Faculty of Pharmacy, University of Ljubljana, Askerceva 7, 1000 Ljubljana, Slovenia.
Int J Pharm. 2010 Mar 30;388(1-2):151-8. doi: 10.1016/j.ijpharm.2009.12.055. Epub 2010 Jan 7.
The primary goal of this study was to formulate Ca-pectinate microcapsules with self-microemulsifying core to enhance the solubility and permeability of BCS class IV drug furosemide. An Inotech IE-50R encapsulator equipped with a concentric nozzle was utilized to transform liquid self-microemulsifying system (SMES) to solid microcapsules. Self-microemulsifying core was optimized with respect to drug loading capacity and encapsulation efficiency and evaluated for its impact on furosemide permeability through rat small intestine and Caco-2 cell monolayers. Retention of the core phase was considerably improved (up to 70-80%) by optimization of the SMES and microcapsules' drying process. Incorporation of furosemide in self-microemulsifying core of microcapsules resulted in improved permeability and drug release characteristics in comparison to microspheres (without SMES in the core). The obtained results illustrate the prospective use of microcapsules with self-microemulsifying core for the delivery of compounds with poor biopharmaceutical properties via the oral route.
本研究的主要目的是制备载有自微乳核心的 Ca-藻酸盐微胶囊，以提高 BCS 类 IV 药物呋塞米的溶解度和渗透性。采用配备同心喷嘴的 Inotech IE-50R 包封机将液体自微乳体系（SMES）转化为固体微胶囊。自微乳核心的载药量和包封效率进行了优化，并评价了其对大鼠小肠和 Caco-2 细胞单层中呋塞米渗透性的影响。通过优化 SMES 和微胶囊干燥工艺，核心相的保留率得到了显著提高（高达 70-80%）。与微球（核心中无 SMES）相比，将呋塞米掺入微胶囊的自微乳核心中可改善渗透性和药物释放特性。所得结果表明，自微乳核心的微胶囊具有用于通过口服途径递送生物药剂学性质差的化合物的潜力。
