Diffusion loading and drug delivery characteristics of alginate gel microparticles produced by a novel impinging aerosols method

作者：Hariyadi Dewi M; Lin Sharon Chien Yu; Wang Yiwei; Bostrom Thor; Turner Mark S; Bhandari Bhesh; Coombes Allan G A^*

来源：Journal of Drug Targeting, 2010, 18(10): 831-841.

DOI：10.3109/1061186X.2010.525651

• Alginate gel microparticles
• ibuprofen
• gentamicin sulphate
• drug release
• activity
• S. epidermidis
• C. albicans

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.

• 出版日期2010-12