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蛋白质和肽类药物的稳定化及递送方法:专利综述

Stabilization and delivery approaches for protein and peptide pharmaceuticals: an extensive review of patents.

作者信息

Swain Suryakanta, Mondal Debanik, Beg Sarwar, Patra Chinam Niranjan, Dinda Subas Chandra, Sruti Jammula, Rao Muddana Eswara Bhanoji

机构信息

Department of Pharmaceutics, Roland Institute of Pharmaceutical Sciences, At/Po: Khodasinghi, Berhampur- 760 010(Ganjam), Odisha, India.

出版信息

Recent Pat Biotechnol. 2013 Apr;7(1):28-46. doi: 10.2174/1872208311307010004.

DOI:10.2174/1872208311307010004
PMID:23441815
Abstract

Proteins and peptides are the building blocks of human body and act as the arsenal to combat against the invading pathogenic organisms for treatment and management of diseases. Majority of such biomacromolecules are synthesized by the human body itself. However, entry of disease causing pathogens causes misleading in the synthesis of desired proteins for antibody formation. In such alarming situations, the delivery of requisite protein and peptide from external source helps in augmenting the body's immunity. The major drawbacks underlying poor biopharmaceutical performance of high molecular weight protein and peptide drugs are due to poor oral absorption, formulation stability, degradation in the gastric milieu, susceptible to presystemic metabolism. Numerous literature recounts the application of myriad drug delivery strategies for the effective delivery of protein and peptides viz. parentral, oral, transdermal, nasal, pulmonary, rectal, buccal and ocular drug delivery systems. There are many reviews on various delivery strategies for protein and peptide pharmaceuticals, but the present review article provides a bird's eye view on various novel drug delivery systems used for enhanced delivery of protein and peptide pharmaceuticals in the light of patent literature. Apart from this, the present manuscript endeavor provides idea on possible causes and major degradation pathways responsible for poor stability of protein and peptide drugs along with recent market instances on them utilizing novel drug delivery systems.

摘要

蛋白质和肽是人体的组成部分,并且作为对抗入侵病原体以治疗和管理疾病的武器库。大多数此类生物大分子是由人体自身合成的。然而,致病病原体的侵入会导致在合成用于抗体形成的所需蛋白质时产生误导。在这种令人担忧的情况下,从外部来源递送必需的蛋白质和肽有助于增强人体免疫力。高分子量蛋白质和肽类药物生物制药性能不佳的主要缺点是口服吸收差、制剂稳定性差、在胃环境中降解、易受首过代谢影响。众多文献叙述了无数药物递送策略在蛋白质和肽有效递送方面的应用,即肠胃外、口服、透皮、鼻腔、肺部、直肠、颊部和眼部药物递送系统。关于蛋白质和肽类药物的各种递送策略有许多综述,但本综述文章根据专利文献,对用于增强蛋白质和肽类药物递送的各种新型药物递送系统提供了一个全景式的视角。除此之外,本手稿还努力提供关于蛋白质和肽类药物稳定性差的可能原因和主要降解途径的观点,以及利用新型药物递送系统的近期市场实例。

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