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固体脂质纳米粒:一种口服生物利用度增强载体。

Solid lipid nanoparticles: an oral bioavailability enhancer vehicle.

机构信息

National Institute of Pharmaceutical Education and Research, Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, SAS Nagar, Punjab, India.

出版信息

Expert Opin Drug Deliv. 2011 Nov;8(11):1407-24. doi: 10.1517/17425247.2011.604311. Epub 2011 Aug 11.

Abstract

INTRODUCTION

The therapeutic efficacy of perorally administered drugs is often obscured by their poor oral bioavailability (BA) and low metabolic stability in the gastrointestinal tract (GIT). Solid lipid nanoparticles (SLNs) have emerged as potential BA enhancer vehicles for various Class II, III and IV drug molecules.

AREA COVERED

This review examines the recent advancements in SLN technology, with regards to oral drug delivery. The discussion critically examines the effect of various key constituents on SLN absorption and their applications in oral drug delivery. The relationship between the complexity of absorption (and various factors involved during absorption, including particle size), stability and the self-emulsifying ability of the lipids used has been explored.

EXPERT OPINION

The protective effect of SLNs, coupled with their sustained/controlled release properties, prevents drugs/macromolecules from premature degradation and improves their stability in the GIT. An extensive literature survey reveals that direct peroral administration of SLNs improves the BA of drugs by 2- to 25-fold. Overall, the ease of large-scale production, avoidance of organic solvents and improvement of oral BA make SLNs a potential BA enhancer vehicle for various Class II, III and IV drugs.

摘要

简介

口服药物的治疗效果往往因胃肠道(GIT)中较差的口服生物利用度(BA)和低代谢稳定性而受到影响。固体脂质纳米粒(SLN)已成为各种 II 类、III 类和 IV 类药物分子潜在的 BA 增强载体。

涵盖领域

本综述考察了 SLN 技术在口服药物递送方面的最新进展。讨论批判性地考察了各种关键成分对 SLN 吸收的影响及其在口服药物递送中的应用。研究了吸收的复杂性(以及吸收过程中涉及的各种因素,包括粒径)、稳定性以及所用脂质的自乳化能力之间的关系。

专家意见

SLN 的保护作用,加上其持续/控制释放特性,可以防止药物/大分子在 GIT 中过早降解,提高其稳定性。广泛的文献调查表明,直接口服 SLN 可将药物的 BA 提高 2 至 25 倍。总的来说,大规模生产的便利性、避免有机溶剂和提高口服 BA 使 SLN 成为各种 II 类、III 类和 IV 类药物的潜在 BA 增强载体。

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