Novel carbopol-based transfersomal gel of 5-fluorouracil for skin cancer treatment: in vitro characterization and in vivo study

被引:103
作者
Khan, Mohammed Ashif [1 ]
Pandit, Jayamanti [1 ]
Sultana, Yasmin [1 ]
Sultana, Sarwat [2 ]
Ali, Asgar [1 ]
Aqil, Mohammed [1 ]
Chauhan, Meenakshi [3 ]
机构
[1] Jamia Hamdard, Fac Pharm, Dept Pharmaceut, New Delhi 110062, India
[2] Jamia Hamdard, Fac Sci, Dept Med Elementol & Toxicol, New Delhi 110062, India
[3] Delhi Inst Pharmaceut Sci & Res, Dept Pharmaceut, New Delhi, India
关键词
5-fluorouracil; carbopol; skin cancer; topical delivery; transfersomal gel; TRANSDERMAL DELIVERY; DEFORMABLE LIPOSOMES; BIOLOGICAL-ACTIVITY; FORMULATION DESIGN; VESICLES; OPTIMIZATION; CELLS;
D O I
10.3109/10717544.2014.902146
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
5-fluorouracil (5-Fu) is an antineoplastic drug, topically used for the treatment of actinic keratosis and nonmelanoma skin cancer. It shows poor percutaneous permeation through the conventionally applicable creams and thus inefficient for the treatment of deep-seated skin cancer. In the present article, transfersomal gel containing 5-Fu was investigated for the treatment of skin cancer. Different formulation of tranfersomes was prepared using Tween-80 and Span-80 as edge activators. The vesicles were characterized for particle size, shape, entrapment efficiency, deformability and in vitro skin permeation. Optimized formulation was incorporated into 1% carbopol 940 gel and evaluated for efficacy in the treatment of skin cancer. 5-Fu-loaded transfersomes (11-2) has the size of 266.9 +/- 2.04 nm with 69.2 +/- 0.98% entrapment efficiency and highest deformability index of 27.8 +/- 1.08. Formulation 11-2 showed maximum skin deposition (81.3%) and comparable transdermal flux of 21.46 mu g/cm(2) h. The TT-2-loaded gel showed better skin penetration and skin deposition of the drug than the marketed formulation. Composition of the transfersomal gel has been proved nonirritant to the skin. We concluded that the developed 5-Fu-loaded transfersomal gel improves the skin absorption of 5-Fu and provide a better treatment for skin cancer.
引用
收藏
页码:795 / 802
页数:8
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