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载药微球的双重乳液技术及其在控制释放中的应用前景。

Prospects of pharmaceuticals and biopharmaceuticals loaded microparticles prepared by double emulsion technique for controlled delivery.

机构信息

Rungta College of Pharmaceutical Sciences and Research, Kohka Road, Kurud, Bhilai 490024, India.

出版信息

Saudi Pharm J. 2013 Apr;21(2):125-41. doi: 10.1016/j.jsps.2012.05.009. Epub 2012 May 26.

Abstract

Several methods and techniques are potentially useful for the preparation of microparticles in the field of controlled drug delivery. The type and the size of the microparticles, the entrapment, release characteristics and stability of drug in microparticles in the formulations are dependent on the method used. One of the most common methods of preparing microparticles is the single emulsion technique. Poorly soluble, lipophilic drugs are successfully retained within the microparticles prepared by this method. However, the encapsulation of highly water soluble compounds including protein and peptides presents formidable challenges to the researchers. The successful encapsulation of such compounds requires high drug loading in the microparticles, prevention of protein and peptide degradation by the encapsulation method involved and predictable release, both rate and extent, of the drug compound from the microparticles. The above mentioned problems can be overcome by using the double emulsion technique, alternatively called as multiple emulsion technique. Aiming to achieve this various techniques have been examined to prepare stable formulations utilizing w/o/w, s/o/w, w/o/o, and s/o/o type double emulsion methods. This article reviews the current state of the art in double emulsion based technologies for the preparation of microparticles including the investigation of various classes of substances that are pharmaceutically and biopharmaceutically active.

摘要

在控制药物释放领域,有几种方法和技术可用于制备微粒。微粒的类型和大小、药物在配方中的微粒中的包封、释放特性和稳定性取决于所使用的方法。制备微粒最常用的方法之一是单乳液技术。通过这种方法制备的微粒可以成功地保留疏水性差、脂溶性的药物。然而,包括蛋白质和肽在内的水溶性化合物的包封对研究人员提出了严峻的挑战。此类化合物的成功包封需要在微粒中实现高药物负载、通过所涉及的包封方法防止蛋白质和肽降解以及从微粒中预测药物化合物的释放速度和程度。通过使用双乳液技术(也称为多重乳液技术)可以克服上述问题。为了实现这一目标,已经研究了各种技术,以利用 w/o/w、s/o/w、w/o/o 和 s/o/o 型双乳液方法制备稳定的制剂。本文综述了基于双乳液技术制备微粒的最新技术,包括对具有药物和生物制药活性的各种类别的物质的研究。

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