Particle size of liposomes influences dermal delivery of substances into skin
Particle size of liposomes influences dermal delivery of substances into skin
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DOI：
10.1016/s0378-5173(03)00183-2
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发表时间：
2003-06-04
影响因子：
5.8
通讯作者：
Fahr, A
中科院分区：
文献类型：
--
作者：
Verma, DD;Verma, S;Fahr, A
在本研究中，研究了囊泡大小对两种荧光标记物质进入人体皮肤的影响。在测量中，将亲水性荧光化合物[羧基荧光素(CF)]或亲脂性高氯酸盐([1，1‘-dioctadecyl-3，3，3’，3‘-tertramethylindocarbo-cyanine)[DII]包裹到囊泡中。通过具有不同大小的孔的聚碳酸酯薄膜过滤器挤压囊泡，制备脂质体制剂。利用Franz扩散池和标准化皮肤剥离技术进行了人体腹部皮肤的体外透皮实验，试图找到脂质体局部给药的最佳尺寸。激光共聚焦扫描显微镜(CLSM)观察脂质体对DII透皮能力的影响。在直径为71 nm的较小脂质体中，DII在皮肤中的荧光最大。与直径为120 nm的脂质体相比，直径为120 nm的脂质体具有更强的透皮吸收作用。激光共聚焦扫描显微镜的研究结果证实了这一点，表明脂质体的透过率与脂质体的大小成反比。(C)2003 Elsevier Science B.V.保留所有权利。
In the present study, the influence of vesicle size on the penetration of two fluorescently labeled substances into the human skin was investigated. For the measurements either a hydrophilic fluorescent compound [carboxyfluorescein (CF)] or a lipophilic one [1,1'-dioctadecyl-3,3,3',3'-tertramethylindocarbo-cyanine perchlorate (DiI)] were encapsulated into vesicles. Liposomal formulations were prepared by extruding the vesicles through polycarbonate membrane filters with pores of different sizes. In vitro penetration studies into human abdominal skin were performed by using the Franz diffusion cell and a standardized skin stripping technique in attempt to find an optimum size for topical drug delivery by liposomes. Confocal laser scanning microscopy (CLSM) was used to visualize the effect of penetration ability of liposomal DiI. The maximum DiI fluorescence in the skin was observed with smaller liposomes of 71 nm diameter. The liposomes with a size of 120 nm diameter showed statistically enhanced penetration of CF into the skin as compared to larger ones. The results indicated that the CF penetration was inversely related to the size of the liposomes, which was confirmed by the data of the confocal laser scanning microscopy studies. (C) 2003 Elsevier Science B.V. All rights reserved.