EFFECT OF PIPER NIGRUM ON IN-VITRO RELEASE OF RIFAMPICIN MICROSPHERES
Abstract
Tuberculosis therapy remains a challenge even today, mainly due to the problems of bacterial resistance, side effects and low patient compliance, associated with anti-tubercular drugs. A bioenhancer is an agent capable of enhancing bioavailability and bioefficacy of a particular drug with which it is combined, without any typical pharmacological activity of its own at the dose used. Microspheres are one of the multiparticulate drug delivery systems prepared to obtain prolonged drug delivery, to improve its bioavailability or stability and to target drug to specific sites. Rifampicin is an important component of fixed dose combination used in first line therapy of tuberculosis. In the present study, we attempted an innovative approach to overcome the above-mentioned problems of tuberculosis therapy by combining both these approaches of microspheres and bioenhancers. Small amount of herbal extract of Piper nigrum were incorporated as a bioenhancer in variable amount for each dose of rifampicin.
The drug loading efficiency and in-vitro release behavior of loaded microspheres were found to be satisfactory. Prolonged release of the drug from the microspheres was demonstrated in a simulated intestinal fluid. In-vitro release of rifampicin from the microspheres containing variable fractions of bioenhancer showed significant increase in release profile i.e. 80.24 and 86.16percent in formulation containing bioenhancer against 44.54percent for the formulation without bioenhancer prepared by complex coacervation method.Â
Keywords: Tuberculosis, Microspheres, Drug release, Bioenhancer, Rifampicin, Piper nigrum
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