Quasi-emulsion Solvent Diffusion Technique Research Articles

Evaluating the potential of ethyl cellulose/eudragit-based griseofulvin loaded nanosponge matrix for topical antifungal drug delivery in a sustained release pattern

Fungal infections are very alarming nowadays and are common throughout the world. Severe fungal infections may lead to a significant risk of mortality and morbidity worldwide. Sustained delivery of antifungal agents is needed to mitigate this problem. In the current study, an attempt has been made to formulate griseofulvin-loaded nanosponges using the quasi-emulsion solvent diffusion technique. For characterization, griseofulvin loaded nanosponges were tested by different instrumental techniques such as optical microscopy, scanning electron microscopy (SEM), powder X-ray diffractometer (PXRD), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and transmission electron microscopy (TEM). The antifungal activity of the nanosponges was assessed against Candida albican strain using the agar well-diffusion method. Finally, the drug-loaded nanosponges' in vitro sustained release activity was evaluated. FTIR spectra showed no chemical interference between the drug and polymers. Some of the peaks of the drug are not visible in the FTIR spectrum, which suggests drug entrapment. PXRD data showed that the drug lost its high crystallinity when entrapped in the nanosponge matrix. From the morphological studies via SEM and TEM, a brief idea of the surface morphology of the nanosponges was obtained. The small pores throughout the structure proved its high porosity. The antifungal sensitivity assay was successful, and a zone of inhibition was observed in all the formulations. The in-vitro drug release study showed sustained behaviour. The sustaining effect was due to the polymer and cross-linker used, which gave rise to a porous scaffold matrix. From the results, it can be concluded that griseofulvin-loaded nanosponges can be used for antifungal drug delivery against various topical skin infections.

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

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

Formulation and Evaluation of Topical Microsponge Based Gel of Clotrimazole

The study's overarching goal is to develop a novel medication delivery method based on microsponge gel containing clotrimazole. Clotrimazole is poorly absorbed from the gastrointestinal tract (GIT), has a short half-life of only 2 h, & is metabolized into inert molecules by the liver. Therefore, clotrimazole's drug delivery method must be modified for topical application. Microsponge delivery is a novel approach to sustained drug release. Microsponges were made with a polymer solution of Eudragit RS 100 in dichloromethane (DCM) and ethanol (1:1) using a quasi-emulsion solvent diffusion technique. A number of metrics, including production yield, entrapment efficiency, particle size measurement, and in vitro drug release studies, were used to each microsponge formulation. For topical administration, the optimized microsponge formulation F6 was transformed into a gel formulation. Prepared gel was compared to a commercially available formulation based on physical factors such as pH, viscosity, spreadability, drug content, and an in vitro diffusion investigation. Most of the formulations were discrete and spherical in shape, indicating a satisfactory production yield, suggesting quasi-emulsion solvent diffusion method is a promising methodology for the fabrication of microsponge. Clotrimazole was released steadily over the course of 12 hours from the microsponge gel formulation MGI (F6). Therefore, the medicine in the form of a microsponge can reduce the risk of adverse effects and increase patient compliance by avoiding skin contact.

Formulation And Evaluation of Quercetin Loaded Nanosponges of Abiraterone Acetate

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

Development of Clindamycin Loaded Oral Microsponges (Clindasponges) for Antimicrobial Enhancement: In Vitro Characterization and Simulated in Vivo Studies.

Clindamycin phosphate (CLP) is a broad-spectrum antibiotic that is used widely for different types of infections. It has a short half-life and hence it should be taken every six hours to ensure adequate antibiotic blood concentration. On the other hand, microsponges are extremely porous polymeric microspheres, offering the prolonged controlled release of the drug. The present study aims to develop and evaluate innovative CLP-loaded microsponges (named Clindasponges) to prolong and control the drug release and enhance its antimicrobial activity, consequently improving patient compliance. The clindasponges were fabricated successfully by quasi-emulsion solvent diffusion technique using Eudragit S100 (ES100) and ethyl cellulose (EC) as carriers at various drug-polymer ratios. Several variables were optimized for the preparation technique including the type of solvent, stirring time, and stirring speed. The clindasponges were then characterized in terms of particle size, production yield, encapsulation efficiency, scanning electron microscopy, Fourier Transform Infrared Spectroscopy analysis, in vitro drug release with kinetic modeling, and antimicrobial activity study. Moreover, in vivo, pharmacokinetics parameters of CLP from the candidate formula were simulated based on the convolution method and in vitro-in vivo correlation (IVIVC-Level A) was built up successfully. Uniform spherical microsponges with 82.3 µm mean particle size with a porous spongy structure were evident. ES2 batch exhibited the highest production yield and encapsulation efficiency (53.75 and 74.57%, respectively) and it was able to exhaust 94% of the drug at the end of 8 h of the dissolution test. The release profile data of ES2 was best fitted to Hopfenberg kinetic model. ES2 was significantly (p < 0.05) effective against Staphylococcus aureus and Escherichia coli compared to the control. Also, ES2 displayed a twofold increase in the simulated area under the curve (AUC) compared to the reference marketed product.

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

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

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

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

DEVELOPMENT AND EVALUATION OF MICROSPONGE GEL OF AN ANTIFUNGAL DRUG

Objective: The objective of the present study was to compare the release effect of Luliconazole from different polymeric (Hydrophilic and Hydrophobic) microsponges prepared using varying concentrations. The best microsponge was selected and incorporated into different gel (Natural and synthetic) and drug release is determined and compared with marketed formulation.&#x0D; Methods: Polymers such as EC, HPMC, Eudragit RSPO and PVA as emulsifier, and solvent DCM is used as solvent. Microsponge were prepared by using the quasi emulsion solvent diffusion technique. FTIR was studied to estimate the incompatibility. Microsponges were evaluated for SEM, particle size, drug content, and In vitro diffusion studies. Optimized microsponge incorporated gel was prepared by using different gel (flax seed gel and Aerosil gel) were evaluated for pH, spreadability, extrudability, drug content and in vitro diffusion studies.&#x0D; Results: Theresults obtainedshowed no physical-chemical incompatibility between the drug and the polymers. EC, HPMC and EC combination was found to be a suitable polymer compared to Eudragit RSPO and other combination in preparation of microsponge. From the evaluation of microsponge, the optimized F1 formulations was incorporated into different gel (flax seeds, aerosil) and compared with marketed formulation in which MG-I (flax seed gel) was considered as good topical anti-fungal microsponge gel based on there physical parameters and drug release kinetics.&#x0D; Conclusion: Microsponge and microsponge gel were successfully prepared for Luliconazole and their evaluation studies of each dosage form revealed that topically applied microsponge gel possess immense potential to control the release rate of medicament to improve the bioavailability as well as patient compliance.

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

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

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

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

Formulation Development and Evaluation of Colon Targeting Nanosponges of Deflazacort Using Box Behnken Design

Deflazacort is a glucocorticoid that is often used as an anti-inflammatory and immunosuppressant for patients suffering from Inflammatory Bowel Disease such as ulcerative colitis (UC) and Crohn's disease (CD). IBD is difficult to manage, and the most difficult issue for doctors is the recurrence. There are several regulated and colon focused medication delivery devices available for therapy, however they have a low success rate. The goal of this work was to create nanosponges loaded with deflazacort using the quasi-emulsion solvent diffusion technique using Eudragit S-100 and to investigate the influence of process factors on response using the Box-Behnken design. The effect of three independent parameters, Eudragit S100, PMMA, and PVA, on two dependent responses, particle size and percent drug entrapment, was investigated. Using the Box-behnken design, seventeen nanosponge formulations were created using the quasi-emulsion solvent diffusion technique and Eudragit S-100 (0.2 percent to 0.5 percent w/v), PMMA (0.2 percent to 0.5 percent w/v), and PVA (0.5 percent -1.5 percent w/v). Particle size, percent drug entrapment, shape and surface morphology, drug content determination, and in vitro drug release behaviour were all evaluated in the nanosponge formulations. The generated nanosponge was virtually spherical in form and spongy in character, with particle size 170.45 nm and a drug entrapment percentage of 73.42 percent. Over a 24-hour period, in vitro drug release of optimised formulations was shown to have a maximum drug release of 90.33.3 percent in colonic fluid with 4 percent w/v caecal content. The observed values of several assessment parameters were found to be in close agreement with the projected values using the Design expert programme. The nanosponge formulation obtained using Eudragit S-100 in low concentration, optimum concentration ratio of eudragit: PVA along with low stirring speed showed desired features. The mathematical models were further designed to develop nanosponge with required characteristics.

Preclinical evaluation from in-silico to in-vivo study of polyherbal microsponge sunscreen gel.

Electromagnetic spectrum of the UV region predominantly becomes the reason for skin's detrimental effects that give the genesis of innumerable skin ailments; because of this reason, the sunscreen products are required before condition in day to day lifestyle; products such as moisturizers, lotions, creams, shampoos, and other hair and skin preparations are accessible and accompanied by sunscreen properties, but they do not provide extended effect, also causes side effects due to harsh chemicals. The present study focuses on the effects of polyherbal extracts containing Microsponge gel for the protection of skin from ultraviolet rays. In the present research, already prepared Microsponge gel through quasi-emulsion solvent diffusion (QESD) technique was used for the HPLC, in-silico, in-vitro antioxidant activity, and in-vivo study. AdmetSAR software tool was utilized for the in-silico study, whereas for the in-vivo study, UV radiations are given on Albino rats using solarimeter. Results shown the active constituents are non-carcinogenic and non-toxic; IC50 values show good antioxidant activity and minimal effect of UV radiations after application of the gel formulation on animal skin. The results manifest prominent effects on animal skin further test for presence of ascorbic acid level and total protein in blood further verify the efficacy of the formulation. The study consequently established a strong ground for further extensive clinical studies.

Formulation and Evaluation of Kaempferol Loaded Nanoparticles against Experimentally Induced Hepatocellular Carcinoma: In Vitro and In Vivo Studies.

The present study was designed to prepare Kaempferol loaded nanoparticles (KFP-Np) and evaluate hepatoprotective and antioxidant effects in hepatocellular carcinoma models. KFP was encapsulated with hydroxypropyl methylcellulose acetate succinate (HPMC-AS) and Kollicoat MAE 30 DP polymers to prepare nanoparticles (Nps) by quasi-emulsion solvent diffusion technique (QESD). The prepared Nps were evaluated for different pharmaceutical characterization to select the optimum composition for the in vivo assessment. An animal model of cadmium chloride (CdCl2)-induced hepatocellular carcinoma in Male Sprague Dawley rats was used in vivo to test the antioxidant and hepatoprotective capacity of free and encapsulated KFP. The prepared Npsshowed nanometric size, low PDI, high drug load as well as encapsulation with a better drug release profile. There was a significant decrease in the increased serum levels of alanine transaminase (ALT), total bilirubin (TBiL), and aspartate transaminase (AST), and the lipid peroxidation’s (MDA) level was attenuated, and levels of markers of the cell antioxidant defence system were restored including Glutathione S-transferase (GST), glutathione (GSH), superoxide dismutase (SOD) and catalase (CAT) via oral pre-treatment with KFP-Np (50 mg/kg b.w. (body weight), 6 weeks). KFP-Np significantly declines an mRNA expression of interleukin-1β (IL-1β), IL-6, and tumor necrosis factor-alpha (TNF-α) as well as decreased nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) protein expression. It also upregulated the mRNA expression and protein expression of nuclear factor erythroid 2-related factor 2 (Nrf2) and heme oxygenase-1 (HO-1). While comparing the protective effects of KFP encapsulated in Kollicoat MAE 30 DP and HPMC-AS, Nps was found to be betterthan free KFP. Insummary, result indicate that encapsulation of KFP in NPs provides a potential platform for oxidative stress induce liver injury.

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

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

Microsponges for controlled release and enhanced oral bioavailability of carbamazepine

The oral absorption and hence the oral bioavailability of carbamazepine (CBZ) is variable even after administration of rapidly dissolving formulation. This problem was attributed to supersaturation of CBZ and transformation to the less soluble carbamazepine dihydrate (CBD). Accordingly, formulation of sustained release products of CBZ is a promising approach to overcome this problem. Microsponges are an emerging formulation which can help in this direction. The aim of this work was to optimize the composition of microsponges for better encapsulation and sustained release of CBZ for oral administration. CBZ microsponges were prepared using quasi emulsion solvent diffusion technique with varying composition of ethyl cellulose and polyvinyl alcohol (PVA). Microsponges were evaluated using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray diffraction. Production yield, entrapment efficiency and surface morphology of microsponges were assessed in addition to drug release. Optimum formulation was administered orally to albino rabbits to evaluate the oral bioavailability with reference to unprocessed CBZ. The Instrumental analysis reflected the encapsulation of CBZ in amorphous or molecularly dispersed form in the microsponges. The size and entrapment efficiency of the microsponges increased with increasing polymer contents. This was associated with reduction in CBZ release. Optimum formulation enhanced the oral absorption of CBZ. This was manifested by 2.6-fold increase in the area under the plasma concentration versus time curve compared to that of unprocessed CBZ. The study introduced microsponges as promising carriers for sustained oral delivery of CBZ.

Microsponge Based Gel of Tea Tree Oil for Dermatological Microbial Infections

Objective: Tea Tree Oil (TTO), derived from Melaleuca alternifolia possesses broad spectrum antimicrobial potential. However, its therapeutic utility is impaired due to its high volatility, poor aqueous solubility and low stability in the presence of light, oxygen and temperature. The present study was attempted to investigate Ethyl Cellulose (EC) microsponges (MSs) as topical carriers for TTO to circumvent above mentioned limitations. Methods: TTO MSs were prepared using quasi emulsion solvent diffusion technique. The effect of formulation variables on the production yield, entrapment efficiency, particle size and drug release of MSs was investigated. The optimized MSs were dispersed into Carbopol 934 gel and evaluated for drug release, skin irritation, antibacterial activity and photostability. Results: Scanning electron microscopy revealed spherical and porous nature of TTO microsponges. The optimized MSs possessed particle size of 36.98 μm, percent entrapment efficiency of 93.12% and percent cumulative drug release of 79.18%, respectively. MS-loaded gels were found nonirritant. In addition, TTO loaded MS gels exhibited good stability. Antimicrobial effect of TTO MS gel showed broader zones of inhibition in comparison to TTO gel. Conclusion: The findings of our study suggest that MS loaded gel could prove alternative to conventional antibacterial formulations for dermatological microbial infections.

Influence of the ethanol/dichloromethane ratio on the preparation of microsponges composed of ethylcellulose and Eudragit or HPMCphthalate for hydrophilic drug delivery

Microsponges (MS) have shown great potential for the incorporation of relatively higher amounts of drugs. This is due to the presence of both surface pores and interconnected channels that provide a greater contact area for the absorption of active agents. However, the use of MS for carrying hydrophobic drugs is limited because the preparation methodology can totally remove hydrophilic drugs. Therefore, this work aimed to investigate possible changes in the proportion of organic solvents used to produce MS containing water-soluble drugs. A modified quasi-emulsion solvent diffusion technique was used to formulate MS with ethylcellulose and Eudragit RS 100 (MS-EE) or ethylcellulose and HPMCphthalate (MS-EH) using different combinations of ethanol/dichloromethane ratios. The effects of the polymeric composition and organic solvent ratio were evaluated on the morphology, size, swelling, yield, drug content, entrapment efficiency and in vitro release of methylene blue (MB), a hydrophilic drug model. Both polymer combinations resulted in spherical and porous particles. MS-EE was larger (8–13 μm) and displayed higher product yield (62–77%), but MS-EH showed a higher drug entrapment (11–41%), which was higher with an increase in the amount of ethanol amount used. Only MS-EH displayed in vitro MB release during 24 h (70%). ATR-FTIR and FT-Raman analyses did not demonstrate chemical interactions between MB and the polymers. Differential scanning calorimetry, thermogravimetry, and x-ray diffraction confirmed the molecular dispersion of MB in the MS polymer matrix. Ex vivo permeation studies by Franz cells and photoacoustic spectroscopy showed that MB could diffuse out from the polymer matrix and permeate both pig skin and mucosa. The particles were shown to be good carriers for MB and they provided controlled drug release and permeation through skin and mucous tissue; however, the MS particles themselves are not able to permeate these membranes. The use of ethanol in the solvent system constitutes a good strategy to obtain MS of ethylcellulose and HPMCphthalate for delivery of MB and suggests that MS is worthy of investigation as carrier for delivery other hydrophilic drugs.

Full Factorial Design, Optimization, In vitro and Ex vivo Studies of Ocular Timolol-Loaded Microsponges

Timolol maleate (TMM) is a hydrophilic model drug. The aim of this study was to formulate TMM-loaded microsponges to sustain TMM release and improve its corneal permeability compared with TMM-aqueous solution. The modified quasi-emulsion solvent diffusion technique (water/oil/oil) was used to prepare TMM-loaded microsponges. The impact of the polymer type (X1) and drug:polymer ratio (X2) were studied and optimized, using full factorial design. The production yield (PY) %, entrapment efficiency (EE) %, particles size (PS), and TMM released % after 6 h were selected as dependent variables. Depended on the desirability value by using the Design-Expert® software version 11, the optimized formulation was selected and subjected to further studies, such as scanning electron microscopy (SEM), porosity determination, powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), ex vivo permeation study, and corneal hydration level. The optimized formulation composed of TMM: EC within the proportion 1:9 exhibited PY of 96.55 ± 4.01%; EE of 72.00 ± 6.08%; PS (d90) of 6283.33 ± 145.71 nm and released 42.12 ± 3.93% of TMM after 6 h. Particles appeared porous with spherical shape. Thermal analysis proved that the drug has been homogeneously dispersed in its amorphous state. The optimized formulation showed higher corneal permeability about 1.45-fold higher than TMM-aqueous solution in a period of 6 h. The modified quasi-emulsion diffusion technique (water/oil/oil) is suitable for improving EE of hydrophilic drug (TMM) and the optimized TMM-loaded microsponge was succeeded to retard the release of TMM and improve its corneal permeability.

FORMULATION AND EVALUATION OF TERBINAFINE HYDROCHLORIDE MICROSPONGE GEL

Objective: The purpose of the present research work was to formulate and evaluate Terbinafine hydrochloride microsponges using quasi emulsion solvent diffusion technique and microsponge gel by using carbopol for controlled release of the drug and consequently avoiding its side effects.&#x0D; Methods: Microsponges containing Terbinafine hydrochloride were obtained successfully with six different drugs: polymer ratios. The formulations were studied for particle size, physical characterization, and in vitro release.&#x0D; Results: A selected THCI microsponge (MS IV) due to its better results when compared to other microsponge formulations was incorporated in different concentrations of carbopol and formulated as gels and evaluated for its pH, viscosity, spreadability, drug content, in vitro release, antifungal activity and in vivo studies. Among the four microsponge gel formulations, THMG II showed better results like pH 6.2, viscosity 3960 cps, spreadability 18.1 g cm/s, drug content of 87.6% and drug release showed fickian release pattern. The antifungal studies showed a zone of inhibition with 15.8 mm when compared to the pure drug, 19.2 mm, marketed formulation 16.0 mm and also showed better antifungal activity on fungal induced guinea pig skin when compared with control.&#x0D; Conclusion: In this study, we found that the controlled release of terbinafine hydrochloride from the microsponge gel reduced side effects and remarkably decreased gel application for fungal treatment.

Development of Risedronate Sodium-loaded Nanosponges by Experimental Design: Optimization and in vitro Characterization

The present investigation focussed on the development of a novel strategy to enhance the bioavailability of risedronate sodium, which has poor and erratic absorption. Nanosponges were statistically developed by full 32 factorial design using Design of Experiment software considering concentration of polymer and stabilizer as independent variables and particle size and entrapment efficiency as experimental responses by utilizing the modified quasi-emulsion solvent diffusion technique. Optimized formulation showed 67.27±1.05 % entrapment efficiency, 155.8±2.17 nm particle size and –35.4 mV of zeta potential. The data from in vitro release study showed burst release for initial 2 h followed by slow and sustained release up to 24 h, which followed a diffusion-controlled release mechanism by the Higuchi model. Scanning electron microscopy study showed uniformly discrete spherical particles with porous surface without any agglomeration. Stability study demonstrated no significant changes in particle size, entrapment efficiency and in vitro release, which indicated that the nanosponge formulation was stable. In conclusion, it appeared that the nanosponges were a suitable nanocarrier system that could play a significant role in improving osteoporotic condition.