inhibitory test, with a percentage inhibition of 86.15±10.96 %. Two thermosensitive hydrogels, poloxamer P407 and P188, were applied and compared as gel-forming agents. It was found that the optimized formulation is composed of 15 % (w/w) poloxamer P407, 0.05 % (w/w) carbopol as a mucoadhesive agent, and 5 % (v/v) ethanol. Transition time and transition temperature of the optimized thermosensitive hydrogel formula were 27.76±1.25 s and 36±1.00 °C, respectively. The viscosity at shear rate 1 S-1 and 25 °C of the optimized formulation was 0.13±0.06 Pa.s, which is suitable for pouring out of the bottle and gargling. Conclusion: This study demonstrates a novel approach to developing thermosensitive hydrogel mouthwash formulations, leveraging Zingiber zerumbet rhizome extracts for enhanced therapeutic efficacy against oral candidiasis. These formulations offer prolonged contact time with affected areas, potentially improving treatment outcome.

Introduction: The aim of this study was to develop an optimized formulation for labeling a third-generation bisphosphonate, zoledronic acid with [99mTc] Tc to achieve the best formulation in preparing an ideal skeletal radiotracer. Radiocomplex yield and purity, stability, biodistribution and imaging in normal rat were investigated. Methods: The samples containing different amounts of zoledronic acid, ascorbic acid and stannous chloride were prepared and labeled with [99mTc]technetium pertechnetate. TLC methods were used to determine the radiochemical purity. The stability was determined in saline and human serum solutions. Lipophilicity was calculated by measuring radio-complex that was divided between organic and aqueous phases. In vitro bone affinity was studied through hydroxyapatite binding assays. Considering the decomposition of radioactivity, biodistribution of radio-complex was assessed based on the percentage of injected activity per gram of organ (% IA/g). Results: [99mTc]Tc-zoledronic acid was prepared easily with high yield while 100 µg, 0.34 µmol of zoledronic acid as a ligand and 100 µg, 0.44 µmol SnCl2 as a reducing agent were used. Radiochemical purity of radio-complex was more than 99% with specific activity of 8050 MBq/µmol. The radio-complex showed rapid blood washout along with high bone uptake value (4.53 ± 0.14 % IA/g at 2 h post injection). Conclusion: Under optimized condition, [99mTc]Tc-zoledronic acid was prepared with high purity and stability together with high bone affinity and rapid blood clearance, make this radio-complex an ideal agent with great potential for skeletal imaging. [ABSTRACT FROM AUTHOR]

The recent advances in ocular drug delivery have been successful in surpassing conventional therapy, owing to its considerable limitations. This study aims to develop and optimize in-situ liposomal ocular system to design once-daily liquid preparation to treat Keratoconjunctivitis sicca. Liposomes of Hyaluronic acid were prepared using soya lecithin by a thin film hydration method. Eight trial formulations were made by keeping drug as fixed ratio and varying the concentration of cholesterol and soya lecithin. The optimized formulation was selected for the formulation of liposomal in-situ hydrogel. Optimization was carried out by Central Composite Design (CCD) studying the factors, amount of cholesterol and soya lecithin and its effects on the responses, % Invitro drug release (R1) and Percent Entrapment Efficiency (% EE) (R2). The best predicted model for R1 was the Quadratic model and, for R2 was Two-Factor Interaction model (2FI) without any significant lack of fit. Optimum formulation was found to be at 1:1:4 (drug: cholesterol: soya lecithin) showed sustained drug release of 31.28% in 8 hours with highest %EE of 47.36%. Liposomal in-situ gel preparation retained better stability throughout the study period when stored at refrigerator temperature and displayed prolonged action (76.44%) when compared to liposomal formulation (68.72%). [ABSTRACT FROM AUTHOR]

This study was carried out to optimize formulation for Heracleum lasiopetalum (golpar) extract nanoencapsulation by response surface methodology (RSM). The primary water‐in‐oil emulsion was fabricated by (5%–10%) golpar extract (GE), (40%–35%) emulsifier span 80 (EM), and (50%–60%) sunflower oil (SO). The coating materials were the mixture of Lepidium sativum seed gum (LSG) and whey protein concentrate (WPC) at different ratios (1:0, 1:1, and 0:1). The yield of nanoencapsulation of GE, particle size, and zeta potential was investigated as responses of RSM. The optimal formulation for water‐in‐oil‐in‐water emulsion of GE were SO: 50.46%, GE 9.52%, and EM: 36.30% in LSG, SO: 57.07%, GE: 7.12%, and EM: 30.85% in LSG:WPC, and SO: 54.98%, GE: 9.05%, and EM: 39.87% in WPC coating. In conclusion, the nanoencapsulation of GE prepared with the optimized formulation by RSM ensures the gradual release and higher stability to sedimentation during storage with nanometric size and high yield of encapsulation. The nanocapsules of GE can be used as a natural antioxidant in food systems. [ABSTRACT FROM AUTHOR]

In this work, we are interested in describing the evolution of the rheological behavior of geopolymer materials since their elaboration until the start of their kinetics of setting. We considered the case where these materials are obtained from the dissolution of a quantity S of metakaolin in a quantity L of alkaline activation solution (sodium-based). In this context and for all the values of the structural identification parameters P = (% Na2O) and R3 = (L/S) in our experiments, it has been established that the rheological behavior is described by the viscoplastic Herschel-Bulkley model. In particular, we have been able to determine how rheological parameters of the model are affected by variations of P and / or R3. For the considered formulations, this analysis is of importance insofar as it was at the base of the identification of critical values of P and R3. Moreover, we verified that for these values, the setting time is maximum. This result is retained to define the optimized formulation of our materials.

The main purpose of this study is to develop and optimize a luminescent road-marking paint to improve the visibility of the traditional used road-marking paint. This paint is produced with an emulsion of an acrylic copolymer containing a self-made modified luminescent powder and various additives. Experimental coatings were manufactured on a laboratory scale and applied using a brush on tinplate panels and asphalt concrete surface. Results found a series of properties which indicated that the paint made with the additives containing sodium hexametaphosphate and sodium carboxymethyl cellulose exhibited a satisfactory performance when mixed with silicone emulsion. The physical, mechanical and corrosion resistance was studied in order to evaluate the feasibility of application onto the road surface. The results show that the paint meets the basic performance requirements of road-marking paint and has little effect on the texture depth of the road surface. The luminous performance, abrasion resistance, adhesion and water resistance at room temperature meets the basic requirements for pavements. [ABSTRACT FROM AUTHOR]

An in-situ forming implant of buprenorphine was prepared by combining PLGA RG756s and PLGA RG504H copolymers, and additives that decreased the initial burst release. The optimum formulation was achieved based on a minimum initial burst release of BP in the in-vitro release medium using a Box-Behnken design. The in-vitro, ex-vivo, and in-vivo release of the optimized formulation was investigated. The rabbit-blood concentrations of the optimized formulation and RBP-6000 (PLGA 504H) were compared to ensure their equivalency. The results indicate that the optimized formulation can reach an effective therapeutic concentration for treating opioid dependence with minimum initial burst release. [ABSTRACT FROM AUTHOR]

Celastrol (CL), a bioactive compound isolated from Tripterygium wilfordii, has demonstrated bioactivities against a variety of diseases including cancer and obesity. However, its poor water solubility and rapid in vivo clearance limit its clinical applications. To overcome these limitations, nanotechnology has been employed to improve its pharmacokinetic properties. Nanoparticles made of biological materials offer minimal adverse effects while maintaining the efficacy of encapsulated therapeutics. Silk fibroin (SF) solution was prepared successfully by extraction from the cocoons of silkworms, and a final concentration of 2 mg/mL SF solution was used for the preparation of CL-loaded SF nanoparticles (CL-SFNP) by the desolvation method. A stirring speed of 750 rpm and storage time of 20 h at −20 °C resulted in optimized product yield. A high-performance liquid chromatography (HPLC) method was developed and validated for the analysis of CL in rat plasma in terms of selectivity, linearity, intra-/inter-day precision and accuracy, and recovery. No interference was observed in rat plasma. Linearity in the concentration range of 0.05−5 µg/mL was observed with R2 of 0.999. Precision and accuracy values were below the limit of acceptance criteria, i.e., 15% for quality control (QC) samples and 20% for lower limit of quantification (LLOQ) samples. Rats were given intravenous (IV) administration of 1 mg/kg of pure CL in PEG 300 solution or CL-SFNP. The pharmacokinetic profile was improved with CL-SFNP compared to pure CL. Pure CL resulted in a maximum concentration (Cmax) value of 0.17 µg mL−1 at 5 min following administration, whereas that for CL-SFNP was 0.87 µg mL−1 and the extrapolated initial concentrations (C0) were 0.25 and 1.09 µg mL−1, respectively, for pure CL and CL-SFNP. A 2.4-fold increase in total area under the curve (AUC0-inf) (µg h mL−1) was observed with CL-SFNP when compared with pure CL. CL-SFNP demonstrated longer mean residence time (MRT; 0.67 h) than pure CL (0.26 h). In conclusion, the preparation of CL-SFNP was optimized and the formulation demonstrated improved pharmacokinetic properties compared to CL in solution following IV administration.

Paeonol exhibits a wide range of pharmacological activities, such as anti-inflammatory, antidiabetic as well as pain-relieving activities. However, its intrinsic properties, such as low water solubility, poor stability and low oral bioavailability, restrict its clinical application. The current study aimed to optimize paeonol-loaded ethosomal formulation and characterize it in terms of encapsulation efficiency (EE), vesicle size (VS), zeta potential (ZP) and polydispersity index (PDI), in addition to differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FT-IR) studies. Here, paeonol-loaded ethosomes were prepared by the injection method and optimized by the single-factor test and central composite design-response surface methodology. The optimized paeonol-loaded ethosomes had an EE of 84.33 ± 1.34%, VS of 120.2 ± 1.3 nm, negative charge of −16.8 ± 0.36 mV, and PDI of 0.131 ± 0.006. Ethosomes showed a spherical morphology under the transmission electron microscope (TEM). DSC, XRD and FT-IR results indicated that paeonol was successfully incorporated into the ethosomes. In-vitro transdermal absorption and skin retention of paeonol from paeonol-loaded ethosomes were 138.58 ± 9.60 µg/cm2 and 52.60 ± 7.90 µg/cm2, respectively. With reasonable skin tolerance, ethosomes could be a promising vehicle for transdermal delivery of paeonol.

The optimization of oral dosage form formulation has been developed for N-4472, N-[2-(3,5-di-tert-butyl-4-hydroxyphenethyl)-4,6-difluorophenyl]-N′-[4-(N-benzylpiperidyl)] urea, which was a poorly water-soluble drug having a lipid-lowering effect. Formulations that contained various surfactants and water-soluble polymers were prepared and the solubility of N-4472 was evaluated in JP XIV first fluid (pH 1.2), JP XIV second fluid (pH 6.8), and distilled water. The highest solubility of N-4472 was achieved when l-ascorbic acid (VC), Gelucire® 44/14, and HCO-60® were used as additives. It was confirmed that this formulation could create microemulsion droplets with a mean droplet size of approximately 20 nm and a sharp droplet distribution pattern in JP XIV first fluid, JP XIV second fluid, and distilled water. When JP XIV second fluid was used as a dissolution medium, however, an eventual decrease of solubility was observed, that is, the fluid became white and cloudy as time passed. It was found that the addition of sodium dodecyl sulfate (SDS) was effective to prevent the lowering of solubility, and that a weight ratio of 1.0/1.5/11.4/4.9/3.8 for N-4472/VC/Gelucire® 44/14/HCO-60®/SDS was optimum for the self-microemulsifying formulation. It was assumed that electrostatic repulsion of microemulsion droplets and an increase of the cloud point by the addition of SDS were responsible for the successful formation of a stable microemulsion. [Copyright &y& Elsevier]

Celastrol (CL), a bioactive compound isolated from Tripterygium wilfordii, has demonstrated bioactivities against a variety of diseases including cancer and obesity. However, its poor water solubility and rapid in vivo clearance limit its clinical applications. To overcome these limitations, nanotechnology has been employed to improve its pharmacokinetic properties. Nanoparticles made of biological materials offer minimal adverse effects while maintaining the efficacy of encapsulated therapeutics. Silk fibroin (SF) solution was prepared successfully by extraction from the cocoons of silkworms, and a final concentration of 2 mg/mL SF solution was used for the preparation of CL-loaded SF nanoparticles (CL-SFNP) by the desolvation method. A stirring speed of 750 rpm and storage time of 20 h at −20 °C resulted in optimized product yield. A high-performance liquid chromatography (HPLC) method was developed and validated for the analysis of CL in rat plasma in terms of selectivity, linearity, intra-/inter-day precision and accuracy, and recovery. No interference was observed in rat plasma. Linearity in the concentration range of 0.05–5 µg/mL was observed with R2 of 0.999. Precision and accuracy values were below the limit of acceptance criteria, i.e., 15% for quality control (QC) samples and 20% for lower limit of quantification (LLOQ) samples. Rats were given intravenous (IV) administration of 1 mg/kg of pure CL in PEG 300 solution or CL-SFNP. The pharmacokinetic profile was improved with CL-SFNP compared to pure CL. Pure CL resulted in a maximum concentration (Cmax) value of 0.17 µg mL−1 at 5 min following administration, whereas that for CL-SFNP was 0.87 µg mL−1 and the extrapolated initial concentrations (C0) were 0.25 and 1.09 µg mL−1, respectively, for pure CL and CL-SFNP. A 2.4-fold increase in total area under the curve (AUC0-inf) (µg h mL−1) was observed with CL-SFNP when compared with pure CL. CL-SFNP demonstrated longer mean residence time (MRT; 0.67 h) than pure CL (0.26 h). In conclusion, the preparation of CL-SFNP was optimized and the formulation demonstrated improved pharmacokinetic properties compared to CL in solution following IV administration. [ABSTRACT FROM AUTHOR]

Paeonol exhibits a wide range of pharmacological activities, such as anti-inflammatory, antidiabetic as well as pain-relieving activities. However, its intrinsic properties, such as low water solubility, poor stability and low oral bioavailability, restrict its clinical application. The current study aimed to optimize paeonol-loaded ethosomal formulation and characterize it in terms of encapsulation efficiency (EE), vesicle size (VS), zeta potential (ZP) and polydispersity index (PDI), in addition to differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FT-IR) studies. Here, paeonol-loaded ethosomes were prepared by the injection method and optimized by the single-factor test and central composite design-response surface methodology. The optimized paeonol-loaded ethosomes had an EE of 84.33 ± 1.34%, VS of 120.2 ± 1.3 nm, negative charge of −16.8 ± 0.36 mV, and PDI of 0.131 ± 0.006. Ethosomes showed a spherical morphology under the transmission electron microscope (TEM). DSC, XRD and FT-IR results indicated that paeonol was successfully incorporated into the ethosomes. In-vitro transdermal absorption and skin retention of paeonol from paeonol-loaded ethosomes were 138.58 ± 9.60 µg/cm2 and 52.60 ± 7.90 µg/cm2, respectively. With reasonable skin tolerance, ethosomes could be a promising vehicle for transdermal delivery of paeonol. [ABSTRACT FROM AUTHOR]