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聚乳酸-乙醇酸共聚物(PLGA)和卵磷脂/壳聚糖纳米粒用于倍他米松戊酸酯经皮靶向传递的比较。

Comparison of PLGA and lecithin/chitosan nanoparticles for dermal targeting of betamethasone valerate.

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Ege University, Bornova, Izmir-Turkey.

出版信息

J Drug Target. 2013 Jul;21(6):542-50. doi: 10.3109/1061186X.2013.769106. Epub 2013 Feb 8.

Abstract

Poly(lactide-co-glycolide) (PLGA) and lecithin/chitosan (LC) nanoparticles were prepared to evaluate the difference in the behavior upon administration on skin, for steroidal treatment. For this purpose, betamethasone-17-valerate (BMV)-loaded nanoparticles with a narrow size distribution and high entrapment efficiency were prepared. Permeation studies showed that both polymeric nanoparticles enhanced the amount of BMV in epidermis, which is the target site of topical steroidal treatment, when compared with commercial formulation. 1.58-Fold increase was determined in the epidermis concentration of BMV by LC nanoparticles with respect to PLGA nanoparticles. Nanoparticles were diluted in chitosan gel (10%, w/w) to prepare suitable formulation for topical application. Accumulation from both gel formulations were found significantly higher than commercial formulation in skin layers (p < 0.05). In addition, pharmacodynamic responses were also investigated as anti-inflammatory and skin-blanching parameters. Both formulations significantly improved these parameters although they contained 10 times less amount of BMV than commercial cream. Moreover, TEWL measurement exhibited no barrier function changes upon the application of nanoparticles on skin. Overall, both nanoparticles improved the localization of BMV within skin layers; but when compared with PLGA nanoparticles, the LC nanoparticles could be classified as a better candidate for topical delivery vehicle in the treatment of various dermatological inflammatory diseases.

摘要

聚(丙交酯-乙交酯)(PLGA)和卵磷脂/壳聚糖(LC)纳米粒被制备来评估其在皮肤上给药行为的差异,用于甾体治疗。为此,制备了具有窄粒径分布和高包封效率的载有倍他米松-17-戊酸酯(BMV)的纳米粒。渗透研究表明,与商业制剂相比,两种聚合物纳米粒都增加了表皮中 BMV 的量,表皮是局部皮质类固醇治疗的靶位。LC 纳米粒使表皮中 BMV 的浓度增加了 1.58 倍。将纳米粒稀释于壳聚糖凝胶(10%,w/w)中,以制备适合局部应用的制剂。两种凝胶制剂在皮肤层中的累积均明显高于商业制剂(p<0.05)。此外,还研究了药效反应作为抗炎和皮肤变白参数。尽管这两种制剂中 BMV 的含量比商业乳膏少 10 倍,但它们都显著改善了这些参数。此外,TEWL 测量表明纳米粒应用于皮肤不会改变屏障功能。总的来说,这两种纳米粒都改善了 BMV 在皮肤层中的定位;但与 PLGA 纳米粒相比,LC 纳米粒可被归类为治疗各种皮肤炎症性疾病的更好的局部递药载体。

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