前药方法：提高药物溶解度的成功工具。

The Prodrug Approach: A Successful Tool for Improving Drug Solubility.

作者信息

Jornada Daniela Hartmann, dos Santos Fernandes Guilherme Felipe, Chiba Diego Eidy, de Melo Thais Regina Ferreira, dos Santos Jean Leandro, Chung Man Chin

机构信息

Faculdade de Ciências Farmacêuticas, UNESP-University Estadual Paulista, Rodovia Araraquara Jaú Km 01, 14801-902 Araraquara, São Paulo, Brasil.

出版信息

Molecules. 2015 Dec 29;21(1):42. doi: 10.3390/molecules21010042.

DOI:10.3390/molecules21010042

PMID:26729077

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6273601/

Abstract

Prodrug design is a widely known molecular modification strategy that aims to optimize the physicochemical and pharmacological properties of drugs to improve their solubility and pharmacokinetic features and decrease their toxicity. A lack of solubility is one of the main obstacles to drug development. This review aims to describe recent advances in the improvement of solubility via the prodrug approach. The main chemical carriers and examples of successful strategies will be discussed, highlighting the advances of this field in the last ten years.

摘要

前药设计是一种广为人知的分子修饰策略，旨在优化药物的物理化学和药理性质，以提高其溶解度和药代动力学特征，并降低其毒性。溶解度不足是药物开发的主要障碍之一。本综述旨在描述通过前药方法改善溶解度的最新进展。将讨论主要的化学载体和成功策略的实例，突出该领域在过去十年中的进展。