Quasi-emulsion Solvent Diffusion Method Research Articles

Statistical Design for Formulation Optimization of Diclofenac Sodium-Loaded Ethylcellulose Microsponges

For a better use of the drug, a decrease in side effects, an improvement in effectiveness, and a uniform release of the active ingredients, sustained-release forms have been developed. The objective of this study is to estimate the effect of the factors on the responses involved in the formulation of Diclofenac Sodium (DC) loaded ethylcellulose (EC) microsponges (MP) using Central Composite Design (CCD). Quasi emulsion solvent diffusion method was used to formulate MP. The ratio of ethylcellulose to Diclofenac Sodium and polyvinyl alcohol (PVA) concentration (w/v%) were selected as independent variables for CCD. Entrapment efficiency (EE) and production yield (PY) were selected as dependent variables. The optimal formulation was characterized by Fourier Transform Infrared (FTIR), Optical Microscopy, and in vitro release. Optimized MP showed an EE of 31.02% and a PY of 66.44%, FTIR studies revealed no chemical interaction between drug and polymer used, MP were spherical and present an average size of 9.21±0.3µm. Kinetic studies revealed that drug release from optimized formulation followed Higuchi model. The results demonstrated the effectiveness of proposed design for development of DC microsponges for the sustained release.

Formulation, Characterization, and Antibacterial Study of Microsponge- Loaded Gel of Clarithromycin for Topical Drug Delivery

Background: Microsponge drug delivery systems comprise spherical and porous micro-spheres for prolonged topical drug delivery. These systems considerably reduce the undesirable side effects, offering improved patient compliance and reduced dosing frequency. Objective: The present study focused on developing topical controlled release preparations of microsponges-loaded gel of clarithromycin to cure bacterial skin infections. Materials and Methods: Four batches of microsponges (F1, F2, F3, and F4) of clarithromycin (CLR) containing fixed amounts of clarithromycin (100 mg), dichloromethane (5 ml), polyvinyl al-cohol (5 % w/v) and distilled water (25 ml) with varying polymer concentrations were prepared by the quasi-emulsion solvent diffusion method and evaluated for % Production Yield, % drug content, % encapsulation efficiency, particle size, polydispersity index (PDI) and % drug release characteris-tics. The selected microsponge formulation (F3) was incorporated in Carpopol 934 gel for topical application. The prepared gel (CLRMS-F3 Gel) was evaluated for physical characteristics, pH, spreadability, viscosity, and in vitro drug release. Furthermore, the gel formulation was compared with pure clarithromycin gel for antibacterial activity against the gram-positive (S. aureus) and gram-negative strain (E. coli.) using the cup and plate method. Results and Discussion: The F3 microsponge formulation exhibited a production yield of 83.75%, drug content (21.5 ± 0.50 %), and encapsulation efficiency of 86.04 ± 2.30%. Their particle size was satisfactory (3.80 ± 0.01 μm), and they were found to be spherical and porous in nature. F3 microsponges released 69.36 ± 1.27% of the drug over a period of 8 hrs and were incorporated into the gel formulations. The gel prepared using F3 microsponges was transparent, homogenous, and exhibited a pH of 6.8 ± 0.02, spreadability of 9.92 ± 0.44 g/cm, and viscosity of 35370.17 ± 493.09 centipoises. The CLRMS-F3 gel released 82.13 ± 0.47% drug in 12 hrs using a zero-order kinetic. The antibacterial activity studies revealed a higher potency against both S. aureus and E. coli of the prepared CLRMS-F3 gel compared to pure CLR gel and azithromycin standard. Conclusion: Based on the above study, it may be concluded that microsponges’ gel formulation can be potentially useful in improving topical drug delivery of antibacterial agents and can give better therapeutic efficacy.

Colon-specific tablets containing naproxen microsponges for effective treatment of inflammatory bowel disease

Naproxen 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 naproxen tablet for colon specific drug delivery for enhanced therapeutic effect. Microsponges were developed by quasi emulsion solvent diffusion method. Compatibility of the drug with excipients was studied by FT-IR & DSC .Prepared microsponges were optimized in order to analyze the effects of independent variables (ratio of drug: eudragit (X1), concentration of PVA ( X2) & stirring speed (X3)) on the particle size (Y1), entrapment efficiency (Y2) and production yield (Y3) using box behnken design. Particle size (Y1), entrapment efficiency (Y2) and production yield (Y3) were the responses selected for simultaneous optimization, with the aid of Derringer’s desirability function. The optimized formulation was subjected to in vitro study. The F1 was selected as optimized formulation based on particle size of 600.75µm , entrapment efficiency of 99.32%, and production yield 94.45% . The results showed that, generally an increase in the ratio of the drug: polymer control release rate of naproxen from micro sponges.

QBD approach for the development of hesperetin loaded colloidal nanosponges for sustained delivery: In-vitro, ex-vivo, and in-vivo assessment

Hesperetin (HT) is a polyphenolic compound with anti-carcinogenic, tumor necrosis, and anti-oxidant properties. The present study reports the fabrication, optimization, and evaluation of HT-loaded nanosponges (HTN)- based gel (HTNG) for sustained anti-inflammatory effect. HTN formulation was prepared by quasi emulsion solvent diffusion method using a 42 factorial design. HTN was subjected to different solid and liquid state characterizations and subsequently loaded in carbopol gel. The effects of pro-inflammatory cytokines (IL- 1β and IL-6) were evaluated using RAW 264.7 macrophage cells, and the anti-inflammatory potential was tested in rats. Tiny, porous, and spherical HTN retarded the drug release (39.98%) up to 8 h compared to the pure drug (70.74%) and physical mixture (73.72%) and followed the Higuchi-matrix model. HTNG had a strong downregulating effect on cytokines. It showed no skin irritation and 18.52% skin permeation at 8 h. Further, HTNG-treated rats exhibited 33.16% inflammation inhibition compared to the control group. In conclusion, nanosponges significantly retarded the topical delivery and could circumvent the bioavailability issues associated with HT.

Microsponges: A Futuristic Approach for Oral Drug Delivery and Current Status

Microsponges are at the forefront of the field of new drug delivery technology, which is rapidlyevolving. Microsponge drug delivery technology holds a lot of potential in terms of reaching the aimof controlled and site-specific drug delivery, thus it’s gotten a great deal of interest from scientists.Microsponges are porous microsphere and biologically inert. Particle size of microsponges was 10-25μm. The Quasi emulsion solvent diffusion method was used to construct microsponges. It is aunique technique for controlled release formulation.This page gives an overview of the Microspongesdelivery system, including the principles and methods of preparation. Particle size and distribution,surface morphology, porosity, and density are all considered as appropriate analytical methods forcharacterization of Microsponges. The advantages, drawbacks, and possible responses of microspongedrug delivery are also examined. The advantages, drawbacks, and alternative solutions of microspongedrug delivery are also explored. These microsponges are included in sunscreens, balms, ointments, andover-the-counter skin care products that are designed for external use. Microsponge drug delivery canprovide increased efficacy for topically active agents with enhanced safety, extended product stabilityand improved aesthetic properties in an efficient and novel manner. They are mostly used for topicaluse and have recently been used for oral administration.

Quasi Emulsion Solvent Diffusion Modification of Underutilized Chenopodium album Starch and its Characterization

The present study was designed to investigate the changes occur on Chenopodium album starch (CAS) after modification through quasi emulsion solvent diffusion (QESD) method. Modification of starch was carried out by HCl (0.1, 0.25, 0.50, 0.75 and 1M) followed by precipitation. The QESD modification significantly reduced the amylose content, water absorption capacity, oil absorption capacity, solubility as well as swelling power of treated starch. Gelatinization behaviour of modified starch showed an increase in pasting temperature. The SEM images showed the formation of regular and spherical shaped larger starch particles. There was an improvement in crystallinity from 20.01 to 29.86% after modification as shown in X-ray analysis. Overall, it indicates that QESD treatment results into formation of spherical crystalline agglomerates.

Application of Box–Behnken Design and Desirability function in the Optimization of Aceclofenac-Loaded Micropsonges for Topical Application

Background: The aim of the present investigation was to develop optimized Aceclofenac-loaded microsponges using Box-Behnken design (BBD) and desirability function. Material and Method: Aceclofenac-loaded microsponges were developed using ethyl cellulose, ethanol and polyvinyl alcohol (PVA). Initially, a trial batch was developed using quasi-emulsion solvent diffusion method, and by optimizing the drug-polymer ratio. A 3-level, 3-factor BBD was used to investigate the effect of PVA, ethanol and stirring speed on particle size and entrapment efficiency (EE). The models used for the optimization were analyzed through ANOVA and diagnostic plots. Finally, the desirability function was used for the selection of optimized formulation composition. Results: A drug-polymer ratio of 1.5:1 was taken as optimized ratio for all the formulations. The developed microsponges were of the spherical shape having size and %EE in the range of 22.54±2.85 µm to 49.08±5.01 µm and 70.57±4.19% to 86.43±2.58 %, respectively. The amounts of PVA, ethanol and stirring speed were noted to have a significant impact on particle size and %EE. Finally, an optimized formulation (size-22.69 and %EE-86.42) was developed with a desirability value of 0.9967. Conclusion: The BBD is a valuable tool for the development of optimized microsponges with desired properties.

Enhancement of Aqueous Solubility, Dissolution Profile, and Oral Bioavailability of Pentoxifylline by Microsponges

Microsponge, a novel drug delivery system, is designed to deliver a pharmaceutically active ingredient efficiently at the minimum dose. Microsponge plays an important role in enhancing drug stability, reducing side effects, and modifying drug release profiles. It is mostly used for transdermal delivery. Recent studies also explored their use for oral administration. This study aimed to explore the potential use of the microsponge technique in improving the aqueous solubility and dissolution profile of pentoxifylline (PTX). In this study, microsponges were prepared by a quasi-emulsion solvent diffusion method by varying concentrations of carriers. Nine different ratios of the PTX:Eudragit E-100 with varying amounts of dichloromethane were used. All formulated microsponges were evaluated for %production yield, compatibility of drug excipient, encapsulation efficiency, in vitro drug release, and in vivo bioavailability, as well as recorded by scanning electron microscopy (SEM) and differential scanning calorimetry(DSC). Our data suggested that the aqueous solubility of PTX microsponges was four times greater than that of pure drug. The in vitro drug release of selected microsponges (M8) was found to be 70%; furthermore, the in vivo study suggested that the selected formulation significantly enhanced drug concentration in the plasma (9,219 ng/mL in 12 hours) in comparison to pure drug PTX (2,476 ng/mL in 12 hours). SEM showed that the prepared microsponges were spherical with porous nature. Fourier-transform infrared spectroscopy and DSC studies confirmed an absence of incompatibility among drugs and selected excipients. The pH of the selected gel was found to be 6.8, which was compatible with those of skin and oral formulations also. All above data suggested a highly successful and beneficial use of the microsponge technique in enhancing aqueous solubility, dissolution profile, and oral bioavailability of PTX. Microsponge-based delivery of PTX may represent an alternative strategy to improve the bioavailability of the drug.

Formulation and Evaluation of Luliconazole Microsponges Loaded Gel for Topical Delivery

Microsponge containing Luliconazole (LCZ) with different proportion of drug:polymer (Ethyl cellulose and Eudragit RS 100) were obtained efficiently using Quasi-emulsion solvent diffusion method. Luliconazole is an anti-fungal drug used for the topical delivery. The purpose of the microsponge formulation is to control the release of LCZ drug to the skin through Microsponge Delivery System (MDS) known to be the novel technique which overcome the maximum concentration of active ingredient, frequency doses, and skin irritation. The prepared microsponges were examined using drug content, % production yield, % entrapment efficiency and in-vitro drug release. The formulation were subjected to in-vitro drug release studies for 6 hr in which it was concluded that Ethyl cellulose microsponges formulated by drug:polymer (1:1) and Eudragit RS 100 microsponges formulated by drug:polymer (1:3) showed maximum controlled release i.e., Increase in drug:polymer ratio (1:1 to 1:9) increased the production yield and entrapment efficiency of microsponges using Ethyl cellulose with no significant effect for Eudragit RS 100.Therefore, both formulation F1 and F2 was dispersed in carbopol gel preparation for controlled delivery of LCZ to the skin. Various physical parameters like pH, spreadability, viscosity and in-vitro drug diffusion studies were evaluated for the prepared gel formulations. Microsponge gel formulation i.e., FG1 showed better results for controlled release of 89.40% as compared to FG2 i.e., 92.18% over the period of 12 hrs which is performed in Franz Diffusion Cell. On basis of in-vitro diffusion studies for LCZ gel formulation, microsponges using Ethyl cellulose (FG1) was found to be best for its controlled release of LCZ for 12 hrs and followed zero order kinetics. Hence, formulated LCZ loaded gel have potential to treat fungal infections i.e., tinea pedis, tinea cruris and tinea corporis.

Development and Characterization of Metronidazole Loaded Microsponges for the Management of Diabetic Foot

The objective of present work was formulation and evaluation of Metronidazole loaded microsponges for the management of diabetic foot ulcer via topical application and to reduce side effects. The microsponges were prepared by quasi-emulsion solvent diffusion method using different concentrations of Ethyl cellulose and Poly vinyl alcohol. The prepared microsponges were evaluated for particle size analysis, SEM, % production yield, % drug entrapment efficiency, in-vitro drug release studies, DSC and antimicrobial studies. FTIR studies shown that there was no interaction between drug and polymers. The optimum sustained release of drug around a period of 12hrs was shown by formulation F8. The n value of optimized formulation indicated that the drug release followed zero order kinetics. It was confirmed from the stability studies that the optimized formulation remained stable at 45±2℃ and 70±5% relative humidity. Keywords: Microsponges, Metronidazole, Diabetic Foot, Quasi-emulsion solvent diffusion, Sustained release, Scanning electron microscopy, Differential scanning calorimetry.

Formulation and Development of Aceclofenac loaded Microsponges Topical Drug Delivery System using quality by Design Approach

The proposed study is focussed at developing Aceclofenacmicrosponges for topic drug delivery systems. QbD was applied for better understanding of the process and to generate design space, using quality target product profile, critical quality attributes, and risk assessment. The aim of the experiment was to prepare a safe, efficacious, stable and patient compliant microsponge dosage form of Aceclofenac. Materials and methods: Pre-formulation studies were carried out which helped in developing an accurate dosage form. UV, FTIR, DSC, and SEM studies were done for pre-formulation and post-formulation evaluations. These study deals with the design and optimization of Aceclofenacmicrosponges loaded topical drug delivery system to the controlled release of active drug into the skin in order to minimize the systemic exposure and minimize local cutaneous reactions to active drugs by DoE method of QbD Approach. AceclofenacMicrosponges were prepared by quasi emulsion solvent diffusion method using Eudragit-RS100 as a polymer, polyvinyl alcohol, Ethanol as Internal phase volume and Liquid paraffin as External phase volume. In this study, we found that the controlled release of aceclofenac microsponges.

Microsponges Loaded Topical Drug Delivery System for the Effective Management of Rheumatoid Arthritis

Rheumatoid arthritis (RA) is an autoimmune disease associated with severe joint pain. Herein, we report aceclofenac (ACF)-loaded cellulosic microsponge gel formulation with sustained anti-inflammatory effects that are required to manage arthritic pain. The microsponges were formulated using quasi-emulsion solvent diffusion method. The optimized formulation was dispersed into Carbopol gel. Further, the optimized formulation was evaluated for pH, viscosity and spreadability, drug content, and kinetic drug release profile. The optimized microsponges loaded topical gel showed R2 value of 0.9930 which was nearest to one which revealed that formulation obeyed Higuchi kinetic model and n value was found to be 0.48 which depicts Fickian transport of drug diffusion. The prepared optimized formulation showed no signs of irritation when applied on hairless skin of rats along with inhibitory effect on inflammation was observed in in vivo studies in animals, hence, ACF-loaded topical drug delivery is considered as a potential platform for the management of RA.

Porous Polymeric Carrier System for Modified Drug Releaseof Boswellic Acid

Microsponges being the polymeric drug delivery systems consist of porous microspheres that can entrap a wide range of active ingredients. Boswellic acid is a pentacyclic triterpenoid having anti-inflammatory, anti-hypertensive, anti-cancer activities. The aim of the study was to develop, characterize and formulate microsponge delivery for topical application. The Microsponges were prepared by quasi emulsion solvent diffusion method using QbD approach. Drug excipient compatibility study was carried out by FT-IR, DSC and XRD. The prepared Microsponges were further evaluated for its physicochemical properties by scanning electron microscopy (SEM), photomicroscopy, transmission electron microscopy (TEM), particle size, zeta potential, and porosity analysis. The optimized Microsponges were incorporated into gel base formulation and evaluated for in-vitro drug release, dissolution studies and ex-vivo permeability studies. Further, microsponge formulations, subjected for animal studies for skin irritation test and clinical efficacy. The present study confirmed the formation of Microsponges of Boswellic acid. It also proves the sustained release of drug through microsponge formation.

A novel plaster containing benzoyl peroxide microsponges: Formulation, development and evaluation

Benzoyl peroxide is a widely used active agent for acne vulgaris treatment that has antibacterial, anti-inflammatory, keratolytic and wound-healing properties. The common complaints for benzoyl peroxide are skin irritation and dryness. To reduce these side effects, microsponge formulations are used as an effective tool in pharmaceutical and cosmetic industries. In this study, a medical plaster was developed containing benzoyl peroxide microsponges which gives an opportunity to explore the potential of the microsponge systems in textile industry. Benzoyl peroxide microsponge was obtained by using quasi-emulsion solvent diffusion method and characterized by SEM, FT-IR, particle size analysis and porosity studies. The microsponges were applied onto 100% cotton woven fabric by using dip-coating technique. In the treatment solution, different binding agents as acrylic binder, and cross-linking agents as poly(ethylene glycol) diglycidyl ether and 1,2,3,4-butanetetracarboxylic acid were used. Microsponges were around 78.4 µm in diameter and had a spherical porous surface. SEM analyses of the treated fabrics proved that the microsponges were succesfully transferred on cotton fabrics. The drug contents of the fabrics containing Benzoyl peroxide loaded microsponge were found to be within the range of 68.512–102.873%. The in vitro drug release results show that the release from both samples was more than 40% within 6 h. The water vapor permeability of plaster prepared with acrylic binder (S1) was significantly higher than the other plasters. This study presents a novel approach for acne treatment based on textiles containing microsponges. The results revealed that microsponges had a promising potential in textile field.

Formulation and Evaluation of Microsponges Gel of Havan Ash for the Treatment of Acne

The aim of this study was to develop the Microsponges containing Havan ash composed gel formulation for the treatment of Acne. Therefore, the topical formulation containing microsponges of Havan Ash will be formulated and evaluated. The preliminary investigation was carried out for the formulation of Havan ash loaded Microsponges by using quasi emulsion solvent diffusion method (MSF1-MSF6). In the preformulation studies of Havan ash the physical description and organoleptic properties, pH, acid insoluble ash, water-soluble ash, IR spectroscopy, identification test, rheological study, atomic absorption spectroscopy is also carried out. On the basis of particle size analysis of Microsponges, percentage yield formulation MSF5 containing Microsponges formula was selected for composition of topical gel formulation. Thus the different gel base formulation (G1-G3) using Carbopol-934 (1,1.5,2.0%) was prepared by emulsification method. By considering all the relevant, physicochemical parameters, G2 gel base was selected for further loading of Havan ash containing Microsponges. The MSF5 formulation was loaded into the selected gel base G2 (1.5%). Then the formulation and evaluation of Havan ash microsponges loaded gel was done. The formulation F3 has better results than other 4 formulations. F3 have its appearance silver colour, consistency very good, Grittiness –ve, homogeneity good, wash ability very good, pH 6.3, Spreadabilty (g.cm/sec) 14.4 ± 0.77 7and viscosity (cps) 18251 ± 50.12, have good result of psychometric analysis. With the revealed results by different evaluation parameters, it is concluded that microsponges drug delivery system has become highly competitive and rapidly evolving technology and more research are carrying out to optimize cost-effectiveness and efficacy of the therapy.
 Keywords: Havan ash, Antimicrobial, Microsponges, Acne vulgaris, Topical gel.

Resveratrol-Loaded Microsponge as a Novel Biodegradable Carrier for Dry Powder Inhaler: A New Strategy in Lung Delivery

The aim of the present study was to prepare a resveratrol-loaded microsponge-based dry powder inhaler (RES-MS-DPI) using the quasi-emulsion solvent diffusion method and to explore its suitability for pulmonary delivery. The prepared microsponges were evaluated for physicochemical properties. Additionally, an in vitro lung deposition study was performed using an Andersen cascade impactor (ACI), while in vivo performance was studied by intratracheal administration. The optimized porous and spherical RES-MS showed particle size, surface charge, entrapment efficiency, mass median aerodynamic diameter (MMAD) and fine particle fraction (FPF) of 2.499 ± 0.56 μm, −25.34 mV, 89.45 ± 0.23%, 2.13 ± 0.21 μm and 48.54 ± 0.25%, respectively, with controlled release. Further, in vitro and in vivo studies of RES-MS showed a twofold improvement in the FPF, and 4.4-, 14.12- and 1.94-fold improvement in the area under the curve (AUC), mean residence time (MRT) and Cmax. The RES-MS exhibited higher aerosolization and lung deposition.

Ecofriendly Ethyl Cellulose Microsponges of Citronella Oil: Preparation, Characterization and Evaluation of Cytotoxicity and Larvicidal assay.

Citronella Oil (CO) was used by the Indian army as mosquito repellant to repel mosquitoes at the beginning of the 20th century and later in 1948, it was registered in the USA for commercial purposes. Due to its ecofriendly nature, CO possesses immense potential as a mosquito repellent. Citronella oil is a valuable alternative to synthetic mosquito repellents commonly used nowadays. However, its volatile nature, poor stability in air and high temperature restrict its application. Its direct application on skin may lead to skin irritation. To surmount the above-mentioned issues, the present research aims to develop Microsponge (MS), a novel dosage form for enhancing the utility and safety of CO. Quasi emulsion solvent diffusion method was chosen for crafting MS using ethyl cellulose with various drug-polymer ratios and characterized. In vitro cytotoxicity evaluation was also carried out to check the dermal safety of COMS. The present results revealed that the size of all prepared formulation lies in the micro range (20 ± 3 to 41 ± 4 μm), with good payload (42.09± 3.24 to 67.08± 6.43%). The results of FE-SEM depicted that MS were spherical in shape with porous nature. Cytotoxicity results indicated that COMS were safe on skin cells, when compared to pure CO. The optimized MS were also assessed for larvicidal assay against larvae of Anopheles culicifacies. The CO micro-formulations were found to possess enhanced stability of this oil. Entrapment of CO in MS resulted in a better vehicle system in terms of safety, stability and handling benefits of this oil.

Formulation and Evaluation of Celecoxib loaded colon Targeted Microsponges

The present research work support preformulation, formulation, development and optimization of colon targeted microsponges containing Celecoxib as a nonsteroidal anti-inflammatory drug. The different batches of formulation were evaluated using celecoxib as active pharmaceutical ingredient, Eudragit as the pH sensitive polymer, polyvinyl alcohol and triethyl Citrate. Colon targeted microsponges of Celecoxib were prepared by Quasi-emulsion solvent diffusion method. The prepared formulations were evaluated for various parameters like Particle size, Percentage entrapment efficiency, Measurement of Zeta Potential, FTIR, in-vitro release study. The result were found to be within standard limits. FTIR study reports indicated that there was no interaction between Celecoxib and other excipients. Zeta Sizer shown that the microsponge size ranges from 61.12 μm to 67.59μm. Percent drug content was between 65.18%– 95.19%. Based on the resultants of the entrapment and particle size of microsponges, formulation M4 was observed to be optimized formulation. The optimized formulation exhibited 71.52% cumulative drug release after 10 h. The optimized batch shows 77.40% yield.

Improved processability of ethambutol hydrochloride by spherical agglomeration

Ethambutol hydrochloride (ETB), high dose anti-tubercular drug exhibits poor micromeritics and compressibility. The current study aimed to enhance flow, compressibility and packing characteristics, thereby improving processability of ETB by spherical agglomeration. Quasi emulsion solvent diffusion method was used for agglomeration process in which saturated aqueous ETB solution was prepared and the crystallization was carried out subsequently at different ratios of acetone and ethyl acetate which act as anti-solvent. Further the process was optimised statistically using 32 factorial design keeping ‘speed of stirring’ and ‘ratio acetone and ethyl acetate’ as independent variables and particle size as dependent variable. Optimised batch of ethambutol hydrochloride spherical agglomerates (ETB-SA) was characterised for sieve analysis, solid state characteristics and Kawakita analysis. The uniformity of ETB-SA was observed with SEM while XRPD studies revealed reduction in crystallinity for ETB-SA. DSC and FTIR indicated no polymeric or chemical alteration during crystallization process. The flow properties of ETB-SA were found superior and its Kawakita parameters indicated improved packability and flowability compared to ETB. ETB has high solubility in water therefore was no significant difference was observed in in vitro dissolution of ETB and ETB-SA. Thus spherical agglomeration, a revered particle engineering technique, continues to be a salient approach for enhancing processability of high-dose drugs like ETB.

Eudragit RS100 based microsponges for dermal delivery of clobetasol propionate in psoriasis management

Clobetasol propionate (CP), a super potent dihalogenated topical corticosteroid for psoriasis, displays common side effects like allergic contact dermatitis, steroid acne, skin atrophy, hypo-pigmentation and systemic absorption, on topical application. Hence, entrapment of CP in an appropriate carrier system could minimise the aforementioned side effects, while controlling its percutaneous absorption. Therefore, motive behind current work was to fabricate and evaluate CP loaded microsponges (MS). The microsponges were successfully crafted by employing quasi-emulsion solvent diffusion method. For preparation of MS, organic phase comprising CP, Eudragit RS 100 and dichloromethane was added to aqueous phase (polyvinyl alcohol solution), while stirring. During optimization of MS formulations, factors (drug: polymer ratio, aqueous and organic phase volume) affecting the physical properties of microsponges were also investigated. The prepared microsponges were found to possess particle size in the range 12.2 ± 8.2–45.80 ± 12.3 μm, entrapment efficiency: 60.00 ± 0.06 to 96.37 ± 0.04 % and drug release: 60.60 ± 0.13 to 92.82 ± 0.15 %. Additionaly, CP loaded microsponges were evaluated for topography, thermal and photostability. Finally, optimized CPMS were incorporated into Carbopol gel base, which was subsequently evaluated. In vitro release of CPMS was compared with plain CP and release results were fitted into different kinetic models. CPMS formulation followed zero order kinetics indicating release of drug at constant rate, with absence of initial burst release. This delivery system resulted in extended CP release and its maximum therapeutic activity, with minimum toxic effects. In vivo antipsoriatic activity of CPMS gel performed using mouse tail model exhibited significant therapeutic efficacy in comparison to plain CP gel, which was further supported by the histopathological findings.