Diffusion loading and drug delivery characteristics of alginate gel microparticles produced by a novel impinging aerosols method
Diffusion loading and drug delivery characteristics of alginate gel microparticles produced by a novel impinging aerosols method
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DOI：
10.3109/1061186x.2010.525651
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发表时间：
2010-12-01
影响因子：
4.5
通讯作者：
Coombes, Allan G. A.
中科院分区：
文献类型：
--
作者：
Hariyadi, Dewi M.;Lin, Sharon Chien-Yu;Coombes, Allan G. A.
亲水性的硫酸庆大霉素(GS)和疏水性的非甾体抗炎药布洛芬(布洛芬)通过分子扩散进入海藻酸盐溶液和CaCl2交联液的气雾剂中，实现了海藻酸凝胶微粒的微胶囊化。用激光光散射法测得平均粒径为30-50微米，GS和布洛芬的载药量分别约为35%和29%。GS在模拟肠液(PBS，pH 7.4，37℃)和模拟胃液(SGF，pH 1.2，37℃)中的释放相似，但在PBS中，微粒在HCl中孵育后，GS的释放速度加快。布洛芬在SGF中的释放受到限制，但在微粒转移到PBS中时可以自由释放，释放效率几乎为100%。在PBS中释放的GS在盐酸中孵育2小时后，对表皮葡萄球菌保持了至少80%的活性，而布洛芬对白色念珠菌保持了50%左右的活性。撞击气雾剂技术显示了生产海藻酸凝胶微粒的潜力，该微粒可用于保护和控制一系列治疗分子的输送。
Microencapsulation of a hydrophilic active (gentamicin sulphate (GS)) and a hydrophobic non-steroidal antiinflammatory drug (ibuprofen) in alginate gel microparticles was accomplished by molecular diffusion of the drug species into microparticles produced by impinging aerosols of alginate solution and CaCl(2) cross-linking solution. A mean particle size in the range of 30-50 mu m was measured using laser light scattering and high drug loadings of around 35 and 29% weight/dry microparticle weight were obtained for GS and ibuprofen respectively. GS release was similar in simulated intestinal fluid (phosphate buffer saline (PBS), pH 7.4, 37 degrees C) and simulated gastric fluid (SGF) (HCl, pH 1.2, 37 degrees C) but was accelerated in PBS following incubation of microparticles in HCl. Ibuprofen release was restricted in SGF but occurred freely on transfer of microparticles into PBS with almost 100% efficiency. GS released in PBS over 7 h, following incubation of microparticles in HCl for 2 h was found to retain at least 80% activity against Staphylococcus epidermidis while Ibuprofen retained around 50% activity against Candida albicans. The impinging aerosols technique shows potential for producing alginate gel microparticles of utility for protection and controlled delivery of a range of therapeutic molecules.