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脂质体对萘普生透皮渗透的影响——体外研究

The impact of liposomes on transdermal permeation of naproxen--in vitro studies.

作者信息

Szura Dorota, Ozimek Łukasz, Przybyło Magdalena, Karłowicz-Bodalska Katarzyna, Jaźwińska-Tarnawska Ewa, Wiela-Hojeńska Anna, Han Stanisław

出版信息

Acta Pol Pharm. 2014 Jan-Feb;71(1):145-51.

PMID:24779203
Abstract

The possibility of applying liposomes as a topical drug delivery system is still a matter of intensive research. The purpose of this study was to determine the suitability of liposomes as carriers of naproxen and to prove their impact on the effectiveness of transdermal permeation of an active substance. The study was conducted with the use of Franz Diffusion Cell System by comparing the efficacy of a preparation containing 20% of phosphatidylcholine (PC) and 10% of naproxen with reference preparations, i.e., a formulation containing 10% of naproxen without PC and the commercial product Naproxen 10%, gel. The largest transdermal penetration flux of naproxen and the highest efficacy of naproxen permeation were obtained for the formulation containing 10% of naproxen and 20% of PC. The study of the influence of liposomes size and topology on the transdermal diffusion of naproxen (large unilamellar vesicle, LUV, multilamellar vesicle, MLV) showed that there was no statistically significant difference in the flux or total amounts of transdermally diffused naproxen between compared formulations. In conclusion, liposomes present in a formulation double the efficacy of the transdermal permeation of naproxen in vitro compared to reference preparations containing no carriers. Better permeation effect of a formulation was not related to the liposome type (LUV or MLV).

摘要

将脂质体用作局部给药系统的可能性仍是深入研究的课题。本研究的目的是确定脂质体作为萘普生载体的适用性,并证明其对活性物质透皮渗透效果的影响。该研究使用Franz扩散池系统进行,通过比较含有20%磷脂酰胆碱(PC)和10%萘普生的制剂与参比制剂的效果,即含有10%萘普生但不含PC的制剂以及市售产品萘普生10%凝胶。对于含有10%萘普生和20%PC的制剂,获得了最大的萘普生透皮渗透通量和最高的萘普生渗透效果。关于脂质体大小和拓扑结构对萘普生透皮扩散的影响的研究(大单层囊泡,LUV;多层囊泡,MLV)表明,在所比较的制剂之间,萘普生透皮扩散的通量或总量没有统计学上的显著差异。总之,与不含载体的参比制剂相比,制剂中存在的脂质体使萘普生体外透皮渗透效果提高了一倍。制剂更好的渗透效果与脂质体类型(LUV或MLV)无关。

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