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氟康唑脂质体凝胶的制备及体外透皮实验

赵珊珊, 杜青*, 曹德英   

  1. 河北医科大学药学院 药剂教研室, 石家庄 050017
  • 收稿日期:2006-11-12 修回日期:2007-05-10 出版日期:2007-06-15 发布日期:2007-06-15
  • 通讯作者: 杜青*

Preparation of liposomal fluconazole gel and in vitro transdermal delivery

Shan-Shan Zhao, Qing Du*, De-Ying Cao   

  1. Department of Pharmaceutics, School of Pharmacy, Hebei Medical University, Shijiazhuang 050017, China
  • Received:2006-11-12 Revised:2007-05-10 Online:2007-06-15 Published:2007-06-15
  • Contact: Qing Du*

摘要: 目的 制备氟康唑脂质体凝胶, 并研究其性质。方法 以薄膜分散法制备氟康唑脂质体, 透射电镜观察脂质体的形态, 粒度分布仪测定粒径, 透皮吸收扩散池测定脂质体凝胶的透皮吸收。结果 氟康唑脂质体的包封率为47.68%。脂质体粒径均匀, 平均粒径为250 ± 8 nm。氟康唑脂质体凝胶的累积透过量(25.27%)低于非脂质体凝胶(36.72%), 而脂质体凝胶的药物皮内滞留量(162 ± 15 μg·cm–2)大于非脂质体凝胶(48 ± 6 μg·cm–2)结论 氟康唑脂质体凝胶剂可显著提高药物的皮内滞留量, 有望成为氟康唑的一种外用新剂型。

关键词: 氟康唑, 氟康唑, 氟康唑, 脂质体凝胶, 脂质体凝胶, 脂质体凝胶, 经皮渗透, 经皮渗透, 经皮渗透, 体外, 体外, 体外

Abstract: Aim Liposomal fluconazole gel was prepared and its properties were studied. Methods The fluconazole liposomes were prepared by film dispersion method. Their shapes and sizes were observed by transmission electronic microscope and particle size analyzer, respectively. The skin permeation of liposomal gel was studied on rat skin by permeation cell. Results The entrapment efficiency of fluconazole liposomes was 47.68%. The fluconazole liposomes were oval or round in shape, and their average diameter was 250 ± 8 nm. The accumulative skin permeation of liposomal fluconazole gel (25.27%) was lower than that of non-liposomal fluconazole gel (36.72%), but fluconazole retained in rat skin of liposomal gel (162 ± 15 μg·cm–2) was higher than that of nonliposomal gel (48 ± 6 μg·cm–2). Conclusion Liposomal fluconazole gel can significantly increase the deposited amounts of fluconazole in rat skin and it may be beneficial for topical use.

Key words: Fluconazole, Fluconazole, Liposomal gel, Liposomal gel, Transdermal delivery, Transdermal delivery, in vitro, in vitro, ,

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Supporting: *Corresponding author. Fax: 86-311-86266050