目的 比较不同比例的大豆磷脂(soy phospholipid,SPC)和氢化大豆磷脂(hydrogenate soy phospholipid,HSPC)组成的复合磷脂脂质体对荧光修饰的羟丙基-β-环糊精(hydroxypropyl-β-cyclodextrin,HP-β-CD)的皮肤递送效果,优选出具有最佳皮内滞留的磷脂组成。方法 将荧光探针异硫氰酸荧光素(fluorescin isothiocyanate,FITC)与HP-β-CD结合,制备得荧光修饰环糊精FITC-HP-β-CD,包封于不同磷脂比例的复合磷脂脂质体内,通过离体皮肤递送实验,考察10 h接收液中环糊精的透过量以及环糊精的皮内滞留量。结果 环糊精的透过量排序为SPC > S/H(3:1)> S/H(1:1)> S/H(1:3)>HSPC>游离FITC-HP-β-CD,而环糊精的皮内滞留量排序则是S/H(1:1)> S/H(1:3)> HSPC > S/H(3:1)> SPC >游离FITC-HP-β-CD。结论 用SPC制备脂质体比HSPC更有利于促进FITC-HP-β-CD透过皮肤,但HSPC的加入会增加FITC-HP-β-CD在皮内的滞留,而SPC与HSPC的质量比为1:1时制备的脂质体对荧光修饰环糊精具有较优的皮肤递送效果,其中皮内滞留效果最优。
Abstract
OBJECTIVE To compare the intradermal delivery effects of composite phospholipid liposomes composed of different proportions of soy phospholipids (SPC) and hydrogenated soy phospholipids (HSPC) on the fluorescent modified hydroxypropyl-β-cyclodextrin(HP-β-CD), and to optimize the phospholipid composition with the best skin retention. METHODS The fluorescent probe, fluorescein isothiocyanate (FITC), was combined with HP-β-CD to prepare fluorescent modified cyclodextrin FITC-HP-β-CD. FITC-HP-β-CD was encapsulated in different composite phospholipid liposomes. The amount of the permeation in the receiving solution and skin retention of the cyclodextrin after 10 h were determined in the in vitro intradermal delivery experiment. RESULTS The order of cyclodextrin permeation of liposomes in the receiving solution was SPC > S/H (3:1) > S/H (1:1) > S/H (1:3) > HSPC >FITC-HP-β-CD,while the order of cyclodextrin intradermal retention was S/H (1:1) > S/H (1:3) > HSPC > S/H (3:1) > SPC > FITC-HP-β-CD. CONCLUSION Using SPC to prepare liposomes is more beneficial to promote the permeation of FITC-HP-β-CD into the skin than HSPC,but the addition of HSPC can increase the skin retention of FITC-HP-β-CD. The S/H(1:1) liposomes have the better intradermal delivery effect on the fluorescent modified cyclodextrin, of which the skin retention effect is the best.
关键词
复合磷脂 /
脂质体 /
羟丙基-β-环糊精 /
皮内滞留
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Key words
composite phospholipid /
liposome /
hydroxypropyl-β-cyclodextrin /
skin retention
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中图分类号：
R944
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