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用于改善皮肤给药的固体分散脂质纳米粒的研发。

Development of solid dispersion lipid nanoparticles for improving skin delivery.

作者信息

Pham Duong T T, Tran Phuong H L, Tran Thao T D

机构信息

Chung-Ang University, Seoul, Republic of Korea.

Deakin University, Geelong Australia, School of Medicine, Australia.

出版信息

Saudi Pharm J. 2019 Nov;27(7):1019-1024. doi: 10.1016/j.jsps.2019.08.004. Epub 2019 Aug 30.

Abstract

Applications of poorly water-soluble drugs in skin delivery pose several challenges to pharmaceutical formulation. This research originally developed solid lipid nanoparticles (SLNs) packaging a modified core of a solid dispersion (SD) in the lipid matrix to modulate the skin release patterns. Curcumin (CUR) was selected as the poorly water-soluble drug applied in the formulation. The designed system, so-called solid dispersion lipid nanoparticles (SD-SLNs), was fabricated by incorporating a solidifying SD or a non-solidifying SD into the core of the SLNs by ultrasonication. Release studies illustrated an important enhancement in the drug release of the proposed system compared to pure CUR and SLN formulations without the presence of SD as the modified core, which indicated the positive effect of the combined colloidal method of SD and SLNs. The physicochemical properties of the SD-SLN systems were also elucidated using powder X-ray diffraction, Fourier transform infrared spectroscopy, and particle size analysis. The drug was found to change to an amorphous state without any molecular interactions along with a marked particle size reduction. This work demonstrated the strong potential of applying a novel SD-SLN system for the skin delivery of a drug with poor water solubility.

摘要

难溶性药物在皮肤给药中的应用给药物制剂带来了诸多挑战。本研究最初开发了一种固体脂质纳米粒(SLNs),其在脂质基质中包裹了固体分散体(SD)的改性核心,以调节皮肤释放模式。姜黄素(CUR)被选为制剂中应用的难溶性药物。所设计的系统,即固体分散脂质纳米粒(SD-SLNs),是通过超声处理将固化的SD或非固化的SD掺入SLNs的核心中制备而成。释放研究表明,与不含SD作为改性核心的纯CUR和SLN制剂相比,所提出的系统在药物释放方面有显著增强,这表明SD和SLNs的联合胶体方法具有积极作用。还使用粉末X射线衍射、傅里叶变换红外光谱和粒度分析对SD-SLN系统的物理化学性质进行了阐明。发现药物转变为无定形状态,没有任何分子相互作用,同时粒径显著减小。这项工作证明了应用新型SD-SLN系统进行难溶性药物皮肤给药的巨大潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d616/6978615/0dbf3c834493/gr1.jpg

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