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纳米结构脂质载体——一种用于亲脂性药物口服递送的多功能载体。

Nanostructured Lipid Carriers- A Versatile Carrier for Oral Delivery of Lipophilic Drugs.

作者信息

Patel Priyanshi, Patel Mitali

机构信息

Maliba Pharmacy College, Uka Tarsadia University, Surat 394350, Gujarat, India.

出版信息

Recent Pat Nanotechnol. 2021;15(2):154-164. doi: 10.2174/1872210514666200909154959.

DOI:10.2174/1872210514666200909154959
PMID:32912129
Abstract

BACKGROUND

Around 40% of newly discovered chemical entities in pharmaceutical industries have poor water solubility and hence they suffer from low oral bioavailability owing to undesirable physicochemical and pharmacokinetic properties. So, it is the challenge for the formulation scientists to develop the oral formulation that can mitigate the pitfalls associated with such lipophilic drugs.

METHODS

Lipid nanoparticles hold a promising tool to decrease the pitfalls of lipophilic drugs as lipid components can effectively increase the absorption of drugs, which leads to improvement in oral bioavailability. They are also considered as safe because they are made up of physiological lipids, which are biocompatible and biodegradable in nature. Amongst the lipid nanoparticles, Nanostructured Lipid Carriers (NLCs) are the second-generation lipid nanoparticles and were developed to conquer the limitations of solid lipid nanoparticles. They increase the solubility, permeability, reduce metabolism, P-glycoprotein efflux, and thereby increase the bioavailability of poorly soluble drugs.

CONCLUSION

This review highlights the various aspects of NLCs, such as structural components, types, in vivo fate, pharmacokinetic, toxicity, recent applications, and patent reviews of NLCs in drug delivery.

摘要

背景

制药行业中约40%新发现的化学实体水溶性较差,因此由于不良的物理化学和药代动力学性质,它们的口服生物利用度较低。所以,开发能够减轻与此类亲脂性药物相关缺陷的口服制剂是制剂科学家面临的挑战。

方法

脂质纳米粒是减少亲脂性药物缺陷的一种有前景的工具,因为脂质成分可以有效增加药物的吸收,从而提高口服生物利用度。它们也被认为是安全的,因为它们由生理脂质组成,这些脂质具有生物相容性且在自然界中可生物降解。在脂质纳米粒中,纳米结构脂质载体(NLCs)是第二代脂质纳米粒,其开发目的是克服固体脂质纳米粒的局限性。它们可提高溶解度、渗透性,减少代谢、P-糖蛋白外排,从而提高难溶性药物的生物利用度。

结论

本综述重点介绍了纳米结构脂质载体的各个方面,如结构成分、类型、体内命运、药代动力学、毒性、近期应用以及纳米结构脂质载体在药物递送方面的专利综述。

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