Emulsion Solvent Diffusion Method Research Articles

Rhein and hesperidin nanoparticles remodel tumor immune microenvironment by reducing CAFs and CCL2 secreted by CAAs for efficient triple-negative breast cancer therapy

In triple-negative breast cancer (TNBC), the tumor immune microenvironment (TIME) is a highly heterogeneous ecosystem that exerts indispensable roles in tumorigenesis and tumor progression. Cancer-associated fibroblasts (CAFs) and cancer-associated adipocytes (CAAs) are the main matrix components in the TIME of TNBC. CAFs mediate the edesmoplastic response, which is a major driver of the immunosuppressive microenvironment to promote tumor growth. In addition, CAAs, a type of tumor-educated adipocyte, participate in crosstalk with breast cancer and are capable of secreting various cytokines, adipokines and chemokines, especially C–C Motif Chemokine Ligand 2 (CCL2), resulting in changes of cancer cell phenotype and function. Therefore, how to treat tumors by regulating the CAFs and the secretion of CCL2 by CAAs in TIME is investigated here. Our research group previously found that rhein (Rhe) has been identified as effective against CAFs, while hesperidin (Hes) could effectively diminish CCL2 secretion by CAAs. Inspired by the above, we developed unique PLGA-based nanoparticles loaded with Rhe and Hes (RH-NP) using the emulsion solvent diffusion method. The RH-NP particles have an average size of 114.1 ± 0.98 nm. RH-NP effectively reduces CAFs and inhibits CCL2 secretion by CAAs, promoting increased infiltration of cytotoxic T cells and reducing immunosuppressive cell presence within tumors. This innovative, safe, low-toxic, and highly effective anti-tumor strategy could be prospective in TNBC treatment.

Formulation and evaluation of Dorzolamide hydrochloride microsponges loaded in situ gel for ocular administration

Due to the unique structure of the eye, which inhibits the entry of drug molecules into the desired site, the ophthalmic delivery of the drug has been one of the most challenging tasks for a pharmaceutical scientist. For this reason, in this investigation a novel microsponge for an anti-glaucoma drug, Dorzolamide hydrochloride, was formulated as in situ gel for ocular administration with an aim to improve its therapeutic efficacy and reduce the systemic adverse effects. The microsponges were prepared by the quasi emulsion solvent diffusion method and was incorporated into 20% pluronic F-127 which led to consistent in situ gel at 35°C. They were evaluated for physicochemical properties like pH, gelling capacity, gelation time, rheological properties and release profile and ocular irritancy test. The prepared Dorzolamide hydrochloride microsponges showed high entrapment efficiency of 85% and mean particle size of 2 μm with polydispersity index (PDI) of 0.77 which are ideal for ocular delivery. These microsponges is formulated into in situ gel which showed higher therapeutic efficacy compared to free drug in gel. It was found to be non-irritant to the rabbit’s eye. These results confirms that Dorzolamide hydrochloride microsponges in situ gels have promising features, benefits and advantages for a novel ophthalmic drug delivery to treat glaucoma.

Effect of White Rice Flour in the Formulation Development and Evaluation of Sumatriptan Succinate Floating Microspheres by Modified Emulsion Solvent Diffusion Method

A sustained release system for Sumatriptan designed to increase its residence time in the stomach without contact with the Microspheres was achieved through the preparation of floating Microspheres by the Modified Emulsion solvent Diffusion method. In the present study attempt has been made to develop sustained released drug delivery system by formulating the floating Microspheres of Sumatriptan using White Rice Flour powder as a natural polymer which is biodegradable, biocompatible, nontoxic, economically cheap cost, devoid of adverse and side effects and easily availability. Sumatriptan Succinate is the succinate salt form of sumatriptan, a member of the triptan class of compounds with anti-migraine property. Sumatriptan succinate selectively binds to and activates serotonin 5-HT1 receptors. The 12 batches of floating Microspheres (MF1 to MF12) were formulated by Modified Emulsion solvent Diffusion method using different ratio of polymers like White Rice Flour power, HPMC K4M and Carbopol. The formulated Microspheres were evaluated by means of different parameters like shape and density of Microsphere, drug content uniformity, In-vitro buoyancy, swelling Index, In-vitro dissolution studies. The formulation MF6 has better sustained release when compared other formulations, hence we conclude that the combination of White Rice Flour powder, HPMC K4M shows better Gastric retention time which sustains the release of the dosage form.

Design, characterization and optimization of Rosuvastatin calcium nanosponges loaded transdermal patch

Rosuvastatin calcium is a low solubility containing anti-lipidemic drug and provides only 20% of oral bioavailability. Following a different route of administration can overcome the first pass metabolism and may improve the bioavailability. Therefore the present study aimed to design and characterize a transdermal patch containing rosuvastatn calcium nanospoges (RST-NSP) to enhance the drug dissolution. Emulsion solvent diffusion method was used in the preparation of (RST-NSP) employing β-cyclodextrin and poly vinyl alcohol as solubility enhancers. Design Expert® 13 was employed to design twenty formulations in which concentration of β-Cyclodextrin in mg (A), ethylcellulose in mg (B) and reaction time in hrs (C) were taken as independent factors, where as entrapment efficiency (%) and particle size were considered two responses. Triple fold increase in solubility, 86 % of entrapment efficiency, 200 nm particle size containing NSP were loaded in transdermal patch by solvent casting method, with hydroxypropyl methyl cellulose and cabopol as polymers in 3:1 ratio. SEM analysis showed the uniform distribution of nanosponges and its morphology. The transdermal patch loaded NSP released the drug up to 10 h. Kinetic modeling on release data showed that the best fitted model was Higuchi model and release mechanism was by Fickian diffusion.

Formulation and evaluation of cidofovir loaded microspheres

The study aimed to produce and assess cidofovir microspheres using the emulsion solvent diffusion method. Microspheres loaded with ethyl cellulose and HPMC were prepared. FTIR analysis confirmed stability with no drug-polymer interaction, and compatibility investigations ensured formulation compatibility. SEM determined particle size, with yields ranging from 84.44% to 87.62% and drug content from 64.8% to 97.2%. Particle sizes ranged from 20 µm to 210 µm, with drug loading capacities of 55.6% to 96.8% and entrapment efficiencies of 55.5% to 89.1%. Swellability studies showed a range of 0.6 to 1.6 seconds. Formulation CM8 exhibited optimal dissolution in vitro at 62.87%. Drug dissolution data were fitted to various models, with R2 values ranging from 0.937 to 0.061. Up to 45 minutes of drug release was observed. Overall, cidofovir-loaded HPMC and ethyl cellulose microspheres showed favorable release properties under optimal conditions.

PREPARATION AND CHARACTERIZATION OF FLUCONAZOLE TOPICAL NANOSPONGE HYDROGEL

Objective: The study aimed to develop a polymeric nanosponge-based hydrogel system for enhanced topical application of fluconazole, an antifungal drug. Methods: Nanosponges were formulated using the emulsion solvent diffusion method using various polymers like hydroxypropyl methylcellulose, ethylcellulose and Eudragit RS 100. Polyvinyl alcohol and ethanol were used to prepare the aqueous and dispersed phases. Nanosponges were dispersed in an appropriate amount of gelling agent Carbopol 940 to get nanosponge gel. Drug–polymer interaction has been carried out by FTIR spectroscopy. The prepared nanosponges were evaluated for various tests like production yield, drug entrapment efficiency, compatibility and SEM studies. The nanosponge hydrogel was tested for pH, drug content, spreadability, in vitro diffusion and kinetic studies. Results: The drug entrapment efficiency of fluconazole nanosponges was found in the range of 52.3±0.84% to 80.8±0.36% for all formulations, respectively. The spreadability of prepared nanosponges gel formulation was in the range between 5.20±0.19 to 7.187±0.85. Particle size analysis showed that the average particle size of fluconazole nanosponges formulated using ethyl cellulose (F5) was found to be 334 nm. The zeta potential was found to be-10.4 mV, indicating the formulated fluconazole nanosponges (F5) had moderate stability. FTIR and DSC studies of pure drug and nanosponges suggested that the formulations were stable and there was no chemical interaction with polymer and other excipients. The optimised fluconazole topical nanosponge hydrogel (FG5) released 90.90% drug in 8 h. Conclusion: Fluconazole topical nanosponge hydrogel could be successfully prepared by emulsion solvent diffusion method. Fluconazole topical nanosponge hydrogel showed promising results under in vitro condition and thus, there exists a scope for evaluation of the developed nanosponge hydrogel for further pharmacokinetic studies, using appropriate test models.

Formulation and Optimization of Valganciclovir-loaded Nanosponges

The objective of our study was to form a novel method of delivering drugs that would improve the effectiveness of valganciclovir, an antiviral medication used to treat cytomegalovirus (CMV) infection in individuals with weakened immune systems. The drug’s induction dosage has limited penetration and requires very high doses. The nanosponges were synthesized using the emulsion solvent diffusion method, employing a 32 full factorial design to determine the combined impact of 2 independent variables: Quantity of ethyl cellulose and stirring speed. The dependent variables assessed were zeta potential, polydispersity index (PDI), and entrapment efficiency. Improved formulation exhibited an entrapment efficiency of 83.61%, a zeta potential. of -17.6 mV, and a PDI of 0.51. The improved formulation exhibited a continuous and controlled release of the medication. The produced nanosponges were characterized using fourier transform infrared (FTIR), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM).

Design and Characterization of Hallow Porous Floating Microspheres of Favipiravir

The present investigation deals with the design and characterization of favipiravir floating microspheres for gastro retentive drug delivery system by employing 3² factorial design and also to investigate the main effects of different independent variables on microspheres that float. The emulsion solvent diffusion method was used to manufacture floating microspheres with Eudragit S 100 as the polymer. These microspheres will extend the release of the medicine, reducing the frequency of administration and the harmful effects caused by fluctuations in plasma concentration with conventional dosage forms. The main effect of independent variables like polymer Eudragit S 100 concentrations (50, 100, 150 mg) and stirring time (1, 2 and 3 hours) on the performance of microspheres. Formulated microspheres were characterized for responses including drug release, particle size, and entrapment efficiency and floating time. Based on the results of the responses, the optimized composition was arrived using the response surface method graphical and numerical optimization method using design of experiments (DoE) software. Then, the optimized formulation (OFES) was prepared and evaluated for the four responses compared with predicted values to find the validity of the selected model. The optimized formulation was further analyzed for drug-excipient compatibility by fourier-transform infrared (FTIR), differential scanning calorimetry (DSC), and also analyzed by X-ray diffraction (XRD), scanning electron microscope (SEM) analysis. Further zeta potential and micrometric properties were also observed. The results for the formulation FES 1 to 9 found were, that particles size ranged from 0.192 to 0.277 μm, entrapment efficiency ranged from 68.65 ± 1.9 to 76.25 ± 3.2%, percentage drug release range was from 89.25 ± 0.24 to 93.68 ± 0 .25%, and floating time range was from 12 to 23 hours. As per the design, OFES an optimized formulation fitted with the concentration of Eudragit S 100 of 139.1 mg and stirring time of 1-hour. Regarding the kinetic release, the responses were best fitted with Higuchi model of R² value of 0.9795 with kinetic mechanism of non-fickian diffusion with R² value of 0.9499, indicating good linearity. The combination of different variables and their effects on responses were investigated well using factorial design, and an optimized formulation was developed for favipiravir.

Targeting Breast Cancer: Encapsulation and In-vitro Studies of α-Amyrin from Capparis zeylanica L.

Historically, Capparis zeylanica L. has garnered attention for its potential effectiveness in treating cancer. This has inspired the researchers to delve into the plant’s properties in search of new and innovative compounds with anticancer properties. Therefore, the current study aimed to encapsulate and characterize α-amyrin phytochemical from leaf extract of C. zeylanica L. and study it for the in-vitro cancer cell line. The high-performance liquid chromatography (HPLC) method development of C. zeylanica L. extracts furnished α-amyrin, whose characterization was established by high-performance liquid chromatography (HPLC), fourier-transform infrared spectroscopy (FTIR), liquid chromatography-mass spectrometry (LC-MS). Molecular docking was performed using Auto Dock Vina software to validate the mechanism of action. The α-amyrin nanosponges was synthesized through the emulsion solvent diffusion method, employing various drug-polymer ratios ranging from 1:1 to 1:5, with pullulan as the chosen polymer. Compatibility was revealed no interaction using FTIR. The cytotoxic properties were assessed on MCF-7 cell lines using MTT assay. The production yield and entrapment efficiency of F1-F5 batches in the range of 43 to 68.36% and 70 to 82.5%, respectively. Batch F5 showed the highest production yield, and entrapment efficiency. The average particle size ranges from 241.3 to 603.2 nm. The F5 formulation had shown the highest drug release (90.40 ± 0.88%). The IC50 value for optimized formulation was 34.54 μg/mL as observed in MCF-7 breast cancer, which was considerable as compared with 5-fluorouracil. In-silico studies revealed that α-amyrin showed good binding affinity to breast cancer PDBIDs and form a stable complex. In our study, α-amyrin has been successfully extracted and further validation through pharmaceutical formulation was done and warranted to solidify its potential as an effective anticancer agent.

Formulation and Characterization of Simvastatin-Loaded Nanosponges: An Innovative Technique for Colon-Targeted Drug Delivery

Background:: To enhance the solubility of simvastatin by improving the surface area of the drug particle by preparing nanosponges that are enclosed in a tablet and capsule oral solid dosage forms, which in turn helps maintain the drug's stability. Objective:: The present investigation aimed to develop a simvastatin nanosponge containing Eu-dragit as a polymer with different ratios of drug-to-polymer concentration to increase its solubility and further improve the oral bioavailability by using nanosponges’ formulation technique. Methods:: The emulsion solvent diffusion method was used to prepare simvastatin nanosponges by using Eudragit S 100, Eudragit L 100, and a combination of both in different drug-to-polymer ratios, i.e., 1:0.5, 1:1, 1:1.5, and 1:2. To characterize the conductivity, molecular changes, and size of the prepared nanosponges, a variety of evaluation parameters, including the compressibil-ity index, Hausner's ratio, angle of repose, microscopy, production yield, entrapment efficiency, drug content, in vitro drug release studies, DSC, XRD, FTIR, and SEM were evaluated. Opti-mized formulation was used to prepare colon-targeted tablets and capsules by taking nanosponges equivalent to 20 mg of simvastatin. Results:: The percentage yield, drug content, and entrapment efficiency of the final formulation were observed at 81 ± 0.26%, 92.4%, and 97 ± 0.56%, respectively. The in vitro drug release of the optimized formulations was 91.42 % at 12 hrs. The drug release followed the Peppas model with a super case II transport mechanism. Conclusion:: The use of the nanosponge delivery system increased the solubility of simvastatin seven times, which in turn increased the drug's bioavailability.

Unveiling the potential of microsponges: Enhancing oral bioavailability

Oral medication administration is widely recognized as the most practical and widely used method. Medications with a short half-life and easy absorption in the gastrointestinal tract are quickly removed by the bloodstream. To avoid these issues, oral controlled-release formulations have been created. There are a ton of novel formulation approaches in the realm of medication delivery systems. One new novel approach that is becoming increasingly well-liked these days is the usage of microsponges. A wide variety of active chemicals can be entrapped by the highly cross-linked, porous, polymeric structure that makes up the Microsponges Delivery System (MDS). Various polymers like ethyl cellulose, polystyrene, etc., have been utilized in forming microsponges and these active microsponges can be incorporated into formulations, such as capsules, gel, and powders, and have a broad package of benefits. The microsponges have satisfactory stability over pH values ranging from 1 to 11, they exhibit reasonable stability at temperatures as high as 130, and entrapment efficiency is great, reaching 50–60%. The preparation of microsponges involves the Quasi-emulsion solvent method, and the emulsion solvent diffusion method the release of drug through microsponges increases with increasing drug-polymer ratio and lowering polymer wall thickness. The microsponges are characterized for visual characterization, zeta potential, entrapment efficiency, and drug content. This review is focused on their advantages over other dosage forms, methods of preparation, characterization, and application of microsponges.

Formulation and evaluation of voriconazole nanocapsules

The current study's goal was to create as well as assess voriconazole nanocapsules using the diffusion of emulsion solvent technology. Voriconazole was made using the emulsion solvent diffusion method and is loaded with ethyl cellulose and HPMC Nanocapsules. The FTIR data showed that there was no drug-polymer interaction and that voriconazole nanocapsules filled with ethyl cellulose were stable. The absence of incompatibility in the formulation was investigated using compatability investigations such as FTIR and DSC. SEM is used to determine the morphological particle size of the voriconazole nanocapsules. F1 through F8 are the complete formulation codes for which the nanocapsules were tested. A percentage yield of 83.32% to 88.61% was discovered. There was 65.8 to 98.5% drug content. The nanocapsules' particle size ranged from 78 µm to 33 µm, while their drug entrapment effectiveness ranged from 54.4% to 91.4% and their drug loading capacity from 56.8% to 97.7%. The study period for swellability was 0.8 to 1.5 seconds. The optimal formulation, F8, showed an in vitro dissolving rate of 61.89%. Numerous mathematical models, including zero order, first order, Higuchi matrix, and Korsmeyer Peppas model, were fitted to the available data on drug dissolution in vitro. The R2 value and m value of the Voriconazole Nanocapsules model were 0.937, 0.399, 0.899, 0.785, and 2.560, respectively. Up to 45 mints of medication were released from the nanocapsules. The HPMC and ethyl cellulose-loaded Voriconazole nanocapsules were made under ideal circumstances and have good release properties.

Formulation Development, Optimization and Evaluation of Flurbiprofen Microsponge Tablet for the Treatment of Rheumatoid Arthritis (RA) by using Box- Behnken Design.

Rheumatoid arthritis (RA) is a chronic, autoimmune and inflammatory disease that mostly impacts the joints. Chronotherapeutics refers to a treatment method in which in-vivo drug availability is timed to match rhythms of disease in order to optimize therapeutic outcomes and minimize side effects. Flurbiprofen is a non-steroidal anti-inflammatory drug, indicated for the relief of inflammation. The aim of the present study was to develop & optimize the microsponges based of Flurbiprofen tablet for Chronotherapeutics for enhanced therapeutic effect. Microsponges were developed by Quasi Emulsion solvent diffusion method. Prepared microsponges were optimized in order to analyze the effects of independent variables like concentration of PVA (X1), Volume of Dichloromethane (X2) & stirring speed (X3) on the Entrapment Efficiency (Y1), Mean particle size (Y2) and Drug release at 8 hr (Y3) using box Behnken design. The optimized formulation was subjected to in vitro study and Comparison with marketed formulation. With release kinetics study. The optimized formulation Batch (F-18) Show particle size of 49.12µm, entrapment efficiency of 87.46%, and drug release at 8 h 70.49%, which is under the acceptance criteria, which is more effective compared with Marketed tablet. The results showed that, as stirring speed increases, the particle size decreases and entrapment efficiency increases. While volume of dichloromethane increases, particle size decreases. Morphology was found to be porous and spherical. Optimized batch of Flurbiprofen microsponge was further formulated in future for invivo study and clinical trials.

Formulation and evaluation of Glibenclamide loaded Nanosponges

Nanotechnology mediated drug delivery has been reported to enhance the drug efficacy, bioavailability, reduced toxicity and improve patient compliance by targeting the cells and tissues to elicit the desired pharmacological action. The main aim of the study was to formulate Glibenclamide loaded nanosponges and to evaluate them. Glibenclamide loaded nanosponges were prepared by Emulsion solvent diffusion method using different polymers (Ethyl cellulose, β- cyclodextrin, Hydroxy Propyl β- cyclodextrin, Pluronic F68). The FTIR test is conducted as the preliminary test, by this test there was no interaction between the drug and polymers. Then nanosponges were evaluated for particle size, PDI, zeta potential, SEM, entrapment efficiency and invitro drug release. The particle size ranged from 640.7 to 876.2 nm, PDI ranged from 0.456 to 0.707, zeta potential from -17.3 to -34.3 mV and entrapment efficiency was ranged from76.21 to 98.23% The cumulative percentage release from all nanosponges varied from 80.35 to 97.56% after 12 hours depending upon the drug and polymers ratio and F5 formulation showed highest drug release i.e., 97.53%. The release kinetic studies showed that the release first order diffusion controlled and the n value (0.8769) from the Korsmeyer- Peppa’s model indicated the release mechanism was non-fickian type.

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.

Magnetic Aggregation-Induced Bone-Targeting Nanocarrier with Effects of Piezo1 Activation and Osteogenic-Angiogenic Coupling for Osteoporotic Bone Repair.

Osteoporosis, characterized by an imbalance in bone homeostasis, is a global health concern. Bone defects are difficult to heal in patients with osteoporosis. Classical drug treatments for osteoporotic bone defects have unsatisfactory efficacy owing to side effects and imprecise delivery problems. In this study, a magnetic aggregation-induced bone-targeting poly(lactic-co-glycolic acid, PLGA)-based nanocarrier (ZOL-PLGA@Yoda1/SPIO) is synthesized to realize dual-targeted delivery and precise Piezo1-activated therapy for osteoporotic bone defects. Piezo1 is an important mechanotransducer that plays a key role in regulating bone homeostasis. To achieve dual-targeting properties, ZOL-PLGA@Yoda1/SPIO is fabricated using zoledronate (ZOL)-decorated PLGA, superparamagnetic iron oxide (SPIO), and Piezo1-activated molecule Yoda1 via the emulsion solvent diffusion method. Bone-targeting molecular mediation and magnetic aggregation-induced properties can jointly and effectively achieve precise delivery to localized bone defects. Moreover, Yoda1 loading enables targeted and efficient mimicking of mechanical signals and activation of Piezo1. Experiments in vivo and in vitro demonstrate that ZOL-PLGA@Yoda1/SPIO can activate Piezo1 in bone defect areas of osteoporotic mice, improve osteogenesis through YAP/β-catenin signaling axis, promote a well-coordinated osteogenesis-angiogenesis coupling, and significantly accelerate bone reconstruction within the defects without noticeable side effects. Overall, this novel dual-targeting nanocarrier provides a potentially effective strategy for the clinical treatment of osteoporotic bone defects.

Design, Development and Evaluation of Nanosponges Loaded Topical Gel for Rejuvenation of Skin

The study aimed the development of nanosponges was the choice due to the numerous advantages of this novel technology over the others. Rutin was chosen as it has excellent antioxidant potential. The compatibility study was performed using Fourier transform infrared (FTIR) and there was no interaction found. The optimization study was brought off by Design expert software (version.13). Nanosponges were prepared by emulsion solvent diffusion method. The prepared sponges were brimmed in a night gel formulation for their suitable delivery to the skin. The prepared nanosponges were evaluated for various parameters such as particle size analysis, entrapment efficiency and zeta potential which were found in the acceptable limit. In-vitro permeation study was carried out using Franz-diffusion cell and the cumulative percent drug permeation was found to be 69 to 84.5% in 30 hours. A gel formulation was prepared using rutin-loaded nanosponges and studied for various parameters such as pH, viscosity, and extrudability for various combinations using NS-4. Ex-vivo drug diffusion study reveals that the night gel took 300 minutes for 78.26 to 94.16% permeation. The IC50 values of the flavonoid combination, NS-4 was found to be 54.70, 52.76, and 51.65 μg/mL in the different in-vitro models viz. DPPH, when compared to that of the standard ascorbic acid. Conclusively, the objective of delivery of rutin using nanosponges as carriers for the target delivery was achieved by NS-4 formulation and successfully delivered as night gel for skin rejuvenation.

Study the Variables Affecting Formulation of Ethylcellulose-based Microsponges Loaded with Clobetasol

Clobetasol propionate (CP) is a super potent corticosteroid widely used to treat various skin disorders such as atopic dermatitis and psoriasis. However, its utility for topical application is hampered due to its common side effects, such as skin atrophy, steroidal acne, hypopigmentation, and allergic contact dermatitis. Microsponge is a unique three-dimensional microstructure particle with micro and nano-meters-wide cavities, which can encapsulate both hydrophilic and lipophilic drugs providing increased efficacy and safety. The aim of the current study is to prepare and optimize clobetasol-loaded microsponges. The emulsion solvent diffusion method is used for the preparation of ethylcellulose (EC)-based microsponges. The impact of various formulation variables on microsponge's properties includes; drug: polymer ratio, polyvinyl alcohol (PVA) quantities, the volume of external phase, and stirring rates investigated. The microsponges were characterized in terms of particle size, product yield, CP entrapment %, and in-vitro drug release behavior. The results report that increasing EC concentration led to a significant increase in particle size, with a decrease in product yield and drug entrapment %. Increasing stirring speed or external aqueous volume or PVA w/v % caused a non-significant decrease in production yield and CP entrapment % but showed a significant decrease, and increase in particle size, respectively. Finally, it was concluded that the ability to use ethylcellous as a Msg polymer matrix to prepare uniform, highly porous particles was confirmed by microscope observation and compatibility with CP.

DEVELOPMENT AND EVALUATION OF FLOATING BEADS OF BACLOFEN AS A GASTRORETENTIVE DOSAGE FORM

Gastro retentive delivery systems are designed to be retained in the stomach for a prolonged time and release their active ingredients and thereby enable sustained and prolonged input of the drug to the upper part of the gastrointestinal (GI) tract. The goal of any drug delivery system is to provide a therapeutic amount of drug to proper site in the body to achieve promptly and then maintain a desired drug concentration. Baclofen is a gamma-aminobutyric acid (GABA) agonist used as a skeletal muscle relaxant used for the relief of painful and uncomfortable muscle spasms caused by a variety of conditions. Twelve different formulation of Baclofen floating beads were successfully developed using emulsion solvent diffusion method. The beads had good yield and showed high, drug entrapment efficiency. The flow properties of beads were within the acceptable range and therefore would be easily filled into capsules. Study concludes successfully delivery of Baclofen by the means of floating beads.

FORMULATION AND EVALUATION OF GASTRO-RETENTIVE MICROSPHERE OF SAXAGLIPTIN ANTIDIABETIC AGENT

The objective of this study was to develop a gastro-retentive microsphere of Saxagliptin. Saxagliptin is an orally active hypoglycemic drug of the newdipeptidylpeptidase-4(DPP4) inhibitor class of drug. Nine formulations of Saxagliptin microsphere are prepared by Emulsion solvent diffusion method using polymers like Eudragit RS 100 and Ethyl cellulose at different drug to polymer ratios and Polyvinyl Alcohol as Stabilizing agent by Emulsion Solvent Diffusion Method. The formulations were optimized on the basis of percent buoyancy and in vitro drug release. The prepared microspheres were evaluated for physicochemical parameters and found to be within range. KEYWORDS: Gastro retentive, Saxagliptin, Ethyl cellulose, Floating microsphere, Eudragit RS 100, Polyvinyl alcohol