The microsponges formulations were prepared by quasi-emulsion solvent diffusion method employing eudragit RS as a polymer. Afterwards, microsponge formulations were prepared by gradually increasing the drug: polymer ratio. The surface morphology, particle size, production yield, and drug entrapment efficiency of microsponges were examined. Shape and surface morphology of the microsponges were examined using scanning electron microscopy. The drug entrapment efficiency of the microsponges was found in the range of
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The aim of the present study was to improve the release rate of curcumin by microsponges prepared through quasi-emulsion solvent diffusion technique using ethylcellulose and PVA as carriers. The prepared microsponges were further filled in hard gelatin capsule shell and then loaded in carbopol gel to evaluate its potential in oral and topical drug delivery.
Further, it was observed from the studies on release rate that microsponges filled in hard gelatin capsule shells batch MS4 showed Furthermore, the microsponges loaded in carbopol gel were evaluated for ex vivo drug deposition studies and it was found that The estimated drug remained in the skin was The drug release profile data were found to be fitted best into the zero-order model with anomalous transport mechanism of drug release in both cases.
Microsponges have unique dissolution and compression properties due to their sponge-like texture Jangde They are highly effective, stable, non-irritant, non-toxic, non-allergic, non-mutagenic and also minimum side effects with improved patient compliance Amrutiya et al. Further, these active microsponges can be incorporated into formulations, such as capsules, gel and powders, and share a broad package of benefits Pawar et al. The microsponges have demonstrated their use in cosmetics and pharmaceuticals viz.
Salwa et al. Curcumin CUR is a yellow colored naturally occurring polyphenol compound obtained from the rhizomes of Curcuma longa , family Zingiberaceae. It is a highly pleiotropic molecule which can interact with different molecular targets involved in inflammation Ornchuma et al. It can change inflammatory response by downregulating the activity of cyclooxegenase2 COX2 , lipoxygenase, and inducible iNOS nitric oxide synthase enzyme.
Curcumin being a natural substance is non-toxic even at higher dose Aziz et al. The present study was designed with the objective to enhance the dissolution and thus the release rate of the drug and bioadhesive potential of the preparation. Curcumin-loaded microsponges were prepared by quasi-emulsion solvent diffusion method using ethyl cellulose EC and polyvinyl alcohol PVA. The prepared microsponges were filled in hard gelatin capsule shells and also loaded in carbopol gel.
The capsules were evaluated by different pharmacopoeial tests and also the mechanical strength of the gel was determined by texture analyzer. The total drug content, production yield, mean particle size and entrapment efficiency were calculated. The formed microsponges were demonstrated for their applications in oral and topical delivery systems. The preparation was further evaluated for its in vitro drug release behavior and ex vivo bioadhesion studies using a Franz diffusion cell.
Polyvinyl alcohol, dichloromethane, methanol, lactose monohydrate, magnesium stearate, triethanolamine, polyvinyl alcohol, propylene glycol, carbopol P and N -methylpyrrolidone were procured from SD Fine-Chem.
Limited, Mumbai. All other chemicals were of reagent grades and used as procured. Curcumin CUR microsponges were prepared by quasi-emulsion solvent diffusion method Jain and Singh The internal phase was then added dropwise into the aqueous external phase containing polyvinyl alcohol 0. The mean particle size and polydispersity index PdI of all the batches of microsponges were measured using Mastersizer Malvern Instruments Ltd.
The total drug content was calculated as follows Eq. Prior to observation, the samples were mounted on metal grids, using double-sided adhesive tape and coated with gold under vacuum. After filling the CUR microsponges in capsule shells along with the excipients starch, acacia, sodium lauryl sulfate, lactose monohydrate and magnesium stearate, the filled capsules were evaluated for their organoleptic properties size, shape and color, etc.
The weight variation and the disintegration tests were performed on filled capsules as per the methods specified in IP All the experiments were performed in triplicate. Curcumin microsponges were then uniformly dispersed in carbopol gel. To this aqueous dispersion, propylene glycol and N -methylpyrrolidone were added as permeation enhancers. After visual examination of the gel for its consistency, color and homogeneity, the gel was further evaluated for following parameters.
The measurement of pH of formulation was done in triplicate and the mean value was calculated. Diameters of spread circles initial and final were measured in cm and were taken as comparative values for spreadability. Rheology includes the measurement of viscosity in centipoise, which indicates resistance of a fluid to flow. The viscosity of gel was measured by Brookfield viscometer using spindle No.
Structural analysis of carbopol gel and curcumin microsponges gel was done to determine their mechanical properties such as hardness, cohesiveness, and adhesiveness.
From the resulting texturogram, hardness and adhesiveness were calculated Bhatia and Ahuja Drug deposition study was performed on the excised rat abdominal skin using a Franz diffusion cell Padamwar and Pokharkar Epidermal side of the skin was exposed to ambient condition, while dermal side was kept facing the receptor solution.
The samples were withdrawn at different time intervals. The skin was carefully removed and drug present on the skin surface was cleaned with distilled water and analyzed for drug content. Drug was extracted from the skin using a modified procedure Echevarria et al.
The lag time t L , h was determined from the x -intercept of the slope at steady state. Quasi-emulsion solvent diffusion method has been used for the development of CUR microsponges.
These microsponges were filled in capsule shells and were also loaded in carbopol gel. The microsponges were characterized by various parameters and evaluation of the capsules and gel was carried out by different techniques. It is found that on increasing the drug to polymer ratio, the increase in production yield and mean particle size is observed up to batch MS4, that is having drug to polymer ratio , but as the drug to polymer ratio is increased the decrease in production yield and entrapment efficiency is observed.
This may probably be due to lesser availability of polymer to entrap the drug and the growth in mean particle size may be due to increasing drug to polymer ratio.
The total drug content and entrapment of the drug depend on the successful molecular association of the drug with the polymers. TDC and EE of the microsponges were found in the range of The probable reason for this decrease in TDC and EE could be that the optimum concentration of polymer is not available to coat or entrap the drug molecules.
In spectra of CUR, as shown in Fig. The spectra of EC, Fig. However, comparison of the spectra demonstrated no new characteristic peaks in the microsponge which indicated no physical or chemical interactions between curcumin and carrier polymer. Ethyl cellulose being an amorphous substance does not possess sharp endothermic peaks whereas the thermogram of CUR shows a sharp endotherm at The thermogram of curcumin microsponges shows a broad endotherm at The shifting of endotherms and appearance of a new exotherm and decrease in heat of fusion indicate that some modifications have occurred.
SEM micrographs displayed that microsponges formed are predominantly spherical and entire curcumin crystals are not seen. X-ray diffractogram of EC is typical of amorphous materials with no sharp peaks. The batch MS4 was subjected to 3-month stability study at accelerated conditions and was analyzed for physical appearance, in vitro drug release and FTIR spectroscopy.
The in vitro percentage drug release came out to be Thus, all these parameters suggested that the formulation MS4 may have good shelf life. The average weight of capsule formulations was found to be within pharmacopoeial limit. All the batches of CUR microsponges-loaded capsules were evaluated for drug release behavior. The drug release was determined in methanolic phosphate buffer pH 7. It can be inferred from the graph that the batch MS4 shows Therefore, it is inferred from the study that microsponges2 have displayed enhanced dissolution of curcumin as compared to pure drug.
The release rate data of CUR microsponges-loaded capsules were fitted into various kinetics models to estimate their release kinetics and mechanism of release. The non-opaque pale yellow gel with a pH of 6. An apparatus suggested by Mutimer et al. Viscosity of carbopol and microsponge gel was determined using Brookfield viscometer. There is no significant difference in viscosity of both the gels and a drop in viscosity is observed with the increasing rpm for both the gels as shown in Fig.
The topical formulation must exhibit acceptable mechanical characteristics such as low hardness and high adhesiveness. The maximum detachment force; F max, i. The height of the peak is the maximum force required to separate the probe from the gel i. The texturograms as shown in Fig. It was observed from Fig. Hence, no significant difference is observed in the hardness and adhesiveness of the gels.
Texture analysis of a carbopol gel and b CUR microsponges gel. At the end of the study, the drug CUR remained in the skin was found to be The permeation flux and permeability coefficient are found to be The objective of developing polymeric microsponge delivery system was to deliver curcumin in a sustained manner for an extended period of time, to reduce frequency of administration and to improve its bioavailability.
Therefore, in the present study curcumin microsponges were prepared by simple, reproducible and rapid quasi-emulsion solvent diffusion method. The prepared microsponges were then incorporated in capsule dosage form and were loaded in carbopol gel. Varied drug—polymer ratio reflected a remarkable effect on particle size, total drug content and encapsulation efficiency.
The curcumin microsponges filled in the capsule shells showed Further, the curcumin microsponges loaded in the carbopol gel showed The amount of drug remained in the skin was found to be Thus, curcumin microsponges prepared in this study were found to be promising as newfangled delivery system offering prolonged release of drug and, hence, would be more useful than conventional formulation therapy in oral as well as in topical drug delivery.
The authors M. Bhatia, M. Saini declare that they have no conflict of interest. This article does not contain any studies with human and animal subjects performed by any of the authors. Publisher's Note.
We'd like to understand how you use our websites in order to improve them. Register your interest. The aim of the present research was to develop Fluconazole loaded microsponge-based topical delivery system for controlled release and enhanced drug deposition in the skin. Microsponges containing fluconazole were prepared by an emulsion solvent diffusion method.
Formulation and evaluation of curcumin microsponges for oral and topical drug delivery
The aim of the present study was to improve the release rate of curcumin by microsponges prepared through quasi-emulsion solvent diffusion technique using ethylcellulose and PVA as carriers. The prepared microsponges were further filled in hard gelatin capsule shell and then loaded in carbopol gel to evaluate its potential in oral and topical drug delivery. Further, it was observed from the studies on release rate that microsponges filled in hard gelatin capsule shells batch MS4 showed Furthermore, the microsponges loaded in carbopol gel were evaluated for ex vivo drug deposition studies and it was found that The estimated drug remained in the skin was The drug release profile data were found to be fitted best into the zero-order model with anomalous transport mechanism of drug release in both cases.
Formulation and Evaluation of Optimized Oxybenzone Microsponge Gel for Topical Delivery
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