Quasi-emulsion Solvent Diffusion Research Articles

Modification of Ceritinib Crystal Morphology via Spherical Crystallization

The formulation process for some drugs can be challenging, due to their unfavorable physical and mechanical properties and poor water solubility. Powder technology has made a significant impact in regard to the modification of the particles in active pharmaceutical ingredients (APIs) to produce high-quality granules. Spherical particles are preferred over other shapes, due to their high tap and bulk density, reduced dustiness, better flowability, strong anti-caking properties, and better mechanical performance during tableting. The present study investigates the possibility of obtaining spherical crystals of ceritinib, a drug used for the treatment of anaplastic lymphoma kinase (ALK)-positive advanced non-small cell lung cancer, which belongs to BCS class IV drugs and has a platy crystal structure. Ceritinib spheres were prepared by spherical agglomeration, in a ternary system, and quasi-emulsion solvent diffusion, with the addition of polyvinylpyrrolidone, as well as a combination of these two methods. With the combined method of spherical crystallization, crystals with the most favorable morphology and the narrowest distribution of particle sizes were obtained, which was the reason for further optimization. The influence of different impeller geometries and mixing rates on the morphology of the obtained crystals was examined and the optimal conditions for the process were selected. Using empirical correlations and a visual criterion, the process was scaled up from a 0.1 L to a 1 L batch crystallizer. The obtained crystals were characterized by light and scanning electron microscopy. The addition of a bridging liquid and/or a polymer additive did not change the internal structure of the ceritinib crystals, which was confirmed by X-ray powder diffraction.

Formulation and Assessment of Tolnaftate Microsponges for Topical Medication Deliverance

Objective: This study aimed to develop and evaluate the sustained delivery of Tolnaftate using topical polymeric microsponges. Materials and Methods: Tolnaftate-loaded microsponges made of ethyl cellulose were prepared via quasi-emulsion solvent diffusion. The effects of the drug-to-polymer ratio on active drug content, particle size, and entrapment efficiency were examined. The optimized formulation was incorporated into a Carbopol gel and evaluated for drug content, pH, viscosity, and in vitro drug release. The study considered internal phase volume, stirring rate, and emulsifier concentration as variables and analyzed their impact on entrapment efficiency and particle size. Results: Increasing stirring speed reduced particle size and improved entrapment efficiency, while a higher volume of dichloromethane decreased particle size. Scanning electron microscopy revealed porous and spherical microsponges. The 1.5:1 drug-to-polymer ratio yielded the highest active drug content, optimal entrapment efficiency, and smallest particle size, making it the preferred ratio for further studies. Conclusions: The drug release from the microsponge gel was more sustained compared to both the marketed product and pure drug gel. An ex vivo drug deposition study using rat abdominal skin showed satisfactory drug deposition. These polymeric microsponges show potential as a topical drug delivery system for antifungal therapy.

Formulation, Design, Optimization, and Characterization of Novel Long-acting Injectable Dosage Form of Anti-psychotic Drug

Background: The current research aimed to create and analyze a new long-acting Brexpiprazole (BRX) injectable for successful anti-psychotic drug therapy in order to decrease dosage frequency and increase patient compliance. Systems for drug transport to particular body sites or regulating release rates with accuracy are known as drug delivery systems (DDS). By affixing the drug to a carrier particle like liposomes, nanoparticles, microspheres, etc., which modifies the drug's absorption and release properties, using carrier technology, drugs may be delivered in an intelligent manner. Methods: Utilizing Resomer RG 502 H and RESOMER® RG 752 H extended-release Polymer, Using a quasi-emulsion solvent diffusion, microspheres were made, and emulsification and solvent evaporation process. Results: The produced microspheres were assessed for stability tests, in vitro drug release, flow characteristics, and drug entrapment efficiency. FTIR experiments were used to establish how well the drug excipients worked together. The acarbose microspheres that were created had an 89.9 to 96.1 percent drug entrapment efficiency. The impact of factors like polymer content on medication release was studied. The Stability study of the formulation was carried out under different conditions, and data were established. Comparative pharmacokinetic studies between marketed oral formulation and Brexpirazole microsphere test formulations in Wistar/SD Rats were carried out and concluded. Conclusion: Brexpiprazole (BRX) novel long-acting injectable formulation, could be used effectively for the treatment of mentally challenged anti-psychotic patients worldwide.

Fabrication and Characterization of Andrographolide-loaded Microsponges to Enhance Oral Bioavailability of Drug against Colon Cancer Using HT29 Cells

Background: The current research aimed to determine ways to improve the bioavailability of andrographolide (AGP) for use in colon cancer treatment by developing and evaluating microsponges loaded with the drug. Methods: Utilising the quasi-emulsion solvent diffusion approach, microsponges containing AGP were synthesised. A total of ten formulations were prepared using different concentrations of drug, polymer and other excipients. Particle size, shape, and differential scanning calorimetry (DSC) were used to characterise the microsponges that were created. To find out the rate at which the microsponges would expel their contents, researchers measured their release dynamics. In vitro anticancer activity of formulation was determined using HT29 cells Results: Results showed that the percentage yield of the formulations ranged from 10.85-41.03%. The highest drug concentration was achieved in formulation F8 with a particle size of 33.7 nm. SEM analysis demonstrated that the particles were round and possessed a rough and porous surface. Increasing the ratio of ethyl cellulose to AGP reduces surface roughness. The microsponge's DSC difractogram reveals prominent peaks at 18°, 24°, and 38° (2 θ) with reduced intensity, suggesting that the microsponges' crystalline character has diminished. In vitro drug release study showed 93.85% release upto 12 hours. Mathematical models showed normal release of the formulations with “n” values greater than 0.90 of all the formulations. Formulation F8 decreased the HT-29 cells' ability to survive. The percentage of cell cytotoxicity was 75.54 at 100μg/ml. Since AGP microsponges had a detrimental effect on the survival of colorectal cancer cells. Conclusion: It can be concluded from the study that prepared formulations possess anticancer properties against cancerous cells and can be used as an alternative anticancer drug.

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.

Development, optimization, and in-vivo bioavailability study of erlotinib hydrochloride loaded microsponge for colon targeting

The present investigation aimed to develop as well as optimize microsponge containing erlotinib hydrochloride (ETB) that was composed of ethyl cellulose (EC) and pectin. The water solubility and enzymatic susceptibility make it easier to fabricate the microsponge formulation. The ETB loaded microsponge was manufactured using quasi-emulsion solvent diffusion process. By this technique, organic solution of the primary component is emulsified with stabilizing agents that are soluble in water. To design the formation of the microsponge, 32 factorial design was implemented. It was investigated how the response variables like particle dimension, entrapment efficiency, ETB diffusion at 12 ​h were influenced by independent variables such as rotation speed and the pectin to ethyl cellulose ratio. The optimal microsponge formulation loaded with ETB (F0) composed of 1:2.8 ratio of pectin to ethyl cellulose (EC) with stirring rate at 478 ​rpm. Particle dimension, entrapment efficiency, and ETB release at 12 ​h from optimized formulation were shown 104.89 ​± ​0.62 ​nm, 82.36 ​± ​2.85 ​%, and 85.49 ​± ​1.84 ​% respectively. The In-vivo pharmacokinetic study conducted on rabbit model shows a significant improvement in bioavailability. The optimized microsponge formulation has been found to have a higher Cmax than the ETB aqueous suspension. The stability of the formulation has been determined by the accelerated stability study of optimized microsponge formulation. This study indicated that the optimized formulation retained its stability even after 90days. In general, the present investigation demonstrated that drug loaded microsponge based formulation is a suitable method to improve the therapeutic efficacy and bioavailability of ETB.

Enhancing flowability of lamivudine through quasi-emulsion solvent-diffusion (QESD) crystallization: A comprehensive study on surfactant impact, particle morphology by QbD concepts and tablet compression challenges

Lamivudine (LMD), an enantiomer of 2′-deoxy-3′-thiacytidine, plays a crucial role in combatting HIV-1 and managing hepatitis B virus infections. Despite its effectiveness, challenges arise from its difficult flowability and tendency to agglomerate during storage, necessitating a granulation step before tablet compression, as direct compression has proven ineffective. This study aimed to optimize Lamivudine spherical agglomerates using response surface methodology, delving into the intricate relationship between design factors (concentration of tween, span, and acetone) and experimental outcomes (yield and particle size) through central composite design. Analysis of variance (ANOVA) was employed for optimization, with the Quasi-emulsion solvent-diffusion (QESD) crystallization technique utilized for the checkpoint batch. This technique, involving a single solvent and antisolvent with surfactants, showcased remarkable enhancements in flowability and reduced storage agglomeration. The impact of various surfactants [Hydroxy Propyl Methyl Cellulose (HPMC), polysorbate 80, and sorbitane monooleate] on particle morphology, flowability, and storage agglomeration during crystallization was thoroughly assessed. While achieving direct compression into tablets, the porous structure of LMD agglomerates presented challenges in tablet press production speeds, prompting adjustments such as reducing punch speed or implementing a precompression step. Positive outcomes were realized for disintegration and in vitro drug release in comparison to direct compression and wet granulation methods. In conclusion, the QESD crystallization technique successfully yielded hollow, spherical LMD agglomerates with enhanced properties, representing a significant milestone in pharmaceutical formulation.

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

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

Development of 4-phenylbutyric acid microsponge gel formulations for the treatment of lewisite-mediated skin injury.

Lewisite, a chemical warfare agent, causes skin blisters, erythema, edema, and inflammation, requiring mitigation strategies in case of accidental or deliberate exposure. 4-phenyl butyric acid (4-PBA), a chemical chaperone, reduces endoplasmic reticulum stress and skin inflammation. The study aimed to encapsulate 4-PBA in microsponges for effective, sustained delivery against lewisite injury. Porous microsponges in a topical gel would potentially sustain delivery and improve residence time on the skin. Microsponges were developed using the quasi-emulsion solvent diffusion method with Eudragit RS100. Optimized formulation showed 10.58%w/w drug loading was incorporated in a carboxymethylcellulose (CMC) and Carbopol gel for in vitro release and permeation testing using dermatomed human skin. A sustained release was obtained from all vehicles in the release study, and IVPT results showed that compared to the control (41.52 ± 2.54µg/sq.cm), a sustained permeation profile with a reduced delivery was observed for microsponges in PBS (14.16 ± 1.23µg/sq.cm) along with Carbopol 980 gel (12.55 ± 1.41µg/sq.cm), and CMC gel (10.09 ± 1.23µg/sq.cm) at 24h. Optimized formulation showed significant protection against lewisite surrogate phenyl arsine oxide (PAO) challenged skin injury in Ptch1+/-/SKH-1 hairless mice at gross and molecular levels. A reduction in Draize score by 29%, a reduction in skin bifold thickness by 8%, a significant reduction in levels of IL-1β, IL6, and GM-CSF by 54%, 30%, and 55%, respectively, and a reduction in apoptosis by 31% was observed. Thus, the translational feasibility of 4-PBA microsponges for effective, sustained delivery against lewisite skin injury is demonstrated.

Formulation of microsponges of anti-fungal drugs and their pharmacokinetic and in vitro analysis

Microsponges are uniform, spherical, porous polymeric microspheres having myriad interconnected voids of particle size range 5-300 μm. These microsponges have the capacity to entrap a wide range of active ingredients such as emollients, fragrances, essential oils, sunscreens and anti-infective, etc. and then release them onto the skin over a time in response to a trigger. Microsponge Delivery System (MDS) can be used to resolve the problem associated with these conventional approaches. The drug entrapped microsponges can be incorporated into a formulated product, such as a gel, cream, liquid or powder. Microsponge is as tiny as a particle of talcum powder. Although they are microscopic in size, these systems are too large to pass through the stratum corneum thus preventing excessive accumulation of drugs within the epidermis and dermis, and hence systemic entry of the drugs. They increase the rate of solubilization of poorly water soluble drugs by entrapping such drugs in pores of the microsponges. In this study, Flutrimazole and Oxiconazole nitrate microsponge were prepared by quasi-emulsion solvent diffusion method. The microsponges thus prepared, were evaluated for production yield, loading efficiency, particle size analysis, SEM, IR, DSC, PXRD, characterization of pore structure, in-vitro release study of microsponges, and stability. Then, gels loaded with microsponge and plain drug were formulated and evaluated for rheology, diffusion, skin irritation and antifungal activity. Antifungal activity of Flutrimazole and Oxiconazole nitrate containing microspongic gels were compared with marketed formulations. The microsponges showed good production yield, loading efficiency and particle size. All characteristic peaks of the drugs were concordant with IR spectra of pure drugs. PXRD and DSC studies revealed amorphization of drugs. SEM images showed that styrene microsponges prepared by suspension polymerization were finely spherical and uniform, while Eudragit microsponges prepared by quasi-emulsion solvent diffusion method were comparatively less spherical. According to intrusion and extrusion curves, majority of the pores present in Eudragit microsponges were spherical type, whereas the pores of styrene microsponges were mainly cylindrical-hole type. BET multipoint adsorption isotherm studies revealed that the percent of porosity of styrene microsponges is comparatively higher than Eudragit based microsponges. During the storage of drug-entrapped microsponges at 40±2°C and 75±5% RH for 6 months, surface morphology and release of drug showed no notable changes. Viscosity determination of gel showed that gels loaded with microsponge are more viscous than gel loaded with plain drug. The controlled drug release was observed with all the microspongic gels. Antifungal activity of gels containing microsponge entrapped Flutrimazole and Oxiconazole nitrate showed that antifungal activity of drugs was retained even after entrapment in microsponges and it was higher as compared with the gel containing free drug and marketed formulation. Gels containing drugs entrapped in microsponges.

Preparation, characterisation and in vitro anti-inflammatory activity of Baicalin microsponges

Baicalin, a flavonoid extracted from traditional Chinese medicine, Scutellaria baicalensis has significant anti-inflammatory effects. Microsponges are drug delivery systems that improve drug stability and slow the release rate. The combination of baicalin and the microsponges produced a new and stable system for its delivery, resulting in a novel formulation of baicalin. Baicalin microsponges (BM) were prepared using the quasi-emulsion solvent diffusion method. Effects of the mass ratio of the polymer (ethylcellulose) to baicalin, the concentration of the emulsifier polyvinyl alcohol (PVA), the stirring speed on the encapsulation efficiency (EE), and yield of the microsponges were investigated by combining the one-factor test and Box-Behnken design (BBD). The preparation process was standardised using 2.61:1 mass ratio of ethyl cellulose to baicalin, 2.17% concentration of PVA, with stirring at 794 rpm. Optimised BM formulations were evaluated for the parameters of EE (54.06 ± 3.02)% and yield of (70.37 ± 2.41)%, transmission electron microscopy (TEM), and in vitro cell evaluation. Results of the in vitro anti-inflammatory assay showed that baicalin microsponges-pretreated-lipopolysaccharide (LPS)-induced RAW264.7, mouse macrophages showed reduced inflammatory response, similar to that seen in baicalin-treated macrophages.

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

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

Evaluation of Insulin Loaded Microspheres for Oral Delivery

Microsphere-based colon-specific medication delivery devices should improve bioactive chemical administration and residence periods. In the first step, insulin microspheres were made using Eudragit RL 100 and L-100 by quasi-emulsion solvent diffusion. Microspheres were made since prior research showed that colon tissue macrophages could take up drug carrier systems with a molecular weight of 956 m or less. The uptake process allows accurate medication delivery to the specified site. Microspheres’ longer residence time than conventional drug delivery methods may allow dosage reduction and therapeutic efficacy. Because microspheres are permeable, they may be compacted and used to make stronger tablets. Thus, the CPDRS1 formulation performs well, enabling insulin delivery via an anti-diabetic microsphere. Drug-polymer ratio affects microsphere size and form. Variations in emulsifying agent amounts affect microsphere sizes and manufacturing yield. Using appropriate polymer and emulsification agent concentrations improves insulin-loaded Eudrajit L microsphere (Eudrajit RL) formulation and manufacturing yield

Review on Microspheres: A Novel Approach in Drug Delivery System

A well-designed controlled drug delivery system has the potential to address the limitations of conventional drug therapy and enhance the therapeutic effectiveness of a drug. Microspheres, which are characterized by their particle size being 1-1000 μm, are considered a novel and controlled drug delivery system. The spherical shape of microspheres contributes to their advantageous properties. This review focuses on the utilization of microspheres as a novel drug delivery system. These characteristics can be modified by altering the materials, methods, polymers, or techniques used in the production of microspheres. Microspheres are composed of natural or synthetic polymers. They are utilized in drug delivery systems to achieve prolonged or controlled drug release, enhancing bioavailability, stability, and action at specific sites at predetermined rates. Microspheres can be manufactured using various natural or synthetic materials. Different types of microspheres include bio adhesive, magnetic, floating, radioactive, polymeric, biodegradable polymeric, and synthetic polymeric microspheres. These microspheres are prepared using methods such as spray drying, solvent evaporation, single emulsion technique, double emulsion technique, phase separation coacervation technique, spray drying and spray congealing, solvent extraction, and quasi-emulsion solvent diffusion. Microspheres have a wide range of applications and evaluation parameters. Keywords: Microsphere, Novel Drug Delivery, Types of Microspheres, Methods of preparation Microspheres, Biodegradable.

Formulation, optimization, and in-vitro evaluation of polymeric microsponges for topical delivery of vanillin

The development of ethylcellulose-based polymeric microsponges for the topical delivery of therapeutic agents has attracted the interest of pharmaceutical scientists around the globe in recent years. This work represents preparation, optimization (using Box–Behnken design [BBD]), and characterization (in-vitro and ex-vivo) of ethylcellulose microsponges loaded with vanillin for effective topical delivery to treat wounds. Vanillin-ethylcellulose microsponges were prepared by using quasi-emulsion solvent diffusion and optimized formulation (F9) (containing 100 mg ethylcellulose, 10 mL dichloromethane, 100 mg vanillin, and 90 mg polyvinyl alcohol) developed showed particle size (90.3 ± 2.9 µm), high entrapment of vanillin (79.0 ± 2.8%), and optimum colloidal properties (zeta potential = −37.91 ± 2.44 mV; polydispersity index (PDI) = 0.224 ± 0.23). Optimized formulation extended the release of vanillin (96.68 ± 3.11%) in-vitro for 24 h. Vanillin-ethylcellulose microsponges (F9) dispersed in Carbopol 940 gel showed limited ex-vivo skin permeation (steady-state flux, JSS = 243.7 ± 6.2 µg/cm2/h) and higher skin retention (82.46 ± 6.74%) for 24 h in pig ear skin compared to plain vanillin Carbopol 940 gel (steady-state flux, JSS = 1350 ± 10.8 µg/cm2/h, skin retention = 33.66 ± 4.53%). Results of confocal laser scanning microscopy (CLSM) of Vanillin-ethylcellulose microsponges (F9) Carbopol 940 gel revealed accumulation of microsponges in the stratum corneum layer of skin as a depot. Microsponges-based Carbopol 940 gel also displayed excellent in-vitro antibacterial activity (zone of inhibition = 24.2 ± 1.3 mm) against Staphylococcus aureus for 24 h compared to plain vanillin Carbopol 940 gel (zone of inhibition = 10.30 ± 1.2 mm) that was considered good for its wound healing activity. Therefore, developed vanillin-loaded ethylcellulose microsponges could be effectively used in the treatment of wounds by reducing side effects associated with vanillin and promoting its localized delivery in Carbopol 940 gel form.

Formulation and Evaluation of Terbinafine Hydro-chloride Loaded Microsponges Gel

Background: Microsponges are porous, polymeric microspheres employed for sustained topical treatment. They may modify the release pattern, lessen adverse effects, and improve stability. Terbinafine HCL is a fungicidal allylamine derivative with a wide range of antifungal activity. It is used to treat various skin disorders like ringworm, athlete’s foot, and jock itch. Objective: The aim of the current study focuses on the development of terbinafine HCL microsponges that will release the drug in a sustained pattern to prevent side effects and then put those microsponges into a gel. Method: The quasi-emulsion solvent diffusion method was employed to develop Microsponges by using various drug: polymer ratios. Result: The results of the FTIR spectra showed that there was an absence of interaction between Terbinafine HCL and the excipients. Based on the evaluation parameter, it was found that batch MS3 showed the highest entrapment efficiency of 86.32%. Polymer EC showed better results. Microsponges and Microsponges gel showed sustained release of drug till 8 and 10 hours, respectively. The gels were shown to be stable throughout a wide temperature range, according to the stability studies. Conclusion: It was concluded that the Microsponges release the drug in a stained manner. The production process for microsponge technology has the potential to improve patient compliance with terbinafine hydrochloride microsponge gel.

DEVELOPMENT OF ACECLOFENAC LOADED MICROSPONGE GELS: A STATISTICAL QUALITY BY DESIGN (QBD) APPROACH TOWARDS OPTIMIZATION AND EVALUATION

Objective: The current research aims to deliver Aceclofenac in a controlled manner through a microsponges-loaded drug delivery system for the treatment of inflammation. Methods: The formulations were prepared by the Quasi-emulsion solvent diffusion method and characterized for particle size and drug entrapment efficiency. For the optimization of the formulation through the Quality by Design (QbD) approach, Quality target product profiles (QTPP) were set up considering various key factors that affect the quality of the formulation. Further optimization of the important factors in relation to the major Critical Quality Attributes (CQAs) was conducted by applying full factorial design using the Design of Expert Software (11.0 software, Stat-Ease, Inc., USA). The optimized formulation was incorporated into the gel, and characterized for morphological analysis by Scanning Electron Microscopy (SEM), drug content, and ex-vivo permeation studies (DD solver, Version 2.0). Results: It was found that process parameters such as drug-to-polymer ratio, the volume of the internal phase, and concentration of the emulsifier and polyvinyl alcohol (PVA), played a crucial role in improving the drug entrapment efficiency and particle size. On the other hand, stirring time did not significantly affect the particle size. Through Design of Expert (DOE) analysis, a PVA concentration of 0.641 mg/ml and an internal phase volume of 12.5 ml were identified to be the ideal concentrations to obtain the optimized microspongal gel formulation (MS4). Characterization studies were carried out on MS4, which displayed a drug encapsulation of 94%, with a Cmax of 81.62 mg/ml, and a Tmax of 12 h. Stability studies carried out as per the International Conference of Harmonization (ICH) guidelines confirmed no noticeable change in physical appearance and drug content. Conclusion: Overall, this study focused on optimizing the formulation of microsponges for efficient dermal drug delivery, considering various critical variables and process parameters. The resulting optimized formulation demonstrated promising drug release and potential for the effective management of inflammation disorders.

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 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 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.