Search

Jana K Alwattar,1,2 Mohammed M Mehanna3,4 1Department of Pharmaceutical Sciences, School of Pharmacy, Lebanese International University, Beirut, Lebanon; 2Pharmaceutical Nanotechnology Research Lab, Faculty of Pharmacy, Beirut Arab University, Beirut, Lebanon; 3Department of Pharmaceutical Sciences, School of Pharmacy, Lebanese American University, Byblos, Lebanon; 4Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, EgyptCorrespondence: Mohammed M Mehanna, Department of Pharmaceutical Sciences, School of Pharmacy, Lebanese American University, Byblos, Lebanon, Tel +96171708661, Email mohammed.mehanna@lau.edu.lb; mohamed.mehanna@alexu.edu.egBackground: Cancer ranks as the second most common cause of mortality as depicted by the World Health Organization, with one in six deaths being cancer-related mortality. Taking the lead in females, breast cancer is the most common neoplasm. Raloxifene, a selective estrogen receptor modulator, has been utilized as a chemotherapeutic agent for the treatment of breast cancer in postmenopausal women. However, its poor aqueous solubility hinders its clinical applications. Beta-cyclodextrin-based framework is a novel class of nano-vectors that used to potentiate the solubility and dissolution rate of poorly soluble drugs.Aim: The present study investigates the solubility and dissolution rate enhancement as well as the potential cytotoxic activity of raloxifene-loaded nanosponges formulation.Methods: The fabrication and optimization of cyclodextrin nanosponges crosslinked with diphenyl carbonate was portrayed through stoichiometric selection of cyclodextrin-to-crosslinker ratio. The complexation phenomenon and nanosponges formation were validated using FTIR, PXRD, TEM, and SEM examination.Results: Raloxifene-loaded nanosponges exhibited a 440± 8.5 nm particle size, a negative zeta potential of 25.18± 2.3 mV and a partial drug incorporation. Moreover, the drug loaded nanosponges demonstrated an in-vitro significantly enhanced dissolution behavior. Furthermore, the in-vitro cytotoxicity of the raloxifene-loaded nanosponges on MCF-7 breast cancer cell lines was statistically significant compared to the complex-free raloxifene.Conclusion: The cytotoxic behavior provided evidence that the incorporation of raloxifene within the nanosponges structure enhanced its anticancer activity and represents a potential nanocarrier for anticancer agent delivery.Keywords: raloxifene, nanosponges, anticancer, beta-cyclodextrin, breast cancer

This study aimed to evaluate the formulation and characterization of Rifaximin-loaded nanosponges for enhanced colon-targeted drug delivery, with a focus on percentage yield, entrapment efficiency, particle size, zeta potential, and in vitro drug release. Rifaximin-loaded nanosponges were synthesized using various methods, and formulations were optimized based on their performance. Key parameters, including production yield, drug encapsulation efficiency, particle size distribution, surface charge and release kinetics, were analyzed. Formulation F3 showed the highest percentage yield at 73.32% ± 0.15, indicating efficient production, while other formulations yielded between 68.14% and 71.15%. The entrapment efficiency (%EE) for F3 was also favorable at 72.65% ± 0.14, suggesting effective drug encapsulation, with other formulations showing %EE values from 66.45% to 70.23%. Particle size analysis revealed a mean particle size of 145.1 nm for F3, favorable for drug delivery, while its zeta potential of -36.2 mV indicated good stability due to reduced aggregation. The in vitro release data for F3 demonstrated a significantly enhanced release profile, with 98.85% of Rifaximin released within 12 hours. The Korsmeyer-Peppas model (R² = 0.9885) best fit the release kinetics, suggesting a mechanism involving both diffusion and polymer relaxation. In conclusion, formulation F3 of Rifaximin-loaded nanosponges showed optimal yield, high encapsulation efficiency, favorable particle size, stability and an enhanced release profile, indicating it as a promising candidate for improved bioavailability and targeted delivery of Rifaximin to the colon. [ABSTRACT FROM AUTHOR]

Nanosponges are versatile carriers due to their exceptional capability to improve the solubility of poorly water-soluble drugs, taste masking and enhancement of stability. This study investigates potential of nanosponges, prepared by crosslinking β-cyclodextrin with diphenyl carbonate in 1:4 ratio for enhancing solubility of Efonidipine. Nanosponges were characterized in terms of particle size. Phase solubility studies and solution state interaction studies were employed to understand the nature and strength of drug: nanosponge complexation. Complexes were prepared by kneading method and spray drying. Saturation solubility, in vitro dissolution studies and molecular modeling studies were performed. Complexes were characterized by differential scanning calorimetry (DSC), infrared spectroscopy, X ray powder diffraction (XRPD) and scanning electron microscopy. Phase solubility studies revealed 1:2 complexation between drug and carriers. Saturation solubility studies showed significant solubility increase with both beta CD and nanosponges. The increase was higher in case of spray dried complexes in all media. An 18 fold increase was observed in case of spray dried complexes in distilled water. DSC and PXRD confirmed amorphization of drug in the complexes. Thus solubility enhancement of EFD could be attributed to complexation and amorphization. Molecular modeling studies revealed the mode of entrapment of efonidipine in the carriers. In conclusion the versatility of nanosponges in encapsulating both hydrophilic and hydrophobic drug molecules holds immense promise for personalized medicine and targeted therapy, ultimately leading to improved patient outcomes. Moreover, the study introduces the efficacy of spray drying as a scalable and practical approach to maximize the solubility-enhancing benefits of nanosponges. This research highlights the potential of nanosponges to overcome a fundamental challenge in pharmaceuticals, opening new avenues for drug delivery and therapeutic advancement. [ABSTRACT FROM AUTHOR]

A new, user-friendly Ultra Performance Liquid Chromatography (UPLC) method was developed using Analytical Quality by Design (QbD) for precise analysis of Dacarbazine in both bulk powder and Dacarbazine-loaded Nanosponges. This method follows ICH guidelines and uses a statistically designed approach to optimize the separation conditions for Dacarbazine. A central composite design was implemented to identify the ideal combination of organic solvent (mobile phase composition) and flow rate. The UPLC method was successfully optimized for rapid separation (1.3 minutes) for Dacarbazine using a mobile phase consisting of 70% Methanol: 30% Orthophosphoric acid (0.1%) at a flow rate of 1.0 mL/min, using a Hypersil C18 column. The method exhibited excellent linearity with a correlation coefficient value of 0.997 across a concentration range of 4-20 μg/mL, accuracy (drug recovery of 96-100%) and sensitivity (LOD 1.15 μg/mL, LOQ 3.50 μg/mL) and it successfully quantified the drug in the formulated Dacarbazine-loaded Nanosponges. This QbD-driven UPLC method offers a valuable tool for reliable Dacarbazine quality control in pharmaceuticals providing rapid analysis, high accuracy, and low detection limits. [ABSTRACT FROM AUTHOR]

While vaccines have been highly successful in protecting against various infections, there are still many high-priority pathogens for which there are no clinically approved formulations. To overcome this challenge, researchers have explored the use of nanoparticulate strategies for more effective antigen delivery to the immune system. Along these lines, nanotoxoids are a promising biomimetic platform that leverages cell membrane coating technology to safely deliver otherwise toxic bacterial antigens in their native form for antivirulence vaccination. Here, in order to further boost their immunogenicity, nanotoxoids formulated against staphylococcal α-hemolysin are embedded into a DNA-based hydrogel with immunostimulatory CpG motifs. The resulting nanoparticle-hydrogel composite is injectable and improves the in vivo delivery of vaccine antigens while simultaneously stimulating nearby immune cells. This leads to elevated antibody production and stronger antigen-specific cellular immune responses. In murine models of pneumonia and skin infection caused by methicillin-resistant Staphylococcus aureus, mice vaccinated with the hybrid vaccine formulation are well-protected. This work highlights the benefits of combining nanoparticulate antigen delivery systems with immunostimulatory hydrogels into a single platform, and the approach can be readily generalized to a wide range of infectious diseases.

Targeted drug delivery to specific locations is a significant challenge encountered by researchers. Nanosponges have emerged as a promising solution for delivering drugs to their target sites. Nanosponges are nanoparticles with a large surface area, allowing for enhanced penetration compared to conventional drug delivery systems. This new technology offers controlled drug release and has several advantages over other methods. This project aimed to prepare and evaluate a Tacrolimus-loaded Nanosponges hydrogel. The goal was to create a dermatological gel suitable for local drug delivery after topical application, aiming for improved therapeutic effects, better dispersibility and good storage stability. Tacrolimus-loaded Nanosponge was prepared using beta-cyclodextrin and ethylcellulose as polymers, along with polyvinyl alcohol (PVA) as a surfactant. The solvent emulsion diffusion technique is a method for preparing nanosponges, and the variations in the formulation using different polymers and drug-polymer ratios offer the opportunity to fine-tune the nanosponge’s properties to meet specific requirements for drug delivery applications. A Tacrolimus-loaded nanosponge hydrogel was formulated using carbopol 934. The results of the study indicated that the optimized batch of nanosponges with high entrapment efficiency was chosen for formulating the gel incorporating carbopol 934. The gel that was prepared was subjected to assessments for pH, viscosity, spreadability, in-vitro diffusion, permeation and stability. The findings suggest that Tacrolimus can be effectively formulated in low doses of nanosponges-loaded hydrogel for atopic dermatitis.

Gas-loaded nanocarriers (G-LN) show promise in improving heart transplantation (HTx) outcomes. Given their success in reducing cell death during normothermic hypoxia/reoxygenation (H/R) in vitro, we tested their integration into cardioplegic solutions and static cold storage (SCS) during simulated HTx. Wistar rat hearts underwent four hours of SCS with four G-LN variants: O2- or N2-cyclic-nigerosyl-nigerose-nanomonomers (CNN), and O2- or N2-cyclic-nigerosyl-nigerose-nanosponges (CNN-NS). We monitored physiological-hemodynamic parameters and molecular markers during reperfusion to assess cell damage/protection. Hearts treated with nanomonomers (N2-CNN or O2-CNN) showed improvements in left ventricular developed pressure (LVDP) and a trend towards faster recovery of the rate pressure product (RPP) compared to controls. However, nanosponges (N2-CNN-NS or O2-CNN-NS) did not show similar improvements. None of the groups exhibited an increase in diastolic left ventricular pressure (contracture index) during reperfusion. Redox markers and apoptosis/autophagy pathways indicated an increase in Beclin 1 for O2-CNN and in p22phox for N2-CNN, suggesting alterations in autophagy and the redox environment during late reperfusion, which might explain the gradual decline in heart performance. The study highlights the potential of nanomonomers to improve early cardiac performance and mitigate cold/H/R-induced stunning in HTx. These early improvements suggest a promising avenue for increasing HTx success. Nevertheless, further research and optimization are needed before clinical application. [ABSTRACT FROM AUTHOR]

Some composite materials have been prepared, constituted by a cyclodextrin-bis-urethane-based nanosponge matrix in which a reduced graphene oxide/silver nanoparticles photocatalyst has been dispersed. Different chain extenders were employed for designing the nanosponge supports, in such a way as to decorate their hyper-cross-linked structure with diverse functionalities. Moreover, two different strategies were explored to accomplish the silver loading. The obtained systems were successfully tested as catalysts for the photodegradation of emerging pollutants such as model dyes and drugs. Enhancement of the photoactive species performance (up to nine times), due to the synergistic local concentration effect exerted by the nanosponge, could be assessed. Overall, the best performances were shown by polyamine-decorated materials, which were able to promote the degradation of some particularly resistant drugs. Some methodological issues pertaining to data collection are also addressed. [ABSTRACT FROM AUTHOR]

Abstract. Background. The prevalence of joint diseases affecting cartilage tissue and all components of the joint due to trauma and degenerative-dystrophic conditions has notably risen in recent years. Despite an extensive body of research, addressing large bone and cartilage defects remains a significant clinical challenge. This reality underscores the imperative to innovate treatment methods and enhance existing approaches. In this review, we will examine and analyse contemporary materials and techniques for replacing cartilage defects, including hydrogels, nanofibers, 3D membranes, and BioCartilage. Additionally, it explores key aspects of orthobiology, specifically the utilisation of mesenchymal stem cells and exosomes. The article also considers instances of employing modern methods to replace cartilage defects in both experimental and clinical studies. The purpose was to investigate, analyse, and interpret data on the application of contemporary materials and methods for cartilage defect replacement as described in experimental, clinical, and review studies. Materials and methods. A comprehensive literature search was conducted using terms such as osteochondral defect, BioCartilage, nanofiber, allograft cartilage, mesenchymal stem cell, hydrogel, and nonwoven membranes. The search was conducted on the basis of Google Scholar, CrossRef, PubMed databases for the last 5 years. Logical analysis and evaluation were performed on the results of studies encompassing diverse modern technologies and principles for replacing cartilage tissue defects. Results. Microfracturing and tunneling are quite effective methods in replacing cartilage defects with cartilage-like regenerate. Their effectiveness reduces with increasing mechanical and axial loads on the formed regenerate. Experimental studies show that physical properties of hydrogel can be compared to native cartilage tissue. Moreover, hydrogel can be used as a matrix for the delivery of anti-inflammatory and some biological drugs. However, this method needs more specific clinical and experimental studies to be put into practice. The use of exosomes to replace osteochondral defects is a simple method, but rapid degradation limits its effectiveness. Combining exosomes with hydrogel or hyaluronic acid can solve these problems by prolonging their release and degradation, enhancing biological activity and biocompatibility. Bioprinting and nanofiber sponge (3D membrane) have reasonable theoretical and experimental value for replacing cartilage defects and require further clinical studies. Promising methods of cartilage tissue regeneration are the implantation of autologous chondrocytes, the use of ChondroFiller and BioCartilage. For a wider assessment of the results of using these treatment methods, longer clinical studies are needed. Conclusions. An analysis of more than 36 literature sources, including review, experimental, and clinical studies, reveals a structured summary of the latest research and developments in cartilage tissue defect repair. There is no universal technology for replacing cartilage defects that would be suitable for all patients. Therefore, this review highlights the advantages of different methods for cartilage defect repair adapted to specific clinical cases. Based on the analysis of literature data regarding the use of implant materials to correct cartilage defects in orthopaedics and traumatology, it can be concluded that the chosen direction of scientific research is relevant and significant. Additionally, certain aspects of the development of this issue can be outlined, and questions requiring further study and resolution can be identified. [ABSTRACT FROM AUTHOR]

Advancements in nanotechnology have ushered in nanosponges, biodegradable polyester structures with nanometersized cavities, designed for targeted drug delivery. Initially developed for topical applications, these nanosponges have evolved to be administered orally and intravenously. They exhibit a porous structure for controlled drug release, addressing issues like toxicity and poor bioavailability. Capable of carrying both hydrophilic and lipophilic drugs, nanosponges serve as versatile carriers for substances like enzymes, proteins, vaccines, and antibodies. Their characteristics include size and polarity control, crystalline forms, non-toxicity, stability in various conditions, suspension and regeneration capabilities, and a 3D structure for targeted capture and release. The composition involves a polymer, a cross-linking agent, and specific drug criteria. Advantages encompass targeted delivery, flavor masking, reduced side effects, water solubility, adjustable particle size, and easy commercial production. Disadvantages include limited encapsulation for larger molecules. The mechanism involves an open structure allowing prolonged release. Various types based on cyclodextrin offer unique properties. Factors affecting nanosponges include polymer nature, drug characteristics, complexation temperature, and degree of substitution. Preparation methods include solvent, ultrasound-assisted, melt, bubble electrospinning, and emulsion solvent diffusion methods. Comprehensive characterization includes drug entrapment efficiency, saturation state interaction, in vitro release studies, porosity measurement, and spectroscopic techniques. Applications span solubility enhancement, sustained delivery, oral and topical systems, protein delivery, protection from degradation, pollutant removal from water, cancer treatment, antiviral applications, enzyme immobilization, and modulation of drug release. [ABSTRACT FROM AUTHOR]

Effective drug delivery at a targeted site had given the possibility to perform the precise function to control the release rates and have a better compliance on the health care system but the chemistry possessing complex form had made conditions complicated. But the invention of nanosponges has given a significant approach toward solving this problem. Nanosponges are tiny sponges having size of about a virus and can be filled with variety of drugs. This sponges can circulate around the body until interact with specific target site and stick on surface and start releasing drug in a controlled manner. Some cyclodextrins based nanosponges proposed nanodelivery system and form porous insoluble nanoparticle having crystalline and amorphous nature. Important characteristic of these sponges is their solubility in aqueous form and give a effect to the drugs with poor solubility. This review is focusing on the preparation methods, applications of nanosponges in the field of drug delivery. [ABSTRACT FROM AUTHOR]

Nanosponges are unique sponge‐like carrier systems with numerous cavities and a mesh‐like network throughout their surface. They are categorized into three types based on the material of construction, i.e., polymer‐, inorganic‐, and bio‐derived material‐based nanosponges. Unlike conventional nanoparticles, nanosponges bear countless interconnected voids and mesh‐like network that enables maximum drug, imaging probe, or photosensitizer loading via absorption, encapsulation, conjugation, or complexion. The voids can be further sealed using suitable lipids or polymers to avoid leakage of drugs at the non‐target site, protect therapeutics from biological conditions, and control the release of therapeutics for a prolonged period. Recently, nanosponges have grasped the attention of researchers in the area of cancer by overcoming the drawbacks associated with the conventional delivery of immunotherapeutic, targeted therapeutic, and chemotherapeutic agents. Interestingly, several reports have also witnessed their potential in cancer theranostics. Owing to this supremacy, nanosponges could be an apt platform for cancer therapy and diagnosis. The current review discusses the general aspects, types, and preparation methods of nanosponges. In addition, the ambit of nanosponges in treating different types of cancer is meticulously discussed, along with detailed descriptions of their corresponding patents. Furthermore, the role of nanosponges in phototherapy and cancer theranostics are selectively canvassed. [ABSTRACT FROM AUTHOR]

Background: The purpose of this work was to complex budesonide with cyclodextrin-based nanosponges to improve its solubility and stability. The current study focused on polysaccharide systems that have undergone minimal chemical alteration and have been used to target the colon. These targeted delivery and polysaccharide-based complexation methods are anticipated to aid in the creation of medication formulations for disorders affecting the colon, such as colorectal cancer. The goal of the current work was to use a Quality by Design (QbD) strategy to create budesonide-loaded nanosponges. The system consisted of nanosponges loaded with budesonide. Methods: Nanosponges were formulated through microwave-assisted synthesis. Studies on drug release were conducted with a method changing power of hydrogen (pH) with enzyme. Quality by Design-based optimization with a 32 full factorial design was applied for the optimization of the process parameters including the β-cyclodextrin:diphenyl carbonate ratio and the reaction time. Responses were measured for three dependent variables: practical yield, percentage drug release, and percentage drug release at the fifth hour. Results and Conclusions: The optimization model indicated a yield of 76.21%, a percentage drug release at the fifth hour of 24.61%, and a total drug release after 7 hours of 87.58%. The observed responses of the optimized process closely matched the predicted values. The above budesonide-loaded nanosponge formulations provide a targeted medicine for the colon and may be an effective method for treating colonic illness.

The ability to employ waste products, such as vegetable scraps, as raw materials for the synthesis of new promising adsorbing materials is at the base of the circular economy and end of waste concepts. Dextrin-based nanosponges (D_NS), both cyclodextrin (CD) and maltodextrin (MD), have shown remarkable adsorption abilities in the removal of toxic compounds from water and wastewater, thus representing a bio-based low-cost solution which is establishing itself in the market. Nevertheless, their environmental safety for either aquatic or terrestrial organisms has been overlooked, raising concern in terms of potential hazards to natural ecosystems. Here, the environmental safety (ecosafety) of six newly synthesized batches of D_NS was determined along with their full characterization by means of dynamic light scattering (DLS), thermogravimetric analysis (TGA), Fourier transformed infrared spectroscopy with attenuated total reflection (FTIR-ATR) and transmission electron microscopy (SEM). Ecotoxicity evaluation was performed using a battery of model organisms and ecotoxicity assays, such as the microalgae growth inhibition test using the freshwater Raphidocelis subcapitata and the marine diatom Dunaliella tertiolecta, regeneration assay using the freshwater cnidarian Hydra vulgaris and immobilization assay with the marine brine shrimp Artemia franciscana. Impact on seedling germination of a terrestrial plant of commercial interest, Cucurbita pepo was also investigated. Ecotoxicity data showed mild to low toxicity of the six batches, up to 1 mg/mL, in the following order: R. subcapitata > H. vulgaris > D. tertiolecta > A. franciscana > C. pepo. The only exception was represented by one batch (NS-Q+_BDE_(GLU2) which resulted highly toxic for both freshwater species, R. subcapitata and H. vulgaris. Those criticalities were solved with the synthesis of a fresh new batch and were hence attributed to the single synthesis and not to the specific D_NS formulation. No effect on germination of pumpkin but rather more a stimulative effect was observed. To our knowledge this is the first evaluation of the environmental safety of D_ NS. As such we emphasize that current formulations and exposure levels in the range of mg/mL do not harm aquatic and terrestrial species thus representing an ecosafe solution also for environmental applications.

Effective drug distribution at the intended or particular location is a critical issue that researchers are now dealing. Nanosponges have significantly increased in importance in medication delivery using nanotechnology in recent years. An important step toward solving these problems has been the development of nanosponges. Recently created and proposed for use in drug delivery, nanosponge is a unique type of hyper‐crosslinked polymer‐based colloidal structures made up of solid nanoparticles with colloidal carriers. Nanosponges are solid porous particles that may hold pharmaceuticals and other actives in their nanocavities. They can be made into dosage forms for oral, parenteral, topical, or inhalation use. The targeted distribution of drugs in a regulated manner is greatly aided by nanosponge. The utilization of nanosponges, their benefits, their production processes, the polymers they are made of, and their characterization have all been covered in this review article. [ABSTRACT FROM AUTHOR]

Aim: Objective of work was to compare role of β-Cyclodextrin (β-CD) and Nanosponges (NS) prepared with different cross-linking ratios and different drug loading ratios to enhance solubility and dissolution rate of Albendazole (ALB). Materials and Methods: Diphenyl Carbonate (DPC) was used as cross-linker for preparing NS with various β-CD and DPC ratios (1:2 and 1:4). Solvent evaporation was used to make binary complex. ALB and NS were dissolved in Dichloromethane (DCM) in 1:1 and 1:2 ratios and triturated until solvent evaporated. Phase solubility, saturation solubility and in vitro dissolution studies were performed. Solid state characterization as well as spectral and thermal analyses was done. Results: Stability constant for complexes ALB-β-CD, ALB-NS (1:2 ratios) and ALB-NS (1:4 ratios) were found to be 1715M-1±18.3, 1902M-1±29.5 and 1945M-1±30.1 respectively. Maximum solubility of all complexes was observed in fed state simulated intestinal fluid (FeSSIF). The increase was to the tune of 3-8 folds for all binary complexes at 1:1 and 1: 2 drug loading ratios. Dissolution rate increased by 47%-67% for drug loading ratio 1:1 and 55-71% for drug loading ratio 1:2 in FeSSIF in 150 min. Conclusion: β-CD based NS improved solubility of ALB. Presence of drug in molecular form in nanochannels and amorphization were responsible for increase in solubility. Nanosponges prepared in ratio 1:4 and drug loading in ratio 1:2 showed highest increase in solubility and dissolution rate. [ABSTRACT FROM AUTHOR]

Introduction: Cancer contributes to a high mortality rate worldwide spanning its diversity from genetics to resistant therapeutic response. To date emerging strategies to combat and manage cancer are particularly focused on the development of targeted therapies as conventional treatments account for the destruction of normal cells as well. In this regard, medicinal plant-based therapies are quite promising in imposing minimal side effects; however, limitations like poor bioavailability and stability of bioactive phytochemicals are associated with them. In parallel, nanotechnology provides nominal solution to deliver particular therapeutic agent without compromising its stability. Methods: In this study, Solanum nigrum, an effective medicinal plant, loaded arabinoxylan cross-linked ß-cyclodextrin nanosponges (SN-AXCDNS) were designed to evaluate antitumor activity against breast cancer. Therefore, SNAXCDNS were prepared by using cross-linker melt method and characterized by physicochemical and pharmacological parameters. Results: Hydrodynamic size, zeta potential and entrapment efficiency (EE%) were estimated as 226 ± 4 nm, -29.15 ± 5.71 mV and 93%, respectively. Surface morphology of nanocomposites showed spherical, smooth, and porous form. Antitumor pharmacological characterization showed that SN loaded nanosponge demonstrated higher cytotoxicity (22.67 ± 6.11 µg/mL), by inducing DNA damage as compared to void SN extract. Flow cytometry analysis reported that encapsulated extract promoted cell cycle arrest at sub-G1 (9.51%). Moreover, in vivo analysis demonstrates the reduction in tumor weight and 85% survival chances in nanosponge treated mice featuring its effectiveness. In addition, in silico analysis revealed that ß-cyclodextrin potentially inhibits MELK in breast cancer cell lines (B.E = -10.1 Kcal/mol). Conclusion: Therefore, findings of current study elucidated the therapeutic potential of ß-cyclodextrin based nanosponges to be an alternative approach regarding the delivery and solubilization of antitumor drugs. [ABSTRACT FROM AUTHOR]

Cyclodextrin nanosponges are solid nanoparticles, designed by cross-linking of cyclodextrin polymer; it has been used widely as a good delivery system for water insoluble drugs. The aim of this study is to enhance the solubility of Piroxicam (PXM) using β-Cyclodextrin based nanosponges formulations. PXM nanosponge (PXM-NS) formulations were prepared using β-cyclodextrin and carbonyldiimidazole as a cross linker, three ratios of β-cyclodextrin to crosslinker in addition to three drug to nanosponges ratios were tested. Piroxicam nanosponge formulations were characterized for its particle size, zeta potential, physical compatibility and in vitro release. Stability studies at three temperatures (4 °C, 25 °C and 40 °C) were done for optimal formula. Finally, the in vivo analgesic activity and pharmacokinetic parameters of the optimal formula were conducted. The optimized PXM-NS formula (PXM-NS10) showed particle size (362 ± 14.06 nm), polydispersity index (0.0518), zeta potential (17 ± 1.05 mV), and %EE (79.13 ± 4.33). The dissolution study showed a significant increase in the amount of PXM dissolved compared with the unformulated drug. Stability studies confirmed that nanosponge showed accepted stability for 90 days at 4 °C and 25 °C. In vivo analgesic studies verified that there was a significant enhancement in the analgesic response to PXM in mice, and 1.42 fold enhancement in the relative bioavailability of PXM-NS10 as compared to commercial tablets. Nanosponge prepared under optimal conditions is an encouraging formula for increasing the solubility and therefore the bioavailability of Piroxicam. [ABSTRACT FROM AUTHOR]

Purpose: Our work aims to cross-linked cyclodextrin-based nanosponges for allyl methyl sulfide delivery, physicochemical characterization, and in vitro study. Method: Plain nanosponges were created using the melting technique to react β-cyclodextrin with the cross-linker diphenyl carbonate at a molar ratio of 1:4, respectively. AFM, FESEM, GC–MS, PDI and zeta potential, PXRD, and FTIR were used to characterize the drug-loaded nanosponges. Additionally, compared to free allyl methyl sulfide, allyl methyl sulfide-nanosponges loaded nanosponges showed superior antioxidant and anti-inflammatory activities. Result: The depth and surface characteristics of the particles were quantified using AFM. It was discovered that the nanosponge size was about 185 nm. The FESEM showed that the AMS-loaded formula had a very porous structure and a sponge-like shape. GCMS: The volatile components in the AMS were identified in the current experiment using GC–MS. With the largest percentage area among them, AMS was identified as a key component (19.753%). PDI and zeta: the AMS loaded NS at a 1:4 w/w ratio was chosen. The table below displays the AMS-typical NS particle size. For AMS-NS, the particle size distribution was likewise within the intended range. FTIR: C-H aliphatic structuring was found in the drug at 2977, 2915, and 2832. Similarly, C–C-structuring was found at 990,913,851. These peaks are also present in the drug-polymer matrix. PXRD: all strong peaks become muted after drug loading into the NS because of a transition to an amorphous state, indicating full drug entrapment. Antioxidant: AMS and AMS-NS were reduced when compared to the standard. This capacity is represented as the number of equivalents of ascorbic acid. Illustrates the DPPH inhibition effect of AMS and AMS-NS at different concentrations. It was observed that the DPPH inhibition effect of AMS was increased. Moreover, the loaded AMS-NS showed a higher reduction in the DPPH concentrations than the standard. Anti-inflammatory: AMS-NS reduced denaturation; the results were compared to the standard and significantly reduced. Conclusion: The study demonstrated that the complexation of AMS with NS would be a workable strategy for formulation were much greater. Because of this, these investigations showed that nanosponges might be utilized to distribute AMS. Upcoming research on the beta-cyclodextrin nanosponges' potential for in vivo medication delivery against cancer. [ABSTRACT FROM AUTHOR]

Nanotechnology advancements have resulted in the creation of tailored medicine delivery systems. Because of its potential to address a wide range of unexplored difficulties, nanotechnology-based medication delivery systems are acquiring significant relevance in the modern day. Nanosponges are microscopic sponges the size of a virus (250 nm-1 μm) having cavities that may be filled with a wide range of hydrophobic and hydrophilic medicines also overcome issues such as medication toxicity and low absorption. Nanosponges are solid porous particles with the ability to load medications and other actives into their nanocavity; they can be manufactured in oral, topical, parenteral or inhalation dosage forms. Crosslinking cyclodextrin with carbonyl or di-carboxylate can be used to create nanosponges (Crosslinkers). Another key features of nanosponges includes their aqueous solubility, which allows them to be used efficiently for medications with low solubility. Nanosponges can also be used as a vehicle for enzymes, proteins, vaccines and antibodies. [ABSTRACT FROM AUTHOR]

Introduction: Cancer contributes to a high mortality rate worldwide spanning its diversity from genetics to resistant therapeutic response. To date emerging strategies to combat and manage cancer are particularly focused on the development of targeted therapies as conventional treatments account for the destruction of normal cells as well. In this regard, medicinal plant-based therapies are quite promising in imposing minimal side effects; however, limitations like poor bioavailability and stability of bioactive phytochemicals are associated with them. In parallel, nanotechnology provides nominal solution to deliver particular therapeutic agent without compromising its stability.Methods: In this study, Solanum nigrum, an effective medicinal plant, loaded arabinoxylan cross-linked β-cyclodextrin nanosponges (SN-AXCDNS) were designed to evaluate antitumor activity against breast cancer. Therefore, SN-AXCDNS were prepared by using cross-linker melt method and characterized by physicochemical and pharmacological parameters.Results: Hydrodynamic size, zeta potential and entrapment efficiency (EE%) were estimated as 226 ± 4 nm, −29.15 ± 5.71 mV and 93%, respectively. Surface morphology of nanocomposites showed spherical, smooth, and porous form. Antitumor pharmacological characterization showed that SN loaded nanosponge demonstrated higher cytotoxicity (22.67 ± 6.11 μg/mL), by inducing DNA damage as compared to void SN extract. Flow cytometry analysis reported that encapsulated extract promoted cell cycle arrest at sub-G1 (9.51%). Moreover, in vivo analysis demonstrates the reduction in tumor weight and 85% survival chances in nanosponge treated mice featuring its effectiveness. In addition, in silico analysis revealed that β-cyclodextrin potentially inhibits MELK in breast cancer cell lines (B.E = −10.1 Kcal/mol).Conclusion: Therefore, findings of current study elucidated the therapeutic potential of β-cyclodextrin based nanosponges to be an alternative approach regarding the delivery and solubilization of antitumor drugs.

This study demonstrated a rapid method of producing PtPd via chemical reduction by varying metal composition and types of capping agents. The effect of different compositions between the two-metal precursor, Pt and Pd, is invested by tuning at various volume ratios of 3:1, 1:3, and 1:1 and comparing them with their single counterparts. The FESEM results show that all prepared samples exhibit nanosponges structure. PtPd of 1:1 ratio has the highest ECSA of 14.25 m²/g, while PtPd with PVP exhibits a high ECSA value of 692.7 m²/g compared to those without capping agent (287.8 m²/g), indicating large active sites, which increases its catalytic function. [ABSTRACT FROM AUTHOR]

Many active pharmaceutical ingredients show low oral bioavailability due to factors such as poor solubility and physical and chemical instability. The formation of inclusion complexes with cyclodextrins, as well as cyclodextrin-based polymers, nanosponges, and nanofibers, is a valuable tool to improve the oral bioavailability of many drugs. The microencapsulation process modifies key properties of the included drugs including volatility, dissolution rate, bioavailability, and bioactivity. In this context, we present relevant examples of the stabilization of labile drugs through the encapsulation in cyclodextrins. The formation of inclusion complexes with drugs belonging to class IV in the biopharmaceutical classification system as an effective solution to increase their bioavailability is also discussed. The stabilization and improvement in nutraceuticals used as food supplements, which often have low intestinal absorption due to their poor solubility, is also considered. Cyclodextrin-based nanofibers, which are polymer-free and can be generated using environmentally friendly technologies, lead to dramatic bioavailability enhancements. The synthesis of chemically modified cyclodextrins, polymers, and nanosponges based on cyclodextrins is discussed. Analytical techniques that allow the characterization and verification of the formation of true inclusion complexes are also considered, taking into account the differences in the procedures for the formation of inclusion complexes in solution and in the solid state. [ABSTRACT FROM AUTHOR]

Actarit tablets of interpenetrating polymer networks were prepared using carboxy methyl tamarind gum and cyclodextrin nanosponges for increasing oral bioavailability. Formulations with different carboxymethyl tamarind gum concentrations were freeze dried to create actaritloaded interpenetration polymer networks, which were then analysed for drug loading equilibrium swelling and characterised using FTIR, DSC, and XRD. Actarit loaded IPN tablets were prepared and evaluated for in-vitro and in-vivo studies. The drug loading in the IPNs ranged from 59.36 to 65.72%, and swelling in the presence of 0.1N HCl in the IPNs was substantially lower (P 0.05) than in the presence of phosphate buffer pH 6.8. Studies using FTIR, DSC, and XRD confirmed that Actarit and IPNs formed a molecular combination. Actarit loaded IPN tablets' average weight, thickness, hardness, friability, and percentage of drug content were all within acceptable ranges. The drug release was highest for F3 (99.86%) and for marketed 98.67%. From in vivo bioavailability studies, the pure drug's Cmax was 404.34±12.87 ng/ml, significantly higher when compare with marketed product and optimized IPN actarit tablets of 385.21±9.43 and 342.76±13.56 ng/ml respectively. The Tmax of pure drug, marketed and optimized formulation were 1.5±0.05, 2.0±0.06 and 4.0±0.04 h respectively. The formulation of the marketed and optimized formulation exhibited a higher AUC0- ∞ (815±14.23 and 915±28.33 ng.h/ml) than the pure drug (800.76±15.76 ng.h/ml). The optimized tablet formulation showed a significantly higher AUC0-t and MRT than the pure drug and marketed product. The bioavailability of Actarit's cyclodextrin nanosponges based IPNs tablets were significantly improved when compared to the pure drug. [ABSTRACT FROM AUTHOR]

A set of four composite materials was prepared, consisting of a nanosponge matrix based on β-cyclodextrin in which carbon nitride was dispersed. The materials were characterized by the presence of diverse cross-linker units joining the cyclodextrin moieties, in order to vary the absorption/release abilities of the matrix. The composites were characterized and used as photocatalysts in aqueous medium under UV, visible and natural solar irradiation for the photodegradation of 4-nitrophenol, and for the selective partial oxidation of 5-hydroxymethylfurfural and veratryl alcohol to the corresponding aldehydes. The nanosponge-C3N4 composites showed higher activity than the pristine semiconductor, which can probably be attributed to the synergic effect of the nanosponge, capable of increasing the substrate concentration near the surface of the photocatalyst. [ABSTRACT FROM AUTHOR]

Cell‐based therapies comprising the administration of living cells to patients for direct therapeutic activities have experienced remarkable success in the clinic, of which macrophages hold great potential for targeted drug delivery due to their inherent chemotactic mobility and homing ability to tumors with high efficiency. However, such targeted delivery of drugs through cellular systems remains a significant challenge due to the complexity of balancing high drug‐loading with high accumulations in solid tumors. Herein, a tumor‐targeting cellular drug delivery system (MAGN) by surface engineering of tumor‐homing macrophages (Mφs) with biologically responsive nanosponges is reported. The pores of the nanosponges are blocked with iron‐tannic acid complexes that serve as gatekeepers by holding encapsulated drugs until reaching the acidic tumor microenvironment. Molecular dynamics simulations and interfacial force studies are performed to provide mechanistic insights into the "ON‐OFF" gating effect of the polyphenol‐based supramolecular gatekeepers on the nanosponge channels. The cellular chemotaxis of the Mφ carriers enabled efficient tumor‐targeted delivery of drugs and systemic suppression of tumor burden and lung metastases in vivo. The findings suggest that the MAGN platform offers a versatile strategy to efficiently load therapeutic drugs to treat advanced metastatic cancers with a high loading capacity of various therapeutic drugs. [ABSTRACT FROM AUTHOR]

Nanocarriers for oxygen delivery have been the focus of extensive research to ameliorate the therapeutic effects of current anti-cancer treatments and in the organ transplant field. In the latter application, the use of oxygenated cardioplegic solution (CS) during cardiac arrest is certainly beneficial, and fully oxygenated crystalloid solutions may be excellent means of myocardial protection, albeit for a limited time. Therefore, to overcome this drawback, oxygenated nanosponges (NSs) that can store and slowly release oxygen over a controlled period have been chosen as nanocarriers to enhance the functionality of cardioplegic solutions. Different components can be used to prepare nanocarrier formulations for saturated oxygen delivery, and these include native α-cyclodextrin (αCD), αcyclodextrin-based nanosponges (αCD-NSs), native cyclic nigerosyl-nigerose (CNN), and cyclic nigerosyl-nigerose-based nanosponges (CNN-NSs). Oxygen release kinetics varied depending on the nanocarrier used, demonstrating higher oxygen release after 24 h for NSs than the native αCD and CNN. CNN-NSs presented the highest oxygen concentration (8.57 mg/L) in the National Institutes of Health (NIH) CS recorded at 37 °C for 12 h. The NSs retained more oxygen at 1.30 g/L than 0.13 g/L. These nanocarriers have considerable versatility and the ability to store oxygen and prolong the amount of time that the heart remains in hypothermic CS. The physicochemical characterization presents a promising oxygen-carrier formulation that can prolong the release of oxygen at low temperatures. This can make the nanocarriers suitable for the storage of hearts during the explant and transport procedure. [ABSTRACT FROM AUTHOR]

Fisetin (FS) is considered a safer phytomedicine alternative to conventional chemotherapeutics for breast cancer treatment. Despite its surpassing therapeutic potential, its clinical utility is hampered by its low systemic bioavailability. Accordingly, as far as we are aware, this is the first study to develop lactoferrin-coated FS-loaded β-cyclodextrin nanosponges (LF-FS-NS) for targeted FS delivery to breast cancer. NS formation through cross-linking of β-cyclodextrin by diphenyl carbonate was confirmed by FTIR and XRD. The selected LF-FS-NS showed good colloidal properties (size 52.7 ± 7.2 nm, PDI < 0.3, and ζ-potential 24 mV), high loading efficiency (96 ± 0.3%), and sustained drug release of 26 % after 24 h. Morphological examination using SEM revealed the mesoporous spherical structure of the prepared nanosponges with a pore diameter of ~30 nm, which was further confirmed by surface area measurement. Additionally, LF-FS-NS enhanced FS oral and IP bioavailability (2.5- and 3.2-fold, respectively) compared to FS suspension in rats. Antitumor efficacy evaluation in vitro on MDA-MB-231 cells and in vivo on an Ehrlich ascites mouse model demonstrated significantly higher activity and targetability of LF-FS-NS (30 mg/kg) compared to the free drug and uncoated formulation. Consequently, LF-FS-NS could be addressed as a promising formulation for the effective management of breast cancer. [ABSTRACT FROM AUTHOR]

Significant activity improvement was achieved by associating graphene oxide-silver composite photocatalysts with cyclodextrin-based nanosponge materials, due to the synergistic effect provided by the supramolecular host abilities of the nanosponge. Three photocatalysts were prepared, fully characterized (FT-IR, ss-NMR, Raman, XRD, SEM, EDX, AFM, ICP, TGA, potentiometric titration), and tested for the oxidative photodegradation of some dyes and phenols, chosen as model organic pollutants. Compared to the unsupported photocatalyst, the nanosponge-based materials showed enhanced performances (being able to carry out the degradation even of dyes which do not react in the presence of the unsupported catalyst), and good recyclability. The activity improvement is attributed to a local concentration effect provided by the nanosponge, able to capture the organic substrate in the proximity of the actual photocatalyst. The results presented herein provide a helpful basis for designing advanced catalytic systems.

Ibrutinib (ITB) is a specific and novel irreversible inhibitor of Bruton's tyrosine kinase enzyme, for which reason it exhibits potential chemotherapeutic effects against a few types of B-cell cancers. The objective of this study was to design and characterize the targeted anti-cancer moiety of ITB encapsulated in polymeric nanosponges (IBNS 1-5). The IBNSs were fabricated using the ultrasonication-assisted solvent evaporation technique. They were optimized for robust nanocarriers by varying the ratio of ethylcellulose (50–200 mg), using a constant amount 50 mg of polyvinyl alcohol ((PVA) stabilizer), and drug ITB. Optimized INBS4 containing 50 mg of ITB, PVA, and 162.5 mg of EC was prepared and was studied for anti-cancer potential. Particle analysis and EE and DL calculation of optimized IBNS4 were 640.9 nm, 0.35, −30.2 mV in size, PDI, and ζp, respectively. Physicochemical characterization (FTIR and DSC) studies of IBNS4 showed that the drug was compatible with excipients, and was encapsulated properly within the core of nanosponges. In vitro drug release studies revealed that IBNS4 followed the Higuchi matrix model with anomalous non-Fickian release kinetics. The in vitro diffusion study of I-NS4 exhibited sustained release for 24 h. Enhanced cytotoxicity effects against the MCF-7 observed with the developed NSs (IBNS4) showed 1.96 times more cytotoxic potential compared to the pure drug (ITB). [ABSTRACT FROM AUTHOR]

Pt alloy nanostructures have been explored as promising anode catalysts for methanol oxidation reaction. However, the Pt catalyst have continued to face challenges that are yet to be resolved. Studies have shown that the size and geometric structure can influence a material's catalytic activity and is related to the synthesis technique. In this study, PtPdNi nanostructures were produced at different synthesis duration. FESEM results show that all the samples exhibited nanosponges structure. The PtPdNi synthesized for 150 s, exhibited higher catalytically active toward methanol oxidation and resistance to carbon monoxide poisoning. [ABSTRACT FROM AUTHOR]

Abemaciclib (AC) is a novel, orally available drug molecule approved for the treatment of breast cancer. Due to its low bioavailability, its administration frequency is two to three times a day that can decrease patient compliance. Sustained release formulation are needed for prolong the action and to reduce the adverse effects. The aim of current study was to develop sustained release NSs of AC. Nanosponges (NSs) was prepared by emulsion-solvent diffusion method using ethyl-cellulose (EC) and Kolliphor P-188 (KP-188) as sustained-release polymer and surfactant, respectively. Effects of varying surfactant concentration and drug: polymer proportions on the particle size (PS), polydispersity index (PDI), zeta potential (ζP), entrapment efficiency (%EE), and drug loading (%DL) were investigated. The results of AC loaded NSs (ACN1-ACN5) exhibited PS (366.3–842.2 nm), PDI (0.448–0.853), ζP (−8.21 to −19.7 mV), %EE (48.45–79.36%) and %DL (7.69–19.17%), respectively. Moreover, ACN2 showed sustained release of Abemaciclib (77.12 ± 2.54%) in 24 h Higuchi matrix as best fit kinetics model. MTT assay signified ACN2 as potentials cytotoxic nanocarrier against MCF-7 and MDA-MB-231 human breast cancer cells. Further, ACN2 displayed drug release property without variation in the % release after exposing the product at 25 °C, 5 °C, and 45 °C storage conditions for six months. This investigation proved that the developed NSs would be an efficient carrier to sustain the release of AC in order to improve efficacy against breast cancer.

The aim and objective of the present study was to formulate and evaluate Tamoxifen nanosponges for targeted delivery. Nanosponges were prepared using ethyl cellulose as the polymer and polyvinyl alcohol as the stabilizing agent by solvent evaporation method. The Nanosponges prepared were evaluated for different parameters like the drug: polymer ratio, stirring speed and time. The encapsulation and the diffusion study of the formulation were done. Particle size analysis and scanning electron microscopy of the nanosponges were performed and from this study it was found that the nanosponges were spherical in shape and have porous nature. The nanosponges prepared were incorporated into the gel base of carbapol. In diffusion study of the nanosponge gel was performed. Similarly F6 and F7 exhibited the best release of 90.19% and 87.10% respectively at the end of 48 hours amoung all the five formulations of Tamoxifen - eudragit nanosponges. [ABSTRACT FROM AUTHOR]

Objectives: The objective of the research is to formulate a nanosponges loaded hydrogel of Metformin Hydrochloride for the treatment of Psoriasis. Psoriasis is currently treated with a variety of topical and systemic therapies. Many of these treatments, however, are expensive and involve side effects, such as immunosuppression. As a result, there is a need to develop therapies that are effective, have fewer adverse effects, and are less expensive. Materials and Methods: The Solvent Emulsion Diffusion Process was used to create Metformin Hydrochloride nanosponges. Ethyl cellulose was used as a polymer, polyvinyl alcohol was used as an emulsifying agent, and an organic solvent mixture of Dichloromethane and Ethanol (1:1) was used to make nanosponges. The optimized batches of nanosponges were used for the formulation of Hydrogels using different gelling agents like Carbopol 934, HPMC K4, Sodium alginate and Acacia with same concentration. Results: The formulated Metformin Hydrochloride nanosponges were characterized by various tests like the Production yield, Entrapment efficiency, FT-IR, Zeta potential, Scanning Electron Microscopy, etc. Batch F5 showed the highest entrapment efficiency with the lowest particle size and hence was considered as the optimized batch for the formulation of the Hydrogels. The FT-IR ensured the compatibility of the drug with the polymer, the Zeta potential was good enough to produce formulations with good stability. The SEM analysis of batch F5 demonstrates that the nanosponges are segregated, spherical in shape with smooth surface and are porous in nature with particle size less than 1µ. Conclusion: Nanosponges loaded Hydrogel of Metformin HCl for the treatment of Psoriasis was successfully formulated, optimized and evaluated. [ABSTRACT FROM AUTHOR]

Sesamol (SES) possesses remarkable chemotherapeutic activity, owing to its anti-inflammatory and antioxidant potential. However, the activity of SES is mainly hampered by its poor physicochemical properties and stability issues. Hence, to improve the efficacy of this natural anti-inflammatory and cytotoxic agent, it was loaded into β-cyclodextrin nanosponges (NS) prepared using different molar ratios of polymer and crosslinker (diphenyl carbonate). The particle size of SES-laden NS (SES-NS) was shown to be in the nano range (200 to 500 nm), with a low polydispersity index, an adequate charge (−17 to −26 mV), and a high payload. Field emission scanning electron microscopy, thermogravimetric analysis, and Fourier transform infrared spectroscopy were used to characterize the bioactive-loaded selected batch (SES-NS6). This batch of nanoformulations showed improved solubilization efficacy (701.88 µg/mL) in comparison to bare SES (244.36 µg/mL), polymer (β-CD) (261.43 µg/mL), and other fabricated batches. The drug release data displayed the controlled release behavior of SES from NS. The findings of the egg albumin denaturation assay revealed the enhanced anti-inflammatory potential of SES-NS as compared to bare SES. Further, the cytotoxicity assay showed that SES-NS was more effective against B16F12 melanoma cell lines than the bioactive alone. The findings of this assay demonstrated a reduction in the IC50 values of SES-NS (67.38 μg/mL) in comparison to SES (106 μg/mL). The present investigation demonstrated the in vitro controlled release pattern and the enhanced anti-inflammatory and cytotoxic activity of SES-NS, suggesting its potential as a promising drug delivery carrier for topical delivery. [ABSTRACT FROM AUTHOR]