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脂质球作为脂质载体系统的前瞻性概述。

A perspective overview on lipospheres as lipid carrier systems.

作者信息

Dudala Thushara Bindu, Yalavarthi Prasanna Raju, Vadlamudi Harini Chowdary, Thanniru Jyotsna, Yaga Gowri, Mudumala Naga Lakshmi, Pasupati Vivek Kumar

机构信息

Pharmaceutics Division, Sree Vidyankethan College of Pharmacy, Tirupati, Andhra Pradesh, India.

出版信息

Int J Pharm Investig. 2014 Oct;4(4):149-55. doi: 10.4103/2230-973X.143112.

DOI:10.4103/2230-973X.143112
PMID:25426435
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4241619/
Abstract

Both hydrophilic and lipophilic therapeutics can be delivered successfully into deep and peripheral tissues such as cerebrospinal fluid and central nervous system by encapsulating them with crystalline lipids as lipospheres. The advent of lipospheres was meant to deliver both therapeutic moieties with enhanced efficacy and added stability to reach out intended tissue areas. Although extensive information is available on physicochemical, analytical and biopharmaceutical aspects of lipospheres, there was no specific order pertaining to critical composition and rationale of component selection available for academic and pilot scale processing of lipospheres. With the interest of compiling key points in a typical formulation of lipid lipospheres, this article was intrigued to discuss melt method, co-solvent, microemulsion, super critical fluid, spray drying and spray congealing techniques that were employed to scale up lipospheres. The selection criteria for both the drugs and lipids in liposphere formulations were demonstrated here. The quality assessment with variables like loading capacity and entrapment efficiency was explained. A note on preliminary screening factors to determine the liposphere formation such as liposphere dimensions with morphological scenario was detailed in this article. This article also includes the stability and storage issues with reference to photolysis. The marked differential in enhancing solubility and permeability characteristics of Class II and IV drug candidates by liposphere delivery systems with an evident of in vivo outcomes were emphasized.

摘要

通过将亲水性和亲脂性治疗药物包裹在作为脂质球的结晶脂质中,可成功将其递送至深部和外周组织,如脑脊液和中枢神经系统。脂质球的出现旨在递送具有更高疗效和稳定性的两种治疗成分,以到达预期的组织区域。尽管关于脂质球的物理化学、分析和生物制药方面有大量信息,但对于脂质球学术和中试规模制备的关键组成和成分选择原理,尚无特定顺序。出于汇编脂质脂质球典型配方要点的兴趣,本文旨在讨论用于扩大脂质球规模的熔融法、共溶剂法、微乳法、超临界流体法、喷雾干燥法和喷雾凝固技术。本文展示了脂质球配方中药物和脂质的选择标准。解释了诸如载药量和包封率等变量的质量评估。本文详细介绍了确定脂质球形成的初步筛选因素,如具有形态学情况的脂质球尺寸。本文还包括了与光解相关的稳定性和储存问题。强调了脂质球递送系统在增强II类和IV类候选药物的溶解度和渗透性特征方面的显著差异以及明显的体内结果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/782a/4241619/a8e405fe9d2b/IJPI-4-149-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/782a/4241619/a8e405fe9d2b/IJPI-4-149-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/782a/4241619/a8e405fe9d2b/IJPI-4-149-g001.jpg

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