Abstract

Objective: Medroxyprogesterone Acetate (MPA) using a transdermal drug delivery system for contraception by passive diffusion is limited by the skin barrier properties. Penetration enhancers such as olive oil (fatty acid permeation enhancer) and DMSO (chemical enhancer) can be used. The objective of this study was to overcome MPA penetration problem by using olive oil and DMSO.
 Methods: An in vitro penetration study using the Franz diffusion cells was performed. The first penetration study used MPA in olive oil (O) and MPA in coconut oil (C) with the concentration 100 μg/ml to each sample and MPA suspension as a control with the same concentration. The second study used MPA in olive oil with the concentration 200.0 μg/ml (A), MPA in olive oil with 0.5% DMSO with the concentration 200.0 μg/ml (B), and MPA in olive oil with 1% DMSO with the concentration 200 μg/ml (C).
 Results: MPA penetration test for olive oil+0.5% DMSO had flux value 4.24±0.074 μg/cm2. hr and it was not significantly different (t-test, P>0.05) with olive oil+1% DMSO. While the MPA penetration test in only Olive oil had flux value 0.90±0.0087 μg/cm2. hr.
 Conclusion: This research concluded that olive oil and 0.5% DMSO could improve the penetration of MPA into skin membrane by 4.5 times more than olive oil alone.

Highlights

  • Medroxyprogesterone acetate is a synthetic progestin which is used as long-acting hormonal contraceptive and anabolic steroid

  • The materials that were used in this study were: medroxyprogesterone acetate (Sigma Aldrich), olive oil, virgin coconut oil, hydroxypropyl methylcellulose, phosphate buffer pH 7.4, dimethylsulfoxide were from Merck (Darmstadt, German), methanol, double-distilled water, formic acid and acetonitrile were of an analytical grade that purchased from Jakarta, Indonesia

  • Medroxyprogesterone Acetate (MPA) penetration test was conducted in coconut oil and olive oil as natural penetration enhancer with MPA suspension as control and amount of penetrated as shown in fig. 2

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Summary

Introduction

Medroxyprogesterone acetate is a synthetic progestin which is used as long-acting hormonal contraceptive and anabolic steroid. Using a transdermal drug delivery system for contraception presents some clinical advantages over conventional oral contraception [2]. The once-weekly administration is more convenient for women than oncedaily administration with oral contraception and should improve efficacy by decreasing the degree to which it is dependent on user compliance [3]. Transdermal delivery of contraceptive hormones eliminates variability in gastrointestinal (GI) absorption, due to factors such as stomach pH, stomach emptying rate, GI motility, and GI transit time. The drug is delivered directly into the systemic circulation, avoiding the hepatic first-pass metabolism experienced with oral contraception and maintaining constant drug concentrations in the circulation by eliminating peaks and troughs in serum concentrations climatic that occur with oral administration [4]

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