Abstract

FORMULATION AND CHARACTERIZATION OF MUCOADHESIVE MICROSPHERES OF QUERCETIN DIHYDRATE

R. C. Jat*, Dr. Suman Jain and Kanika Arora

ABSTRACT

In an effort to augment the prophylactic action of Quercetin Dihydrate against mustard agent poisoning, mucoadhesive microspheres, which have the ability to reside in the gastrointestinal tract for an extended period, were prepared. The microspheres contained Quercetin Dihydrate, an adhesive polymer (ethyl cellulose) and a colon specific polymer (Eutragit S 100). Microspheres were prepared by an oil/water emulsification solvent evaporation method. Two formulation variables polymer concentration and plasticizer concentration were used. The microspheres were characterized by their micromeritic properties, such as % yield, bulk density, tapped density, % compressibility, particle size determination, angle of repose, Carr‘s index, incorporation efficiency, swelling property, in vitro mucoadhesion, in vitro drug release, in- vivo release etc. It was found that the mean particle sizes of the prepared microspheres are found significantly increasing with polymer concentration and decreasing with increasing plasticizer concentration. The FT-IR spectra of the pure drug and formulation F1 indicated that characteristics peaks of Quercetin were not altered, indicating no chemical interactions between the drug and carriers used. The drug entrapment efficiency increased with plasticizer concentration. The Percentage mucoadhesion increases with concentration of ethyl cellulose but not more affect concentration of eudragit. The drug entrapment efficiency was found in range of 73.35±2.7 (batch R1) to 80.61±1.54 (batch F5). . The range of angle of repose was found 19.72±1.33 (batch-F5) to 23.01±1.6 (batch-P1). The Carr‘s index was found in the range of 6.94±1.01 (batch-F1) to 14.45±1.17 (batch-F7). All formulations had excellent flow property. Formulation F5 had free flowing and others have good flowing property. The C.I. decreased with increasing amount of plasticizer and amount of polymer.The best fit release kinetic model was found to be Higuchi for all formulations, which indicated release from matrix type formulation. The In vivo studies on male wistar rats were conducted and plasma concentration time method was employed to study the influence of quercetin by formulating it as microspheres. By Statistical Analysis through sigma plot, the semi log plot of pure drug (Quercetin) and its microspheres shows linearity which indicates that they follow linear kinetics. Thus, it was concluded that the absorption kinetics and availability of quercetin is modified and altered by formulating it as microspheres. It is strongly indicated that formulation of microspheres of quercetin produced a sustained effect on its absorption and availability and several parameters are there which concluded that the microspheres of quercetin are better choice for mustard toxicity as compared to pure drug.

Keywords: Quercetindihydrate, mustard agent poisoning, mucoadhesive microspheres, polymers concentration, plasticizer concentration.