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新型基于卡波姆的 5-氟尿嘧啶传递体凝胶用于皮肤癌治疗:体外特性研究和体内研究。

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

机构信息

a Department of Pharmaceutics , Faculty of Pharmacy .

b Department of Medical Elementology and Toxicology, Faculty of Science , Jamia Hamdard , and.

出版信息

Drug Deliv. 2015;22(6):795-802. doi: 10.3109/10717544.2014.902146. Epub 2014 Apr 15.

Abstract

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 (TT-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 TT-2 showed maximum skin deposition (81.3%) and comparable transdermal flux of 21.46 µg/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.

摘要

5-氟尿嘧啶(5-Fu)是一种抗肿瘤药物,局部用于治疗光化性角化病和非黑素瘤皮肤癌。它在传统应用的乳膏中表现出较差的经皮渗透,因此对于深部皮肤癌的治疗效果不佳。在本文中,研究了含有 5-Fu 的传递体凝胶用于治疗皮肤癌。使用吐温 80 和司盘 80 作为边缘活性剂制备了不同配方的传递体。对囊泡进行了粒径、形态、包封效率、变形性和体外皮肤渗透的表征。将优化的配方掺入 1%卡波姆 940 凝胶中,并评估其在治疗皮肤癌方面的疗效。载有 5-Fu 的传递体(TT-2)的粒径为 266.9 ± 2.04nm,包封效率为 69.2 ± 0.98%,变形性指数最高为 27.8 ± 1.08。配方 TT-2 显示出最大的皮肤沉积(81.3%)和可比较的透皮通量 21.46μg/cm(2)h。与市售制剂相比,载有 TT-2 的凝胶显示出更好的药物皮肤渗透和皮肤沉积。传递体凝胶的组成被证明对皮肤无刺激性。我们得出结论,开发的载有 5-Fu 的传递体凝胶提高了 5-Fu 的皮肤吸收,并为皮肤癌提供了更好的治疗。

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