Role of Lipid Blooming and Crystallite Size in the Performance of Highly Soluble Drug-Loaded Microcapsules

被引:22
|
作者
Lopes, Diogo G. [1 ,2 ]
Becker, Karin [2 ]
Stehr, Michael [3 ]
Lochmann, Dirk [3 ]
Haack, Detlev [4 ]
Zimmer, Andreas [2 ]
Salar-Behzadi, Sharareh [1 ]
机构
[1] Res Ctr Pharmaceut Engn GmbH, Graz, Austria
[2] Karl Franzens Univ Graz, Dept Pharmaceut Technol, Graz, Austria
[3] Cremer Oleo GmbH & Co KG, Witten, Germany
[4] Hermes Arzneimittel GmbH, Grosshansdorf, Germany
关键词
crystal growth; excipients; lipids; microencapsulation; dissolution; crystal structure; polymorphism; solid state; FRACTAL STRUCTURES; COATING PROCESS; WATER; MICROSTRUCTURES; TRANSFORMATION; DISSOLUTION; NANOSCALE; NETWORKS; IMPLANTS; SURFACES;
D O I
10.1002/jps.24660
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Hot-melt coating is of growing interest, because it does not require solvents, resulting in reduced process times and costs. However, excipients for this technology are mainly triacylglycerides (TAGs) or their derivatives, which exhibit polymorphism, surface disruption, and complex crystallite networks, affecting the release profile of produced microcapsules. In this work, anhydrous citric acid crystals were coated with molten tristearin using conventional inlet air temperatures (microcapsules A) and temperatures above the melting point of -form (microcapsules B). Additionally, microcapsules A were tempered to achieve polymorphic stability (microcapsules AB). The product yield and coating efficacy were above 90% and 97%, respectively, demonstrating the feasibility and efficacy of the process. Small angle X-ray scattering analysis confirmed that the tristearin shell of microcapsules B is in the -form with a larger average crystallite size than microcapsules A and AB. Scanning electron microscopy images revealed a nonbloomed surface of microcapsules B. We showed that blooming does not play a critical role in the drug release, but the apparent diffusion coefficient of drug is dramatically reduced by increasing TAGs crystallite size and resulting tortuosity. This work brings new insights on the micrometric properties of solid lipid dosage forms, being an important step to prevent the overuse of excipients with unknown toxicity. (C) 2015 Wiley Periodicals, Inc. and the American Pharmacists Association
引用
收藏
页码:4257 / 4265
页数:9
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