Preparation and the in Vitro Evaluation of Nanoemulsion System for the Transdermal Delivery of Granisetron Hydrochloride

被引:35
|
作者
Zheng, Wen-wu [2 ]
Zhao, Ling [1 ]
Wei, Yu-meng [1 ]
Ye, Yun [1 ]
Xiao, Shun-han [1 ]
机构
[1] Luzhou Med Coll, Sch Pharm, Dept Pharmaceut, Luzhou 646000, Sichuan Prov, Peoples R China
[2] Peoples Hosp Luzhou, Dept Cardiol, Luzhou 646000, Sichuan Prov, Peoples R China
关键词
granisetron hydrochloride; nanoemulsion; transdermal drug delivery; isopropyl myristate; N-methyl pyrrolidone; skin permeation; CANCER-CHEMOTHERAPY; MICROEMULSION; ENHANCEMENT; PERMEATION; NAUSEA; PERMEABILITY; FORMULATION; DICLOFENAC;
D O I
10.1248/cpb.58.1015
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The objective of this study was to develop and evaluate nanoemulsion system for transdermal delivery of granisetron hydrochloride. Pseudo-ternary phase diagram was constructed to ascertain the concentration range of components of nanoemulsion composed of isopropyl myristate (IPM) as an oil phase, tween 85 as surfactant, ethanol as cosurfactant, water as aqueous phase. The effects of the content of IPM as an oil phase and it-methyl pyrrolidone (NMP) as transdermal enhancer on rat skin permeation of granisetron hydrochloride nanoemulsion were studied in vitro. The results showed that the mean particle size of nanoemulsion ranged from 50.4 +/- 1.5 to 82.4 +/- 0.9 nm with homogeneous size distribution. The resulted optimum formulation composed of 2.5% granisetron hydrochloride, 4% IPM, 40% tween 85/ethanol (1:1) and 10% NMP showed that the skin permeation rate was the highest (85.39 +/- 2.90 mu g/cm(2)/h) and enhancement of drug permeability was 4.1-folde for transdermal delivery of granisetron hydrochloridein comparison with the control group (20% of tween 85 and 20% of ethanol micelle solution containing 2.5% of granisetron hydrochloride without IPM), and cumulative permeation amount was the highest (891.8 +/- 2.86 mu g/cm(2)) with the shortest lag time (0.11 +/- 0.02 h) and was stable for at least 12 months. Therefore, the nanoemulsion system developed in this study offers a promising vehicle for the transdermal delivery system of granisetron hydrochloride, which may be as effective as oral or intravenous dosage forms and avoid some difficulties associated with these dosage forms.
引用
收藏
页码:1015 / 1019
页数:5
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