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天然脂质作为固体脂质纳米粒和纳米结构脂质载体的结构成分用于经皮给药。

Natural Lipids as Structural Components of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Topical Delivery.

机构信息

Department of Pharmaceutical Technologies, Faculty of Pharmacy, Medical University of Varna, Varna, Bulgaria.

出版信息

Curr Pharm Des. 2020;26(36):4524-4535. doi: 10.2174/1381612826666200514221649.

DOI:10.2174/1381612826666200514221649
PMID:32410552
Abstract

BACKGROUND

Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) are useful drug delivery systems for dermal application. Thanks to their biocompatible and biodegradable profile, these carriers offer many advantages such as enhanced bioavailability, low toxicity, viable drug targeting and controlled release. SLN and NLC are composed of well-tolerated lipids, including natural fats and oils that are successfully used in the pharmaceutical and cosmetic dermal formulation.

OBJECTIVE

This article presents an overview of the benefits of selecting natural fats and oils as structural components of SLN and NLC for topical application.

METHODS

This review is based on data published over the past 20 years about the development of stable and nontoxic lipid nanoparticles with natural lipids. We shed light on the role of natural fats in skin restoration, as well as on the contributed penetration and occlusive properties of SLN and NLC.

RESULTS

The deliberate selection of excipients (type and lipid ratio) influences the quality of the final dermal formulation. Natural lipids show good compatibility with different active molecules and are able to create stable lipid matrices that facilitate the biopharmaceutical properties of lipid nanoparticles. Patents involving natural fats and oils in SLN and NLC composition are listed, yet it is important to note that the approved marketed formulations are mainly cosmetic, not pharmaceutical, products.

CONCLUSION

Natural lipids can enhance topical drug delivery by adding their ability of improving skin penetration and hydration to the permeation and occlusion properties of SLN and NLC.

摘要

背景

固体脂质纳米粒(SLN)和纳米结构脂质载体(NLC)是用于经皮应用的有用药物传递系统。由于其具有生物相容性和可生物降解的特性,这些载体具有许多优点,例如提高生物利用度、低毒性、可行的药物靶向和控制释放。SLN 和 NLC 由可耐受的脂质组成,包括成功用于药物和化妆品经皮制剂的天然脂肪和油。

目的

本文概述了选择天然脂肪和油作为 SLN 和 NLC 经皮应用结构成分的益处。

方法

这篇综述基于过去 20 年来关于开发具有天然脂质的稳定和无毒脂质纳米粒的研究数据。我们阐明了天然脂肪在皮肤修复中的作用,以及 SLN 和 NLC 的渗透和封闭特性的贡献。

结果

赋形剂(类型和脂质比例)的精心选择会影响最终经皮制剂的质量。天然脂质与不同的活性分子具有良好的相容性,并且能够形成稳定的脂质基质,从而促进脂质纳米粒的生物制药特性。列出了涉及 SLN 和 NLC 中天然脂肪和油的专利,但值得注意的是,批准的市售制剂主要是化妆品,而不是药物产品。

结论

天然脂质可以通过提高其改善皮肤渗透和保湿的能力来增强经皮药物传递,从而增强 SLN 和 NLC 的渗透和封闭特性。

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