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蛋白质和肽类口服给药策略及其临床前景综述。

A review on the strategies for oral delivery of proteins and peptides and their clinical perspectives.

作者信息

Muheem Abdul, Shakeel Faiyaz, Jahangir Mohammad Asadullah, Anwar Mohammed, Mallick Neha, Jain Gaurav Kumar, Warsi Musarrat Husain, Ahmad Farhan Jalees

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Hamdard University, Hamdard Nagar, New Delhi 110062, India.

Center of Excellence in Biotechnology Research (CEBR), King Saud University, Riyadh, Saudi Arab.

出版信息

Saudi Pharm J. 2016 Jul;24(4):413-28. doi: 10.1016/j.jsps.2014.06.004. Epub 2014 Jun 16.

DOI:10.1016/j.jsps.2014.06.004
PMID:27330372
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4908063/
Abstract

In the modern world, a number of therapeutic proteins such as vaccines, antigens, and hormones are being developed utilizing different sophisticated biotechnological techniques like recombinant DNA technology and protein purification. However, the major glitches in the optimal utilization of therapeutic proteins and peptides by the oral route are their extensive hepatic first-pass metabolism, degradation in the gastrointestinal tract (presence of enzymes and pH-dependent factors), large molecular size and poor permeation. These problems can be overcome by adopting techniques such as chemical transformation of protein structures, enzyme inhibitors, mucoadhesive polymers and permeation enhancers. Being invasive, parenteral route is inconvenient for the administration of protein and peptides, several research endeavors have been undertaken to formulate a better delivery system for proteins and peptides with major emphasis on non-invasive routes such as oral, transdermal, vaginal, rectal, pulmonary and intrauterine. This review article emphasizes on the recent advancements made in the delivery of protein and peptides by a non-invasive (peroral) route into the body.

摘要

在现代社会,人们利用重组DNA技术和蛋白质纯化等不同的先进生物技术,研发了多种治疗性蛋白质,如疫苗、抗原和激素。然而,口服治疗性蛋白质和肽在最佳利用方面的主要障碍包括广泛的肝脏首过代谢、在胃肠道中的降解(存在酶和pH依赖因素)、大分子尺寸以及较差的渗透性。通过采用蛋白质结构化学转化、酶抑制剂、粘膜粘附聚合物和渗透促进剂等技术,可以克服这些问题。由于注射途径具有侵入性,蛋白质和肽的给药不方便,因此人们进行了多项研究努力,以开发更好的蛋白质和肽递送系统,主要侧重于口服、透皮、阴道、直肠、肺部和子宫内等非侵入性途径。这篇综述文章重点介绍了通过非侵入性(口服)途径将蛋白质和肽递送至体内的最新进展。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df86/4908063/bff2a658ef88/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df86/4908063/5f363ea4ebbe/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df86/4908063/bff2a658ef88/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df86/4908063/5f363ea4ebbe/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df86/4908063/bff2a658ef88/gr1.jpg

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本文引用的文献

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