Emulsion Solvent Diffusion Method Research Articles

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 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 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

Design of mesalamine loaded micro-particles: Preparation, in vitro and in-vivo characterization

The goal of this study was to develop mesalamine (MS) microparticles that could be ingested by the colon without first passing via the stomach and small intestines. Without resorting to the time-consuming and laborious double emulsion solvent diffusion method, microparticles were successfully fabricated using the Box-Behnken Design method. Microparticle production was optimized, and the effects of many parameters were analyzed (X1: Eudragit S100, X2: Span 80 and X3: agitation speed). Using the Box-Behnken design (BBD), we compared the chosen optimized microparticles to the pure drug solution utilizing in vivo pharmacokinetic study for particle size (Y1), entrapment efficiency (Y2), and drug-release (Y3). It was simple to create spherical, free-flowing, smooth-surfaced microparticles with a zeta potential of −36.52 mV and a size distribution of 264.35 ± 6.28–652.34 ± 6.49 nm. Coefficients of 264.35 ± 6.28–652.34 ± 6.49%, 42.31 ± 2.43–89.74 ± 2.17%, and 52.31 ± 0.43–93.51 ± 0.33% from a quadratic model best fit the observed values of dependent variables. Formulation F4 was selected as the best option because it prevented the drug from being released in the upper GIT before it was ready and instead released it only in the colon, where the pH is optimal. The formulation had a particle size of 266.597 μm, an entrapment efficiency of 93.735%, a cumulative drug release of 95.578 percent, and a desirability factor of 0.998. In comparison to drug solution pharmacokinetics, microparticle pharmacokinetics showed a 6.35-fold decrease in Cmax and MS with an appropriately increased half-life of 8.13 h. (13.67 and 3.46). This enhanced bioavailability of MS released from microparticles is probably due to an increase in the half-life, mean residence time (MRT), and area under the concentration–time curve (AUC0-24) of MS. Over a long length of time with no increase in plasma MS level, it became clear that the novel method of MS-loaded microparticles would provide successful therapy for ulcerative colitis. A pharmacodynamic study found that mesalamine-loaded microparticles dramatically decreased colon edema, necrosis, and bleeding compared to free drug solution. Results from this study suggest that mesalamine-loaded microparticles may be an effective pharmaceutical delivery strategy for the management of ulcerative colitis.

In-situ observation of preparation of PLGA polymeric nanoparticles using liquid cell transmission electron microscopy

Drug delivery systems using polymeric nanoparticles have been widely studied in the field of medicine and pharmacy. However, direct imaging of preparation process of polymeric nanoparticles is challenging due to damage by radiation of incident electron beam and difficulty in reproducing of preparation process. Here, we successfully visualized dynamic preparation behavior of biodegradable poly (dl-lactide-co-glycolide) (PLGA) nanoparticles during an in-situ reaction induced by the addition of PVA solution to PLGA solution. We also observed size of PLGA nanoparticles smaller during the drying process from the liquid state. By reproducing emulsion solvent diffusion (ESD) method, we realized imaging the entire series of preparation process that have not been revealed yet. This information and techniques can contribute to design of future drug formulations. They are also useful in understanding natural property and behavior of damageable materials in the liquid.

NANOSPONGE HEALING APPROACH FOR TREATMENT OF STREPTOCOCCAL GANGRENE

Objective: The envisaged research work aims to develop a nanosponge loaded gel for the treatment of Streptococcal gangrene. Methods: In the present study, permeability is enhanced by targeted drug release formulation of topical clindamycin phosphate nanosponges were prepared by emulsion solvent diffusion method using ethyl cellulose as release retardant polymer and PVA as surfactant or emulsifier. Nanosponges were prepared by emulsion solvent diffusion method by changing drug polymer ratio (1:0.05, 1:0.1, and 1:0.15) and process parameters were optimized using 32 full factorial central design. CP nanosponges were then incorporated into a hydrogel prepared using Carbopol 934. Results and Discussion: The drug loaded nanosponges were evaluated for physical appearance, drug content, entrapment efficiency, and particle size. Characterization of CP nanosponges was done by SEM for the formulation. In vitro release study indicated that the release of CP varied according to the concentration of matrix forming polymer. The best standardized formulation G5 and G6 were further evaluated for microbiological studies. Microbial studies were done using Staphylococcus aureus as the strain organism and the activity of the gel against the organism was evaluated by measuring the zone of inhibition. It was also found to be stable for 2 months during its stability studies. Conclusion: Thus, it was concluded that CP can be formulated as nanosponge hydrogel that can release the drug up to 24 h with increased permeability and targeted release. Therefore, clindamycin phosphate nanosponges prepared are promising drug delivery for topical application as being more useful than conventional formulation therapy.

Comparison between Ethylcellulose and Polymethacrylate Topical Nanosponges Loaded with Butenafi ne Hydrochloride

In this study, nanosponges (NS) loaded with butenafi ne hydrochloride (a broad-spectrum benzylamine antifungal agent) were successfully prepared by emulsion solvent diff usion method using ethylcellulose or polymethacrylate as retarder polymers. PVA was used as a stabilizer. NS 18 formulations were formulated with various ratios of 1:1, 1:2, and 1:3 (%, w/w), using diff erent PVA concentrations of 0.25, 0.5, and 0.75 (%, w/w). The prepared formulations were tested for particle size in terms of diameter, which ranged from (73.6 ± 15.4–991 ± 11.2 nm) for ethylcellulose NS, and from (116 ± 0.96–1439.6 ± 237.4 nm) for polymethacrylate NS. The entrapment effi ciency of the selected formulas (F1, F10) were (74.12 ± 2.60%) and (72.89 ± 1.41%). The selected formulas F1 and F10 were also evaluated for their polydispersity, yield, and in-vitro drug release. The release of BFNS powder in F10 (90.42 ± 1.81%) was higher than that of ECNS F1 powder (78.53 ± 3.24%) within 24 hours. Evaluation tests of the scanning electron microscope (SEM), Fourier transform infrared ray (FTIR), and powder X-ray diff raction (PXRD) confi rmed the NS’ spherical and porous features, the absence of any drug polymer interaction, and the stability of the drug in the delivery system. The two formulas of F1 and F10 were found to exhibit prolonged drug release, which minimizes side eff ects and dosing frequency of BF drug application.

Formulation and Characterisation of Cilnidipine Microsponge Loaded Hydrogels for Antihypertensive Activity

Background: Owing to presystemic metabolism following oral drug delivery, most antihypertensive medications have a low bioavailability. Cilnidipine is a calcium channel blocker used to treat mild to moderate hypertension. Cilnidipine's bioavailability is reduced by 13% due to substantial presystemic metabolism. Objective: The study aimed to fabricate non-irritant and stable microsponge-based hydrogel to enhance the bioavailability of cilnidipine, a weakly water-soluble medication. In addition, the goal was to enhance the permeation rate and retention time at the site of application. Methods: Formulation was developed by using a two-level factorial design with Design Expert software version 13 (14-day free trial). Microsponges were formulated by the emulsion solvent diffusion method, followed by evaluating responses, such as particle size, percentage entrapment efficiency, in vitro drug release, and surface morphology. In addition, X-ray diffraction (XRD) and fourier transform infrared spectroscopy (FT-IR) were performed. Viscosity, swelling behaviour, spreadability, in vitro diffusion, skin irritancy using Wistar albino rats, and in vitro permeation using goat skin were assessed, and stability studies were performed after incorporating the finest formulation into the gel base. Results: Fabricated microsponges were found to be within the required micro dimensions having the necessary porous morphology as demonstrated by scanning electron microscopy studies. Drug entrapment efficiency was found to be in the range of 75-88%. The extended medicament release duration of up to 8 hours was observed. The diffusion data showed controlled release, as demonstrated by Higuchi’s plot. In vitro permeation studies displayed enhanced medicament retention and permeation rate at the site of application. Conclusion: The fabricated microsponge drug delivery system was found to be stable, non-irritant, and having enhanced permeation rate and retention time.

Resveratrol-Loaded Microsponge Gel for Wound Healing: In Vitro and In Vivo Characterization.

The study was aimed to formulate resveratrol (RSV) loaded microsponges to deliver drug at the wound site and incorporate it in the Moringa oleifera Lam. (Moringaceae) gel base to provide an appropriate moist environment for wound management. RSV, a stilbenoid that activates sirtuins and cell-signaling regulators involved in the process of wound healing. Microsponges were prepared by oil in oil emulsion solvent diffusion method by optimizing the independent variables; drug: polymer ratio and volume of internal phase solvent and their effects on entrapment efficiency and particle size. Formulation batches were evaluated for drug content, production yield, entrapment efficiency, and in vitro drug release. The microsponges were further incorporated into M. oleifera gum gel, which was then evaluated for spreadability, viscosity, ex vivo diffusion study and in vivo studies using an excision wound model in rats. Scanning electron microscopy revealed spherical and porous nature of the microsponges in vitro-release study of the optimized batch of RSV microsponges showed 80.88% drug release within 8 h. Differential scanning calorimetry results revealed no drug and polymer interaction during the formation of microsponges. An ex vivo diffusion study through goat skin revealed sustained release of RSV through porous microsponges embedded in the gel base at the wound site. An in vivo study performed using an excision wound model showed wound healing and closure within day 8. Histopathology showed increased re-epithelization and reduced ulceration in RSV microsponge gel-treated group compared with sham operated. RSV microsponge gel delivered the drug at the wound site and the gel base provided a moist environment and influenced cell adhesion, thereby promoting faster wound healing.

SPHERICAL CRYSTALLIZATION: A TOOL TO IMPROVE SOLUBILITY OF DRUGS

Spherical crystallization is a technique in which crystallization and agglomeration are carried out synchronously in one step to form compact spherical form. The most common methods used in spherical agglomeration are quasi emulsion solvent diffusion method, ammonia diffusion system, neutralization technique and co-agglomeration. It succeeded to improve dissolution property of poorly soluble drugs. This can change drug powder properties such as flowability, wettability, packability, compressibility. It has wider applications in improvement of poorly compressible drugs; it has wider application in improvement of compressability of poorly compressible drugs, masking bitter taste of drugs, improving dissolution property, bioavailability and solubility of drugs. Agglomeration crystals converted into tablet forms thus helping us by saving time and reducing cost.

Doxorubicin Hydrochloride-loaded Nanoparticles for Oral Delivery: Optimization using Design of Experiments

Doxorubicin hydrochloride (DOX) has low oral bioavailability due to the presence of active efflux from intestinal P-glycoprotein receptors. Because of the difficulties associated with the oral administration of DOX, there is not yet a commercially available oral formulation of DOX. Nanocarrier system was manufactured utilizing poly (lactic-co-glycolic acid) (PLGA) and treated with chitosan to provide a surface coated. Nanoparticles (NPs) were created using a modified emulsification solvent diffusion (nanoprecipitation) method by electrostatic conjugation of chitosan to modify nanoparticle surfaces. The model was built using a Box-Behnken design with three independent components: X1 (PLGA), X2 (poloxamer 188), and X3 (chitosan concentration). The optimized chitosan-PLGA NPs had a mean particle size of 153.6 nm and a positive zeta potential of 21.51 mV. More than 85% DOX permeated through the everted gut by DOX-loaded chitosan-NPs as compared to NPs prepared with PLGA alone. Chitosan nanoparticles caused a 6-fold increase in DOX intestinal permeability. The findings pointed to the possibility of using chitosan-based nanoparticles of doxorubicin for oral treatment for cancer.