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Abstract

FORMULATION, DEVELOPMENT AND EVALUATION OF NOVEL NANOEMULSION FOR TRANSDERMAL DRUG DELIVERY OF NIMODIPINE

Sheela A. Yadav* and D. S. Rathore

ABSTRACT

The objective of the present study was to develop and optimize the nanoemulsion based transdermal drug delivery system for nimodipine, a poorly water soluble and low bioavailability drug. Characterization of the formulation was done by physicochemical studies. The pseudoternary phase diagrams were developed for various nanoemulsion formulations composed of (Triacetin+IPM), Tween 80 and PEG-400. The nanoemulsion was optimized by using in vitro drug permeation studies through rat skin. The pharmacokinetic evaluation and skin irritation test were carried out in healthy rats. Blood pressure reducing activity of the system was studied in hypertensive rats. The in vitro permeation rate across the rat skin varied with the varying drug: excipient ratio in the nanoemulsion formulation. The optimized formulation showed the maximum flux rate of 212.1μg/cm2/hr was chosen for the further studies. The nanoemulsion formulation exhibited negligible skin irritation. The antihypertensive response was gradual but sustained for prolonged period of time with the transdermal system. The relative bioavailability of nanoemulsion gel was calculated to be 230% in comparison to the oral suspension. The results suggested that this novel nanoemulsion transdermal delivery system exhibited better control of hypertension than conventional oral route.

Keywords: Nimodipine, nanoemulsion, pseudoternary phase diagrams, gel, transdermal delivery, anti-hypertensive.


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