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载槲皮素纳米结构脂质载体的透皮给药系统的研制。

Development of a quercetin-loaded nanostructured lipid carrier formulation for topical delivery.

机构信息

Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan 250012, China.

出版信息

Int J Pharm. 2012 Jul 1;430(1-2):292-8. doi: 10.1016/j.ijpharm.2012.03.042. Epub 2012 Apr 1.

Abstract

The main objective of this study was to evaluate the potential of quercetin-loaded nanostructured lipid carriers (QT-NLCs) as a topical delivery system. QT-NLCs were prepared by the method of emulsion evaporation-solidification at low temperature. The average entrapment efficiency and drug loading of the optimized QT-NLCs were 89.95 ± 0.16% and 3.05 ± 0.01%, respectively. Under the transmission electron microscope, the nanoparticles were spherically shaped. The average particle size was 215.2 nm, the zeta potential was -20.10 ± 1.22 mV and pH value of QT-NLCs system was 4.65. Topical delivery of QT in the form of NLCs was investigated in vitro and in vivo. The results showed that QT-NLCs could promote the permeation of QT, increase the amount of QT retention in epidermis and dermis, and enhance the effect of anti-oxidation and anti-inflammation exerted by QT. Then the mechanism of NLCs for facilitating drug penetration was further investigated through histological sections. In conclusion, NLCs could be a promising vehicle for topical delivery of QT.

摘要

本研究的主要目的是评估载有槲皮素的纳米结构脂质载体 (QT-NLCs) 作为局部递药系统的潜力。QT-NLCs 采用低温乳化蒸发固化法制备。优化后的 QT-NLCs 的平均包封效率和载药量分别为 89.95±0.16%和 3.05±0.01%。在透射电子显微镜下,纳米颗粒呈球形。平均粒径为 215.2nm,Zeta 电位为-20.10±1.22mV,QT-NLCs 体系的 pH 值为 4.65。以 NLCs 的形式进行了 QT 的体外和体内局部递药研究。结果表明,QT-NLCs 可促进 QT 的渗透,增加 QT 在表皮和真皮中的蓄积量,增强 QT 的抗氧化和抗炎作用。然后通过组织切片进一步研究了 NLCs 促进药物渗透的机制。综上所述,NLCs 可能成为 QT 局部递药的有前途的载体。

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