Ito Fuminori, Fujimori Hiroyuki, Honnami Hiroyuki, Kawakami Hiroyoshi, Kanamura Kiyoshi, Makino Kimiko
Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan.
Colloids Surf B Biointerfaces. 2008 Oct 1;66(1):65-70. doi: 10.1016/j.colsurfb.2008.05.011. Epub 2008 May 24.
Monodisperse poly(lactide-co-glycolide) (PLGA) microspheres containing rifampicin (RFP), anti-tubercle drug, as hydrophobic model drug were prepared by solvent evaporation method with a membrane emulsification technique using Shirasu Porous Glass (SPG) membranes. Five kinds of rifampicin-loaded PLGA (RFP/PLGA) microspheres with different sizes were prepared by changing pore size of the membranes. Effect of polyethylene glycol (PEG) added to polyvinyl alcohol (PVA) solution (continuous phase) upon the monodispersity of microspheres was studied. PEG was used as a stabilizer for microspheres dispersing in PVA solution. The most suitable molecular weight of PEG as a stabilizer was 20,000. RFP/PLGA microspheres prepared with PEG20000 were apparently more uniform than those prepared without PEG. The yield of RFP/PLGA microspheres was 100%. The initial burst observed in the release of RFP from RFP/PLGA microspheres was suppressed by the addition of PEG.
采用溶剂蒸发法结合膜乳化技术，使用多孔玻璃（SPG）膜制备了含有抗结核药物利福平（RFP）的单分散聚（丙交酯 - 乙交酯）（PLGA）微球，作为疏水性模型药物。通过改变膜的孔径，制备了五种不同尺寸的载有利福平的PLGA（RFP/PLGA）微球。研究了添加到聚乙烯醇（PVA）溶液（连续相）中的聚乙二醇（PEG）对微球单分散性的影响。PEG用作微球分散在PVA溶液中的稳定剂。作为稳定剂的PEG最合适的分子量为20000。用PEG20000制备的RFP/PLGA微球明显比未添加PEG制备的微球更均匀。RFP/PLGA微球的产率为100%。通过添加PEG抑制了RFP从RFP/PLGA微球释放中观察到的初始突释。
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