Formulation of cladribine emulgel for topical delivery and Evaluation of its transdermal absorption

Abstract

Introduction: Skin is one of the most important tissues of the body that can be affected by autoimmune diseases. In comparison to other drug delivery methods, topical drug delivery method has many advantages which may be mentioned as the possibility of using higher drug concentration on the skin, the possibility of prolonged presence of drug on the skin and consequently reduction of the usage frequency, as well as, the systematic circulation of drug which reduces possible side effects of the drug. Cladribine is a cytotoxic drug and one of the purine analogues which has immunosuppressive effects.

The Objectives: The main objective of this study is to make comparison between percutaneous absorption of Cladribine with emulgel formulation and simple gel formulation.

Methods: At first, formulations of gel and emulgel were produced by Carbopol 934, as gelling agent, for different ratios of drug components. Then, the percutaneous absorption of selected formulations through rat skin was examined by Franz diffusion cell device and amount of drug concentration in samples were analyzed by HPLC device in the wavelength of 365 nm.

Results: The total amount of percutaneous absorption of drug for emulgel formulation in 30, 60 and 240 minutes was 74.6%, 64.2% and 61% higher than that of simple gel formulation, respectively. In addition, the Emulgel flux was about 2.5 times that of simple gel.

Discussion and Conclusion: Emulgel formulation significantly enhances percutaneous absorption of Cladribine compared to simple gel formulation. Hence, it goes without saying that emulgel based formulations would be more suitable and reasonable for use in drugs with topical delivery of Cladribine.