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摘要
吸收性差、半衰期短以及耐药性的发展是一些药物疗效降低的主要因素。亲脂性前药能具有克服这些挑战的某些优势。具有亲脂部分的亲水性试剂的化学衍生物能显著地提高药物在吸收膜上的扩散。而且,筛选出的一些基团的连接(如酯和酰胺)具有提高体内药物稳定性的可能。重要的是,前半部分(目标配体)可能能够改善药物特异性和选择性。本文旨在总结能改善那些低渗透性但具有治疗作用的药物的传递性和疗效的亲脂性前药。此外,简短综述提供近期那些能够改善纳米级别药物运输中亲水性试剂的包装的亲脂类前药的应用。
关键词: 吸收;复方和传递;亲脂性;脂类;连接;前药
Current Drug Targets
Title:Design of Lipophilic Prodrugs to Improve Drug Delivery and Efficacy
Volume: 17 Issue: 15
Author(s): Abhirup Mandal, Mitesh Patel, Ye Sheng, Ashim K. Mitra
Affiliation:
关键词: 吸收;复方和传递;亲脂性;脂类;连接;前药
摘要: Poor absorption, short half-life and resistance development are some of the major factors responsible for reduced drug efficacy. Lipophilic prodrugs can offer certain advantages to overcome these challenges. Chemical derivatization of hydrophilic agents with lipophilic pro-moieties can significantly elevate drug diffusion across absorptive membranes. Moreover, the desired linkage (ester vs. amide) may be selected to improve stability in vivo. Importantly, an appropriate selection of pro-moiety (targeting ligand) may promote drug specificity and selectivity. In this review article, an attempt has been made to summarize lipophilic prodrugs employed to improve delivery and efficacy of a wide range of poorly permeable but highly potent therapeutic agents. In addition, a brief overview on recent application of lipophilic prodrugs to promote encapsulation of hydrophilic agents in nano-sized drug carriers has been provided.
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Cite this article as:
Abhirup Mandal, Mitesh Patel, Ye Sheng, Ashim K. Mitra , Design of Lipophilic Prodrugs to Improve Drug Delivery and Efficacy, Current Drug Targets 2016; 17 (15) . https://dx.doi.org/10.2174/1389450117666151209115431
DOI https://dx.doi.org/10.2174/1389450117666151209115431 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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