Abstract

The crystallization of mefenamic acid in transdermal patch is a major problem that makes the patch unstable and decreases the drug release. The additive was used to inhibit crystallization of a mefenamic acid. Among the different types of additives, polyvinylpyrrolidone (PVP) K30 and PVP K90 were studied and found to be highly effective in inhibiting the crystallization of the drug. The PVP presented as a solubilizer agent for mefenamic acid in matrix patches at the different ratio between drug : PVP, 1 : 2 and 1 : 2.5 for using PVP K30 and 1 : 1.5 and 1 : 2 for using PVP K90. The characterizations showed the homogeneous patches without the crystal form of the mefenamic acid in matrix patches. The release profiles of the mefenamic acid from the patches were investigated by Franz diffusion cells. Over the first 1 h, the release behavior of mefenamic acid from the patches obviously increased when PVP was used as a crystallization inhibitor. However, the ratio between drug : PVP K90 at 1 : 2 was found to be the most effective in increasing the drug release from patch. Thus, the PVP could be used as a crystallization inhibitor for mefenamic acid in matrix patches which will increase the drug release.

Highlights

  • Transdermal patches are an effective alternative route to deliver a small drug molecules through the skin into the systemic blood circulation and to the target organ [1, 2]

  • We prepared the transdermal patches for mefenamic acid using ethyl cellulose and eudragit as a matrix film

  • The mefenamic acid patches were prepared by using ethyl cellulose as a matrix film and using the PVP as a crystallization inhibitor

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Summary

Introduction

Transdermal patches are an effective alternative route to deliver a small drug molecules through the skin into the systemic blood circulation and to the target organ [1, 2]. It will be necessary for the delivered drug to reach its target sites and maintain a concentration at the target in therapeutic level [3, 4]. During this transport process, the drug can undergo severe biochemical degradations and the end products may ineffective and even toxic. Many classes of polymers such as cellulose derivatives, polyvinyl alcohol, carbopol, chitosan, and polyacrylates, have been used for transdermal patches [7, 8]

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