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介孔二氧化硅作为槲皮素的局部纳米载体:表征及体外研究

Mesoporous silica as topical nanocarriers for quercetin: characterization and in vitro studies.

作者信息

Sapino Simona, Ugazio Elena, Gastaldi Lucia, Miletto Ivana, Berlier Gloria, Zonari Daniele, Oliaro-Bosso Simonetta

机构信息

Università di Torino, Dipartimento di Scienza e Tecnologia del Farmaco, Torino, Italy; NIS (Nanostructured Interfaces and Surfaces) Centre, Università di Torino, Italy; "G. Scansetti" Interdepartmental Centre, Università di Torino, Italy.

Università di Torino, Dipartimento di Scienza e Tecnologia del Farmaco, Torino, Italy; NIS (Nanostructured Interfaces and Surfaces) Centre, Università di Torino, Italy; "G. Scansetti" Interdepartmental Centre, Università di Torino, Italy.

出版信息

Eur J Pharm Biopharm. 2015 Jan;89:116-25. doi: 10.1016/j.ejpb.2014.11.022. Epub 2014 Dec 3.

Abstract

The flavonoid quercetin is extensively studied for its antioxidant and chemopreventive properties. However the poor water-solubility, low stability and short half-life could restrict its use in skin care products and therapy. The present study was aimed to evaluate the potential of aminopropyl functionalized mesoporous silica nanoparticles (NH2-MSN) as topical carrier system for quercetin delivery. Thermo gravimetric analysis, X-ray diffraction, high resolution transmission electron microscopy, nitrogen adsorption isotherms, FT-IR spectroscopy, zeta potential measurements and differential scanning calorimetry allowed analyzing with great detail the organic-inorganic molecular interaction. The protective effect of this vehicle on UV-induced degradation of the flavonoid was investigated revealing a certain positive influence of the inclusion on the photostability over time. Epidermal accumulation and transdermal permeation of this molecule were ex vivo evaluated using porcine skin mounted on Franz diffusion cells. The inclusion complexation with the inorganic nanoparticles increased the penetration of quercetin into the skin after 24h post-application without transdermal delivery. The effect of quercetin alone or given as complex with NH2-MSN on proliferation of JR8 human melanoma cells was evaluated by sulforhodamine B colorimetric proliferation assay. At a concentration 60 μM the complex with NH2-MSN was more effective than quercetin alone, causing about 50% inhibition of cell proliferation.

摘要

黄酮类化合物槲皮素因其抗氧化和化学预防特性而受到广泛研究。然而,其水溶性差、稳定性低和半衰期短可能会限制其在护肤品和治疗中的应用。本研究旨在评估氨丙基功能化介孔二氧化硅纳米颗粒(NH2-MSN)作为槲皮素局部给药载体系统的潜力。热重分析、X射线衍射、高分辨率透射电子显微镜、氮吸附等温线、傅里叶变换红外光谱、zeta电位测量和差示扫描量热法能够详细分析有机-无机分子相互作用。研究了该载体对紫外线诱导的黄酮类化合物降解的保护作用,结果表明包合物对光稳定性随时间有一定的积极影响。使用安装在Franz扩散池上的猪皮对该分子的表皮蓄积和透皮渗透进行了离体评估。在给药24小时后,与无机纳米颗粒的包合络合增加了槲皮素在无透皮递送情况下进入皮肤的渗透率。通过磺基罗丹明B比色增殖试验评估了单独的槲皮素或与NH2-MSN形成的络合物对JR8人黑色素瘤细胞增殖的影响。在浓度为60μM时,与NH2-MSN形成的络合物比单独的槲皮素更有效,可导致约50%的细胞增殖抑制。

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