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Abstract

PREPARATION AND EVALUATION OF QUERCETIN MICROSPHERE AS ANTIDOTES OF SULPHUR MUSTARD TO OVERCOME THE POOR BIOAVAILABILITY AND FREQUENT DOSE ADMINISTRATION OF THE DRUG

Ram Chandra Jat*, Dr. Suman Jain, Kanika Arora

ABSTRACT

In an effort to augment the prophylactic action of Quercetindihydrate 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 Quercetindihydrate, 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 polymers concentration and stirring speed were used. Entrapment efficiency is observed more with higher speed of stirring. 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, decreasing with increasing stirring speed.The FT-IR spectra of the pure drug and formulation F1 indicated that characteristics peaks of Quercetin were not altered.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). All formulations had excellent flow property. Percentage mucoadhesion was found in the range of 62.5 ± 1.81 (batch-F1) to 74.9 ± 1.13 (batch-F4). 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 showed 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 was 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: Microspheres,Quercetindihydrate, adhesive polymer (ethyl cellulose), colon specific polymer (Eutragit S 100), stirring speed.


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