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用于槲皮素局部递送的脂质基纳米系统的制备与表征

Preparation and characterization of lipid based nanosystems for topical delivery of quercetin.

作者信息

Bose Sonali, Michniak-Kohn Bozena

机构信息

Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, United States; Pharmaceutical and Analytical Development, Novartis Pharmaceuticals Corporation, One Health Plaza, East Hanover, NJ 07936, United States.

Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, United States.

出版信息

Eur J Pharm Sci. 2013 Feb 14;48(3):442-52. doi: 10.1016/j.ejps.2012.12.005. Epub 2012 Dec 13.

Abstract

The main objective of this study was to evaluate the potential of lipid nanosystems for topical delivery of the naturally occurring flavonoid quercetin. These lipid based nanosystems were manufactured using a solvent free probe ultrasonication process. Formulation factors such as the nature of the lipid (solid/combination of solid and liquid) in solid lipid nanoparticle (SLN) and nanostructured lipid carrier (NLC) systems and drug loading were evaluated to produce an optimum formulation with adequate physical stability for up to 14 weeks at 2-8°C. The mean particle size of the optimized formulation was around 282 nm, with a zeta potential value of -36.57 ± 2.67 mV, indicating the formation of a stable system. Release studies showed a biphasic release profile, characterized by an initial burst release followed by a more controlled release pattern from both SLN and NLC systems. The NLC system showed the highest improvement in topical delivery of quercetin manifested by the amount of quercetin retained in full thickness human skin, compared to a control formulation with similar composition and particle size in the micrometer range. This study demonstrated the feasibility of nanostructured lipid carrier systems for improved topical delivery of quercetin.

摘要

本研究的主要目的是评估脂质纳米系统用于天然存在的类黄酮槲皮素局部递送的潜力。这些基于脂质的纳米系统采用无溶剂探头超声处理工艺制备。对诸如固体脂质纳米粒(SLN)和纳米结构脂质载体(NLC)系统中脂质的性质(固体/固体与液体的组合)以及药物负载等制剂因素进行了评估,以制备出在2-8°C下具有长达14周足够物理稳定性的最佳制剂。优化制剂的平均粒径约为282 nm,zeta电位值为-36.57±2.67 mV,表明形成了稳定的系统。释放研究显示出双相释放曲线,其特征是初始的突释,随后是来自SLN和NLC系统的更可控的释放模式。与具有相似组成和微米级粒径的对照制剂相比,NLC系统在槲皮素的局部递送方面表现出最高的改善,这通过全层人皮肤中保留的槲皮素量得以体现。本研究证明了纳米结构脂质载体系统用于改善槲皮素局部递送的可行性。

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