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口服递送治疗性蛋白质和肽:最新进展综述。

Oral delivery of therapeutic proteins and peptides: a review on recent developments.

机构信息

Department of Biotechnology, Jaypee Institute of Information Technology, Noida, Uttar Pradesh, India.

出版信息

Drug Deliv. 2013 Aug;20(6):237-46. doi: 10.3109/10717544.2013.819611.

Abstract

Advent of recombinant technology in protein synthesis has given birth to a new range of biopharmaceuticals. These therapeutic peptides and proteins are now emerging as an imperative part of various treatment protocols especially in the cancer therapeutics. Despite extensive research efforts, oral delivery of therapeutic peptide or protein is still a challenge for pharmaceutical industries and researchers. Number of factors including high proteolytic activity and low pH conditions of gastrointestinal tract act as major barriers in the successful delivery of intact protein/peptide to the targeted site. Low permeability of protein/peptide across the intestinal barrier is also a factor adding to the low bioavailability. Therefore, because of the short circulatory half-life exhibited by peptides in vivo, they need to be administered frequently resulting in increased cost of treatment and low patient compliance. Nano-carrier-based delivery presents an appropriate choice of drug carriers owing to their property to protect proteins from degradation by the low pH conditions in stomach or by the proteolytic enzymes in the gastrointestinal tract. This review focuses on recent aspects and patents on oral delivery of therapeutic proteins and peptides with special emphasis on nano-carrier-based approach.

摘要

重组技术在蛋白质合成中的出现催生了一系列新型生物制药。这些治疗性肽和蛋白质现在已成为各种治疗方案的必要组成部分,特别是在癌症治疗中。尽管进行了广泛的研究,但治疗性肽或蛋白质的口服递送仍然是制药行业和研究人员面临的挑战。包括胃肠道中高蛋白酶活性和低 pH 条件在内的多种因素是将完整蛋白质/肽递送到靶向部位的主要障碍。蛋白质/肽在肠道屏障中的低渗透性也是导致其生物利用度低的一个因素。因此,由于肽在体内表现出的短循环半衰期,它们需要频繁给药,导致治疗成本增加和患者顺应性降低。基于纳米载体的递药系统因其具有保护蛋白质免受胃部低 pH 条件或胃肠道中蛋白酶降解的特性,成为一种合适的药物载体选择。本文重点介绍了治疗性蛋白质和肽口服递药的最新研究进展和专利,特别强调了基于纳米载体的方法。

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