Comparative in virto diffusion study for Lovastatin transdermal delivery system.

摘要

The major risk factor for the development of coronary heart disease is a high concentration of plasma cholesterol, especially low density lipoprotein (LDL) cholesterol. The single biggest cause of heart and blood vessels disease is atherosclerosis, on the hardening of arteries. Atherosclerosis is silent and fatty infiltration of coronary arteries ultimately leading to coronary heart disease (CHD). Lovastatin is one of the ideal medications which is used in the therapeutic treatment of this diseases.;The present study determines the transdermal delivery of Lovastatin through cellulose membranes and human cadaver skin, and to evaluate the effect of enhancers.;In vitro release studies were carried out by Franz diffusion cells at 37°C. Different concentrations of the Lovastatin solution (0.025%, 0.05%, and 0.1%) were formulated with Methocel gel at four different concentrations (0.125%, 0.25%, 0.5%, and 0.75%). Four different enhancers were used (Caprylic acid, Capric acid, Lauric acid, Sodium Lauryl Sulfate) at 0.1% concentration. The donor compartments contain either the Lovastatin solution or gel. Receiver compartment contain a 1:1 ratio of ethanol and water. The cellulose membrane and human cadaver skin were used to study diffusion of Lovastatin. Samples were taken up to 48 hours for cellulose membrane and 150 hours for cadaver skin. Samples were analyzed using UV spectrophotometer at 240nm.;The obtained data showed that the drug diffusion was better from Methocell gel (0.25%) compared to other concentrations (0.125%, 0.5%, and 0.75%) of the gel. Amount released without enhancers from Lovastatin solution through cellulose membrane were found to be 2.41% and from Methocel gel through cellulose membrane is 1.15%. The drug release through human cadaver skin using (0.25%) gel is 0.49%. Caprylic acid, Capric acid, Lauric acid did not give significant increase in release through cellulose membrane as enhancer. Adding Sodium lauryl sulfate as an enhancer increased the release of drug. Release from gel through cellulose membrane was found to be 1.62% and through cadaver skin was found to be 0.72% respectively.;Doubling the enhancer concentration increased the release through cellulose membrane (1.99%) and human cadaver skin (0.96%) respectively. This study demonstrates that Lovastatin is a good candidate for making gel in transdermal drug delivery system and the amount of Lovastatin released is increasing by using the Sodium lauryl sulfate.