Journal of Chemical and Pharmaceutical Research (ISSN : 0975-7384)

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Original Articles: 2014 Vol: 6 Issue: 6

Enhancement of solubility and dissolution of lercanidipine by liquisolid technique

Abstract

Lercanidipine is a BCS Class II drug having poor aqueous solubility and good permeability through the plasma membranes. Absolute bioavailability of the drug is only 10% and the main reason attributed for such a low bioavailability is poor aqueous solubility of the drug. Different methods have been tried to enhance the solubility of the drug but most of them have not been found satisfactory due to either less enhancement of solubility or limited industrial application. Liquisolid technology is one of the most promising techniques to enhance the aqueous solubility. In the present study the drug was screened with three non-volatile liquid vehicles namely PEG 400, Polysorbate 80 (Tween 80) and Propylene glycol (PG). The best result was obtained with PEG 400 because of the highest solubility of the drug in PEG 400 amongst the non-volatile liquid vehicles. Hence optimization of the formula was done taking PEG 400 to achieve 100% drug release. Avicel PH 102 and Aerosil 200 were used as carrier and coating material correspondingly. The In-vitro dissolution test was carried out with USP Type II (paddle) apparatus taking phosphate buffer (pH 6.8) as dissolution medium. The compatibility of the formulation was checked by FT-IR study. The improved wetting property and increased surface area (molecular dispersion) are believed mechanisms for enhancement of the solubility of lercanidipine. The method of production of liquisolid compact is very easy and there is no use of highly developed equipment, which makes this technology industrially applicable

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