Emulsion Solvent Diffusion Technique Research Articles

A novel strategy to produce spherical SBA-15 by polymeric macrospheres as a template for drug delivery

AbstractMesoporous silica SBA-15 has been a material widely studied for drug delivery due to its high biocompatibility and chemical stability, its ordered mesoporous cavities allow drug loading. However, it has a non-spherical particle shape, making it difficult to use in solid dosage forms, where spherical particles are preferred for better flow and distribution. In this regard, this study presented a novel strategy to produce spheric SBA-15 using polymeric macrospheres of a pharmaceutical grade acidic-resistant copolymer (Eudragit®S) stabilized with Pluronic® 123, as a template. The macrospheres of Eudragit®S were fabricated using the double emulsion (W1/O/W2) solvent-diffusion technique and then were used as a template to synthesize macrospheres of SBA-15 following acidic hydrolysis. The physicochemical analysis revealed that the SBA-15 has a spherical morphology (SEM) with pores arranged in a hexagonal lattice (TEM). The XRD showed signals at 0.71, 0.88 y 2.03 °2θ, that were indexed at the Miller indices (100), (110), (200). Nitrogen adsorption-desorption isotherms (type IV, H3) demonstrated mesoporous characteristics with a pore size of 9.3 nm, a wall thickness of 3 nm, a pore volume of 0.7538 cm³g−1, and a surface area of 640 m²g−1. These SBA-15 macrospheres also showed a zero-order release of ibuprofen. The SBA-15 formation using Eudragit®S macrospheres suggests that P123 on the macrosphere acts as a spherical core, as shown by FT-IR analysis. The acid-resistant copolymer maintained macrosphere integrity, enabling the assembly of the SBA-15 mesostructure in a 24-hour manufacturing time under acidic conditions.

Formulation and Evaluation of Nicotinamide Microsponges – The First Step Towards the Development of a Novel Topical Dosage Form

The objective of this work was to formulate and analyze microsponges of nicotinamide. The said formulation was created using the emulsion solvent diffusion technique, and a 3 level two factor-based factorial design was applied to optimize the effect of the stabilizer (X1), as well as drug (X2), amounts on the entrapment efficiency (Y1) and average particle size (Y2). Various parameters, such as flow characteristics, percentage yield, drug concentration, in-vitro drug release tests, entrapment efficiency, and scanning electron microscopy (SEM), were evaluated. All parameters were found to be within the acceptable range. Design Expert 13 was employed to optimize the microsponges, and the optimal batch was determined by examining the desirability data. From this analysis, the optimal amounts of drug and stabilizer were found to be 302.87 and 59.71 mg, respectively. The reliability of the preparation and evaluation of the optimized batch was confirmed by a less than 5% discrepancy between the observed and predicted values of parameters. SEM images revealed that the microsponges were prepared with uniform and spherical morphology. The study concluded that nicotinamide microsponges were successfully prepared and evaluated. Further steps will involve incorporating this formulation into a novel topical dosage form.

Formulation and Evaluation of Miconazole Nanocapsules

Using the emulsion solvent diffusion technique, the current study's goal was to create and analyze miconazole nanocapsules. Ethyl cellulose as well as HPMC nanocapsules were used to fill the miconazole, which has been produced using the emulsion solvent diffusion method. The FTIR data showed that the miconazole nanocapsules filled with ethyl cellulose nanocapsules were stable and that there was no drug-polymer interaction. To determine whether there is no incompatibility in the formulation, compatibility investigations like FTIR & DSC were utilized. The morphological particle size of miconazole nanocapsules is assessed using SEM. This complete formulation codes for the nanocapsules were F1 to F8. The optimum formulation F6's in vitro dissolution rate was found to be 75.22 percent. A variety of mathematical models, including the zero order, first order, Higuchi matrix, and Korsmeyer peppas model, were fitted to the data on drug dissolution in vitro. The model that the miconazole nanocapsules use has R2 values of 0.937, 0.399, 0.899, and 0.785 and m values of 1593, 0.061, 11409, and 2.560. The Nanocapsules released the medication over 45 minutes. The ethyl cellulose and HPMC nanocapsules that contain miconazole were created under ideal circumstances and exhibit good release properties.

Formulation and Evaluation of Microsponge Gel for Topical Delivery of Antifungal Drug

The quasi emulsion solvent diffusion technique was used to create the clotrimazole microsponges, which were eventually recognized as an efficient carrier for the topical delivery of the medicine. The characteristics of the created system were significantly affected by the drug:polymer ratio. It was discovered that microsponges made for prolonged release formulation were effective, and clotrimazole microsponges with gel produced results that were equivalent. Microsponge gel compositions that were prepared beforehand showed regulated medication release. It has been shown that microsponges can transport medications for topical antifungal therapy successfully. Given how well the formulations kept the medication on the skin, it appears that microsponge gel is a more effective drug delivery mechanism than ordinary gel.

Microsponge-derived mini tablets loaded with immunosuppressive agents: Pharmacokinetic investigation in human volunteers, cell viability and IVIVC correlation

Sirolimus, a potent immunosuppressant, has been demonstrated to have remarkable activity in inhibiting allograft rejection in transplantation. The objective of the study was to fabricate microsponge mini tablets with enhanced solubility and bioavailability. β-Cyclodextrin and NEOCEL C91 were selected to prepare the microsponges (SLM-M) to improve the stability and solubility of sirolimus. The current study involved the quasi emulsion-solvent diffusion technique to design sirolimus-loaded microsponges that were further compressed into mini tablets 4 mm in diameter. Solid-state characterization, dissolution at different pH values, stability, and pharmacokinetic profiles with IVIVC data were analyzed in humans. Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction (XRD) were used to characterize the formulations, and high-performance liquid chromatography (HPLC) was used to assess the drug stability of the compressed microsponge minitablets. The API changed from the crystalline state to an amorphous state, as shown by XRD and DSC. The compressed mini tablets showed a 4-fold enhancement in the drug dissolution profile. A toxicology investigation suggested that mini tablets were safe. In humans, the bioavailability of sirolimus compressed mini tablets from SLM-M was significantly improved. The results suggest that mini tablets prepared with β-cyclodextrin and NEOCEL C91 by a quasi emulsion-solvent diffusion process might be an alternative way to improve the bioavailability of sirolimus. In addition, the manufacturing process is easily scalable for the commercialization of drugs to market.

Formulation And Evaluation of Quercetin Loaded Nanosponges of Abiraterone Acetate

A novel idea in medicine delivery is the use of nanosponges. In the current research, an effort was made to create in-situ gel based on nanosponges that contained abiraterone acetate loaded with quercetin. The major purpose of nanosponges is to offer a prolonged release, lessen the negative effects of conventional dosage forms, and enhance the bioavailability of abiraterone acetate by using quercetin as a natural bioenhancer. Combining ethyl cellulose and eudragit in varying quantities, the quasi emulsion solvent diffusion technique was used to create nanosponges and quercetin as a natural bioenhancer. The formulation properties of the produced nanosponges were assessed. All batches of nanosponges had their manufacturing yield and trapping effectiveness assessed. Formulations F 03-P1 and F 07-P2 were found to be the optimum formulations based on results. Both F 03- P1 and F 07-P2 were used to create the gels G1 and G2. Viscosity, spreadability, drug content, and in-vitro tests showing 28.88% drug release after 24 hours all favored G2 as the optimal formulation. A gel base was created using the optimized formulation after it had been tested for scanning electron microscopy (SEM) analysis. Nanosponges containing gel had evaluated for different tests. According to the study, adding drugs to nanosponges can increase the rate of drug release, improve medication targeting at a particular spot, and hence lessen systemic toxicity.

Effect of Different Stabilizers on Spherical Agglomerates of Montelukast Sodium by Quasi Emulsion Solvent Diffusion (QESD)

Abstract: The present study was focused on the spherical crystallization of an asthmatic drug, Montelukast Sodium (MLS) using quasi emulsion solvent diffusion (QESD) technique in which distilled water was an external phase and the internal phase consisted of Ethanol which acts as good solvent and Ethyl acetate as a bridging liquid for recrystallization and agglomeration process. Apart from being poorly water soluble, MLS exhibits poor flow and compressibility. The spherical agglomeration was carried out in the presence of different stabilizers like acacia, PEG 4000, sodium lauryl sulphate, span 40 and tween 80. The prepared agglomerates were characterized in terms of production yield, drug content, solubility, in-vitro release profile, Xray diffraction (XRD), and Fourier transform infra red spectroscopy (FT-IR).The optimized spherical agglomerates exhibited excellent physicochemical and micromeritic properties, solubility and dissolution rate when compared with pure drug .The XRD also revealed a characteristic decrease in crystallinity. The dissolution studies demonstrated a marked increase in the dissolution rate. FTIR study reveals there are no chemical changes in prepared recrystallized agglomerates. The considerable improvement in the dissolution rate of MLS from optimized crystal formulation was attributed to the wetting effect of polymers, decreased drug crystallinity, altered surface morphology and micronization. If this process can be scaled-up to manufacturing level, this technology has the potential to provide the directly compressed spherical agglomerates with improving the physicochemical and micromeritic properties

Development and Characterization of Polymeric Microsponge as a New Vehicle to Deliver Urea Topically.

Topical delivery of therapeutic agents is considered beneficial due to various advantages like ease of administration, avoidance of the first-pass effect, and improved patient compliance. Therefore, scientists around the globe are exploring this route for the delivery of drugs nowadays. The present patent investigation aimed to prepare, optimize, and characterize the urealoaded microsponges for efficient topical delivery in vitro. Urea-loaded ethylcellulose microsponges were prepared using quasi emulsion solvent diffusion technique and optimized using Box-Behnken design (BBD). Furthermore, they were characterized in-vitro using various techniques like scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR), and X-ray diffraction analysis (XRD). In-vitro drug release and release kinetics analysis was also performed. Urea-loaded microsponges were spherical and porous. Optimized urea loaded microsponges showed a minimum size (39.78 ± 1.98 μm), high entrapment (74.56 ± 2.8%), acceptable polydispersity index (PDI) (0.224 ± 0.081) and zeta potential (-21.9 ± 2.9 mV). These microsponges were capable of sustaining the release of urea for 24 h (91.21 ± 5.20%), and the mechanism of release was the combination of diffusion and erosion. The developed microsponge system could be beneficial for topical delivery of urea as it could reduce the dosing frequency of urea and increase patient compliance through its sustained release.

Exploring potential of diacerin nanogel for topical application in arthritis: Formulation development, QbD based optimization and pre-clinical evaluation

Diacerein (DCN) is a chondroprotective agent which shows inadequate oral bioavailability along with gastrointestinal side effects. This study is intended to develop a topical novel DCN delivery system. DCN nanogel was prepared by emulsion solvent diffusion technique. The formulation was optimized by response surface methodology by taking two independent variables, concentration of carbopol 940 and eudragit RSPO and three dependent variables, particle size, % entrapment efficiency (EE) and % drug release at 24 h. The optimized formulation had adequat% EE, % drug release at 24 h and particle size. The particle size for optimized nanogel was 190.3 nm with % EE of 83.51% whereas % drug release at 24 h was found 90.13%. The optimized DCN nanogel was analyzed by differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (DTIR) and transmission electron microscopy (TEM) studies. The drug release kinetic study has shown that the gel followed Higuchi’s model and the diffusion was anomalous in nature. The nanogel was characterized for physical examination, viscosity, homogeneity and stability parameters and the results obtained were found upto the mark. The ex-vivo permeation study data was in correlation with results of in-vitro study. In-vivo anti-arthritic study proved the efficacy of developed formulation for arthritis in Freund’s Adjuvant Arthritic model. This research work has proved the significant potential of innovated product for arthritis by topical route, as it overcomes the drawbacks of oral route, highly efficient, sustained and targeted the release of drug without any accumulation and toxicity.

DEVELOPMENT AND EVALUATION OF MICROSPONGE GEL OF AN ANTIFUNGAL DRUG

Objective: The objective of the present study was to compare the release effect of Luliconazole from different polymeric (Hydrophilic and Hydrophobic) microsponges prepared using varying concentrations. The best microsponge was selected and incorporated into different gel (Natural and synthetic) and drug release is determined and compared with marketed formulation.
 Methods: Polymers such as EC, HPMC, Eudragit RSPO and PVA as emulsifier, and solvent DCM is used as solvent. Microsponge were prepared by using the quasi emulsion solvent diffusion technique. FTIR was studied to estimate the incompatibility. Microsponges were evaluated for SEM, particle size, drug content, and In vitro diffusion studies. Optimized microsponge incorporated gel was prepared by using different gel (flax seed gel and Aerosil gel) were evaluated for pH, spreadability, extrudability, drug content and in vitro diffusion studies.
 Results: Theresults obtainedshowed no physical-chemical incompatibility between the drug and the polymers. EC, HPMC and EC combination was found to be a suitable polymer compared to Eudragit RSPO and other combination in preparation of microsponge. From the evaluation of microsponge, the optimized F1 formulations was incorporated into different gel (flax seeds, aerosil) and compared with marketed formulation in which MG-I (flax seed gel) was considered as good topical anti-fungal microsponge gel based on there physical parameters and drug release kinetics.
 Conclusion: Microsponge and microsponge gel were successfully prepared for Luliconazole and their evaluation studies of each dosage form revealed that topically applied microsponge gel possess immense potential to control the release rate of medicament to improve the bioavailability as well as patient compliance.

Formulation of Solid Lipid Nanoparticles Loaded with Nociceptin/Orphanin FQ (N/OFQ) and Characterization in a Murine Model of Airway Hyperresponsiveness

Asthma is characterized by chronic inflammation and a variable degree of airway hyperresponsiveness (AHR). Our previous papers documented a role for Nociceptin/Orphanin FQ (N/OFQ) and its receptor N/OFQ peptide (NOP) in AHR. Therefore, the aim of this study was to improve the bioavailability of N/OFQ by developing solid lipid nanoparticles (SLNs). N/OFQ-loaded SLNs were prepared by the Quasi Emulsion Solvent Diffusion (QESD) technique and then characterized. Brown Norway rats were sensitized to ovalbumin (OVA) and treated with an intratracheal administration of saline solution or N/OFQ-SLN. Then, 24 h after the last challenge, functional histological and molecular evaluations were performed. SLNs showed a mean diameter of 233 ± 0.03 nm, a polydispersity index (PDI) value around 0.28 ± 0.02 and a drug release percentage of 84.3. The in vitro release of N/OFQ from SLNs showed that the release of the peptide starts already after two hours of incubation. Animals receiving N/OFQ-SLN showed a significative decrease in allergen-induced AHR compared to the control group. These results showed the positive effects of N/OFQ-SLNs on the inflammatory process and on the mechanical properties of the airways, suggesting that the innovative nanotechnological approach may be therapeutically beneficial for asthmatic patients.

PREPARATION AND IN VITRO CHARACTERIZATION OF SOLID LIPID MICROPARTICLES FOR PROTEIN DELIVERY

Objective: The aim of this research was to assess the effect of the process and formulation parameters during the preparation of solid lipid microparticles. Solid lipid microparticles (SLMs) have evident advantages such as biocompatibility, simplicity of production and characterization, prolonged release, and especially high protein loading capacity, despite being less investigated than lipid nanoparticles.Material and Method: SLMs were prepared via emulsion solvent diffusion technique using glyceryl tridecanoate (GTD) as a biocompatible and biodegradable lipid. The optimum formulation conditions for producing homogenous spherical microparticles were found and represented by a triangle phase diagram area. After optimizing the particle size and encapsulation efficiency by changing the formulation parameters, the microparticles were characterized by in vitro release, morphological analysis, thermal analysis and electrophoretic analysis on the selected formulations.Result and Discussion: The maximum drug loading efficiency was achieved by combining 100 mg of lipid, 60% triacetin and 3% emulsifier. The average microparticle size was observed as 8.9 μm. The in vitro drug release were analyzed in pH 7.4 phosphate buffer and were mainly completed at 8th hour.

Formulation and evaluation of orlistat loaded microsponges for the treatment of obesity

The motivation behind this investigation was to design novel drug delivery system containing orlistat micro sponges. Microsponges containing orlistat and Ethyl cellulose/ Eudragit RS 100 prepared by quasi emulsion solvent diffusion (Technique) method. The formulations were prepared step by step increases Drug: polymer ratio. The particle size (Malvern analyzer), Surface Morphology and structure examination (SEM) Production yield, Drug entrapment Efficiency and in vitro drug release studied of microsponges were examined. Shape or surface morphology and topography of the orlistat microsponges were examined by scanning electron microscopy. The drug orlistat disperse in GIT for better therapeutic effect as microsponges disperse freely in GIT. To improve absorption of orlistat so as to enhance bioavailability, micro sponges is used as delivery systems which show better absorption and bioavailability then other dosage form of orlistat. The particle size were prepared microsponges was observed in the range of 50.45 ± 0.85µm to 57.77 ± 1.35µm. The drug entrapment of the orlistat microsponges was observed in the range of 73.23 ± 0.23 to 83.41 ± 1.17 % The in vitro drug release study of the microsponges over 8 hour range from 59.28 ± 0.41% to 73.16 ± 0.89 %. The objective of this research work was to formulation and evaluation of orlistat loaded microsponges for management of obesity disease. Microsponges drug delivery system landscape have been highly and rapidly evolving. They are allowing for novel product form. Microsponges are safe biologically and extraordinary preferred position programmable release. This delivery system are being integrated to optimize the efficacy or free streaming effectiveness treatment.

Formulation and evaluation of polymeric microspheres of a poorly soluble drug celecoxib

The aim of this present work was to formulate microspheres of BCS Class II drug Celecoxib. The drug was identified by melting point study and FT-IR spectroscopy. Therapeutic success of a drug is greatly depended on its bioavailability. Majority of the recently discovered drugs shows poor solubility (BCS Class II) which decreases the bioavailability upon oral administration. Microspheres are a novel technique to circumvent this obstacle, which can increase bioavailability of drugs significantly. Polymeric microspheres with Polyvinylpyrrolidone and Eudragit L-100, prepared by Emulsion Solvent Diffusion and Evaporation technique, showed a range of drug release profile at intestinal pH 6.8. Different batches of microspheres were prepared by varying the drug-polymer ratio. Microparticulate systems like microspheres improve absorption which increases the bioavailability, ultimately leading to more efficient drug therapy. The microsphere system also provides protection to the gastric mucosa from GIT-irritant drugs thus decreasing toxic effects and sustained releases allows lower dosage frequency. Prepared microspheres were evaluated on various parameters like entrapment efficiency, %yield, particle size, scanning electron microscope analysis, and in-vitro drug release profile. Solid spherical microspheres were produced which showed good entrapment efficiency (43%-91%) and released 70-90% of the drug content in 10hrs.

RESEARCH ARTICLE ON NANOGEL AS TOPICAL PROMISING DRUG DELIVERY FOR PSORIASIS

Background: Transdermal medication administration seems promising, but it is a difficult method to implement for both local and systemic drug effects.
 Objective: The goal of this study was to create a nanogel with a smaller particle size in order to increase the bioavailability of Curcumin, an anti-inflammatory and anti- psoriasis medication.
 Methods:The goal of this research is to create nanosize Curcumin dispersion using an emulsion-solvent diffusion technique with the addition of a gelling agent to create a nanogel. Particle sizes in the formulation range from 100 to 400 nanometers. Curcumin is a medication that is used to treat psoriasis and chronic inflammatory disorders.
 Results: The glycerol:waterco-solvent system was chosen for the preparation of curcumin nanogels with various polymers because it has a higher permeability coefficient than the alcohol:water co-solvent system. In a franz diffusion cell, permeation across cellophane membrane was achieved using 0.9 percent w/v sodium chloride as the receptor fluid. Curcumin-containing gels with eudragit polymer had a higher permeability coefficient.
 Conclusion: In compared to nanogels made with HPMC and methyl cellulose, curcumin nanogels produced with carbopol with permeation enhancer showed greater flux improvement. Curcumin nanogels with carbopol 940 as a gelling agent and Eudragit S-100 as a permeation enhancer.

Ocular Delivery of Atenolol Loaded Microsponge in-situ Gel: Development, Characterization and in-vitro Evaluation

Abstract: Aim/Background: The purpose of the study was to fabricate and evaluate atenolol loaded micro-sponge in-situ gel. Materials and Methods: Oil in Oil Emulsion Solvent Diffusion Technique was used for formulation of microsponges by using different levels of polymers such as Eudragit RS-100 and Ethyl Cellulose. The prepared micro-sponges were evaluated for optical microscopy, percentage yield, drug content, entrapment efficiency and surface morphology studies. The micro sponges were loaded into in-situ gel. The gel was characterized for pH, rheological behavior, in vitro gelling capacity and in vitro drug release study. Results: The smicrosponges were found in the size range of 7.43 to 9.26μm. The formulation F1 has smallest particle size while F9 has largest size. The product yield varies from 66.98% to 89.87 %.The drug content was found to be maximum for formulation F8 which is 94.19%. Similarly, the entrapment efficiency was found maximum for formulation F8 which is 93.89%. The gel was characterized for pH. The pH of drug loaded microsponge gel were found in range of 7.43±0.27 to 9.26±0.61.Similarly, viscosity ranges from 32 to 39 cps. The data of in-vitro release shows that 60.12% drug was released up to 24hr. Conclusion: The mirosponges laden in situ gel was effectively prepared by oil in oil emulsion solvent diffusion method (O/O ESDM). Further, the formulation will provide benefits in terms of sustained/controlled release, reduces dosing frequency and provides better compliance to the patient. Key words: Microsponge, Atenolol, Ethyl Cellulose, Eudragit RS-100, in situ gel.

Formulation and Evaluation of Lamotrigine Loaded Nanosponges

The main purpose of this investigation study is to fabricate nanosponges with good entrapment efficiency and percentage of yield to enhance the solubility and dissolution rate of poorly water soluble antiepileptic molecules of Lamotrigine, which belongs to BCS - II class. Lamotrigine nanosponges were prepared using emulsion solvent diffusion technique and the immediate release tablets of lamotrigine nanosponges were prepared by direct compression method. Nanosponges were formulated using different polymers ratio like EC and PVA. The optimized batch containing ratio 2:1:2 of drug, ethyl cellulose and PVA shows maximum entrapment efficiency and percentage of yield. The optimized nanosponges of lamotrigine (F1) were subjected for Practical yield, drug content, Saturation solubility, zeta potential, Fourier transform Infrared spectroscopy (FTIR), Differential Scanning Calorimetry (DSC) and Scanning electron microscopy(SEM). The optimized formulations (F1) of nanosponge based immediate release tablets compression parameters were also studied. The In-vitro dissolution was carried out by USP apparatus type II (Paddle Method) with 900 ml of 0.1 N HCl at 50 rpm. At definite time intervals, 5 ml of the receptor fluid were withdrawn, filtered and analyzed spectro-photometrically at wave length 265 nm. The compressed lamotrigine nanosponge shows 99.7% at the end of dissolution and it follows first order kinetics and best fit with Higuchi’s model. In this research solubility and dissolution demonstrated for nanosponge formulation.

ROSUVASTATIN CALCIUM NANOSPONGES IN THE FORMULATION OF EXTENDED RELEASE TABLETS

Cyclodextrin has been recognized as a linker molecule that can link with the various drug substances to produce a nano-porous structure called nanosponges (NS) and increase the dissolution rate of poorly soluble drug substances. This work aimed to load rosuvastatin calcium (RSC) with solubility enhancer’s β-cyclodextrin (β-CD) or polyvinyl alcohol (PVA). β-CD based RSC-NS were fabricated by the emulsion solvent diffusion technique; with solubilizer dichloromethane and different ratios of ethyl cellulose as a co-polymer. Characterization of the prepared nanosponges was done by various testing procedures that confirm its nanosize and particle size and drug release. RSC loading in NS was assessed by DSC, FTIR and SEM. Among all the formulations F5 has 78.23 % entrapment efficiency. 2-3 folds of increased solubility were obtained with RSC-NS. F1-F6 formulations released 76.35 % - 98.69 % of the drug at the end of 30 min. In the preparation of extended-release tablets, NS prepared from F5 formulation was used and the best tablet formulation was selected based on various evaluation tests. All the formulations except S3, S8 followed first-order release kinetics. S1 & S2 drug release mechanism is Higuchi while other formulations are Korsemeyer-Peppas, so the release mechanism for most of the formulations is erosion than diffusion.

Acetoxy DMU-loaded carboxymethylchitosan nanocapsules: preparation and in vitro release evaluation followed by an analytical methodology validation

ABSTRACT Acetoxy DMU (Ac.DMU – 1,2,3-trimethoxy-5-(4-acetoxystyryl) benzene) is a potential new drug, compared to resveratrol, due to its improved pharmacokinetic properties. Nanoencapsulation using Ac.DMU and carboxymethylchitosan (CMCh) polymer is a promising alternative for improving the bioavailability of drugs in human bodies. Nanocapsules (NCs) based on CMCh with Ac.DMU (Ac.DMU-NCs) by emulsion solvent diffusion technique in different drug-to-polymer ratios have been prepared with encapsulation efficiency of 69.4% and 51.5% and characterized by dynamic light scattering, ζ-potential, and infrared spectroscopy techniques. In vitro release experiments of free Ac.DMU and Ac.DMU-NCs showed an improvement in the solubility of Ac.DMU by NCs, enabling a fast drug release rate. In addition, the method was validated through analyses of specificity, linearity, limit of detection and quantification, accuracy, and precision according to the standards suggested by the International Conference on Harmonization. UV–Vis spectroscopy used to quantify Ac.DMU ensured reliable results for the amount of encapsulated Ac.DMU. The results suggest a promising potential of NCs as carriers of the hydrophobic drug Ac.DMU for controlled release.

Dapsone-Loaded Microsponge Gel for Acne Management: Preparation, Characterization and Anti-Microbial Activity

Background: Acne vulgaris is a chronic inflammatory disorder involving Propionibacterium acnes and activation of lymphocytes and neutrophils. Dapsone (sulfone drug) possesses potent anti-microbial activities and hence, it is used to cure multiple inflamed acne lesions. Howbeit, its therapeutic utility is hampered, owing to its poor solubility and side effects like mild irritation and dryness. These problems, along with orange-brown discoloration on skin, restrict the topical application of this drug. Objective: The objective of the present investigation was to address the above-mentioned limitations like irritation, dryness, and skin discoloration of dapsone via formulating microsponge based gel of this moiety. Methods: Dapsone microsponges were fabricated and embedded into a carbopol gel for topical application. The drug loaded ethylcellulose microsponges were crafted employing a quasi emulsion solvent diffusion technique. Besides routine characterization, these microformulations were assessed for entrapment, particle size analysis, and drug release. Furthermore, anti-acne potential was also evaluated against Propionibacterium acnes and Staphylococcus aureus to check their therapeutic efficiency. The prepared dapsone microsponge gel was assessed for its viscosity, spreadability, texture, and drug release. Results: Results revealed that dapsone loaded microsponges were successfully fabricated and found to possess good encapsulation efficiency (84.68 ± 5.73%), which is in micro-size range (88.06 ± 2.97 μm to 315.87 ± 1.99 μm) and showed cumulative drug release of 52.52 ± 0.2%. Field emission scanning electron microscopy illustrated spherical, uniform, and spongy microparticles. The developed micro formulation showed promising activity against the chosen acne bacterias and improved stability. Conclusion: The obtained results corroborate the premise that dapsone loaded microsponge gel can be an effective strategy for acne management.