European Journal of Biomedical and Pharmaceutical Sciences

FORMULATION AND EVALUATION OF MICRO BEADS LOADED BIO ADHESIVE VAGINAL GEL OF CLOTRIMAZOLE

Pratibha Dwivedi*, G. Gnanarajan and Preety Kotiyal

ABSTRACT

The objective of this study was to prepare and evaluate the micro beads loaded bio adhesive vaginal gel of clotrimazole. Micro beads provide the sustained release of drug and bio adhesive gel was act as a base for incorporation of micro beads to the vagina. Clotrimazole is an antifungal drug which is having a short half life (2hrs). To improve the bioavailability and stability of drug it was incorporated in micro beads from which it can be released slowly for prolonged period of time. Micro beads provide the sustained release of drug because of the presence of such sustaining and mucoadhesive polymers like sodium alginate, SCMC etc. Bio adhesive gel was prepared by using a bio adhesive polymer that is carbopol 934. Micro beads were prepared by ionotropic gelation method. Bio adhesive gel was prepared by accurately weighed carbopol 934 dispersed in distilled water containing glycerol and stirred the mixture with homogeniser until thickening occurred. Neutralization was done by added triethanolamine drop by drop and maintains the pH. Continue the mixing of solution until the transparent gel was obtained. Micro beads were analysed for drug loading, shape (scanning electron microscopy), flow properties, drug encapsulation efficiency, and the properties were found to be discrete, spherical with free flowing particles. The bio adhesive gel was evaluated for pH, spreadability, extrudability, viscosity, bio adhesion test. The final prepared formulation which is micro beads loaded in bio adhesive gel was evaluated for in vitro release study, drug release kinetics and antifungal studies. The range of swelling index was found to be 52-80% which shows moderate to good swelling property of micro beads. The percent drug loading was founded within the range of 66.23-92.59%. F5 shows the maximum drug loading that is 92.59 which show that F5 possess highest incorporated amount of drug within the micro beads. The percent encapsulation efficiency was founded within the range of 44.56-78.42% which indicates moderate to good efficiency. Spreadibility measurement was found within the range of 5.54-9.59cm² in diameter. In vitro release study on all six formulations of clotrimazole micro beads loaded in bio adhesive gel were carried out in SVF 4.5 using cellophane membrane and modified apparatus. The cumulative percent release was founded within the range of 87.76-79.28% for all six formulations in12 hrs. F1 shows the highest in vitro release of drug. From the results it was observed that as we increase the polymer concentration, release of drugs from micro beads loaded gel decreases.

Keywords: Micro beads loaded bio adhesive gel, bio adhesion, antifungal activity.