Xiang Li1, Renyu Zhang1, Rongcai Liang2, Wei Liu1, Chenhui Wang1, Zhengxing Su1, Fengying Sun3, Youxin Li4. 1. School of Life Science, Jilin University, 2699 Qianjin Street, Changchun, China. 2. School of Life Science, Jilin University, 2699 Qianjin Street, Changchun, China; School of Pharmacy, Yantai University, No. 30 Qingquan Road, Yantai, China. 3. School of Life Science, Jilin University, 2699 Qianjin Street, Changchun, China. Electronic address: sunfengying@jlu.edu.cn. 4. School of Life Science, Jilin University, 2699 Qianjin Street, Changchun, China; School of Pharmacy, Yantai University, No. 30 Qingquan Road, Yantai, China. Electronic address: liyouxin@jlu.edu.cn.
Abstract
OBJECTIVE: The aim of this study was to develop a film-forming gel formulation of rotigotine with hydroxypropyl cellulose (HPC) and Carbomer 934. To optimize this formulation, we applied the Response Surface Analysis technique and evaluated the gel's pharmacokinetic properties. METHODS: The factors chosen for factorial design were the concentration of rotigotine, the proportion of HPC and Carbomer 934, and the concentration of ST-Elastomer 10. Each factor was varied over three levels: low, medium and high. The gel formulation was evaluated and optimized according to its accumulated permeation rate (Flux) through Franz-type diffusion. A pharmacokinetic study of rotigotine gel was performed with rabbits. RESULTS: The Flux of the optimized formulation reached the maximum (199.17 μg/cm(2)), which was 3% rotigotine and 7% ST-Elastomer 10 with optimal composition of HPC: Carbomer 934 (5:1). The bioavailability of the optimized formulation compared with intravenous administration was approximately 20%. CONCLUSION: A film-forming gel of rotigotine was successfully developed using the response surface analysis technique. The results of this study may be helpful in finding an optimum formulation for transdermal delivery of a drug. The product may improve patients' compliance and provide better efficacy.
OBJECTIVE: The aim of this study was to develop a film-forming gel formulation of rotigotine with hydroxypropyl cellulose (HPC) and Carbomer 934. To optimize this formulation, we applied the Response Surface Analysis technique and evaluated the gel's pharmacokinetic properties. METHODS: The factors chosen for factorial design were the concentration of rotigotine, the proportion of HPC and Carbomer 934, and the concentration of ST-Elastomer 10. Each factor was varied over three levels: low, medium and high. The gel formulation was evaluated and optimized according to its accumulated permeation rate (Flux) through Franz-type diffusion. A pharmacokinetic study of rotigotine gel was performed with rabbits. RESULTS: The Flux of the optimized formulation reached the maximum (199.17 μg/cm(2)), which was 3% rotigotine and 7% ST-Elastomer 10 with optimal composition of HPC: Carbomer 934 (5:1). The bioavailability of the optimized formulation compared with intravenous administration was approximately 20%. CONCLUSION: A film-forming gel of rotigotine was successfully developed using the response surface analysis technique. The results of this study may be helpful in finding an optimum formulation for transdermal delivery of a drug. The product may improve patients' compliance and provide better efficacy.