Modifying the release of leuprolide from spray dried OED microparticles
Modifying the release of leuprolide from spray dried OED microparticles
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DOI：
10.1016/s0168-3659(02)00165-7
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发表时间：
2002-08-21
影响因子：
10.8
通讯作者：
Quirk, AV
中科院分区：
文献类型：
--
作者：
Alcock, R;Blair, JA;Quirk, AV
一系列寡糖酯衍生物（OED）已被设计为用于控制释放的药物递送基质。使用疏水离子配对和溶剂喷雾干燥将合成激素类似物亮丙瑞林包封在这些基质中。所产生的颗粒改变了亮丙瑞林的体外（在磷酸盐缓冲盐水中溶解）和体内（大鼠皮下和肺部递送）释放。释放速率取决于载药量，并且可以通过OED的选择和以不同比例组合不同OED来操纵。体内给药前，皮下注射从体外OED颗粒中回收的亮丙瑞林后，血浆促黄体生成激素水平升高证明，OED中包封的亮丙瑞林保留了生物活性。(C)2002 Elsevier Science BV保留所有权利。
A range of oligosaccharide ester derivatives (OEDs) have been designed as drug delivery matrices for controlled release. The synthetic hormone analogue, leuprolide, was encapsulated within these matrices using hydrophobic ion pairing and solvent spray drying. The particles produced modified the release of leuprolide in vitro (dissolution in phosphate buffered saline) and in vivo (subcutaneous and pulmonary delivery in the rat). Release rate was dependent on drug loading and could be manipulated by choice of OED and by combining different OEDs in different ratios. Leuprolide encapsulated in the OEDs retained biological activity as evidenced by elevation in plasma luteinising hormone levels following subcutaneous injection of leuprolide recovered from OED particles in vitro prior to in vivo administration. (C) 2002 Elsevier Science BV All rights reserved.