Wang N, Wu X S
Division of Pharmaceutics and Industrial Pharmacy, Arnold & Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY 11201, USA.
J Biomater Sci Polym Ed. 1997;9(1):75-87. doi: 10.1163/156856297x00272.
Previously synthesized lactic/glycolic acid (PLGA) oligomers with different compositions (i.e. different ratio of lactic to glycolic acid in the oligomers) were further studied regarding their biodegradation and drug delivery application. The PLGA oligomers have fast biodegradation characteristics. They degrade to water soluble substances, i.e. lactic and glycolic acids, at a rate of 31.43-40.68 mg day-1 in a medium of constant pH and 28.04-37.87 mg day-1 in a medium of non-constant pH. The biodegradation rate is affected by the composition of the PLGA oligomers and the pH of the incubating medium. The higher the content of glycolic acid moiety in the oligomer, the faster the biodegradation rate. The lower the pH of the incubating medium, the slower the biodegradation of PLGA oligomers. A sustained-release drug delivery system based on the PLGA oligomers was fabricated as injectable microgranules by thermal blending of the PLGA oligomers and drug. Aspirin was used as a model drug. The oligomeric microgranules have advantages of easy fabrication, high drug loading efficiency, easy administration, and fast biodegradation. This thermal blending preparation method has a high loading efficiency of more than 90%. The PLGA oligomeric microgranules can release drug from 9 to 13 days depending on the oligomer composition. Both drug release rate and release duration are influenced by composition of the oligomers. The PLGA oligomeric matrix has the capability of protecting aspirin from hydrolysis. The lactic/glycolic acid oligomeric microgranules have potential use for sustained-release drug delivery.
此前合成的具有不同组成(即低聚物中乳酸与乙醇酸的不同比例)的乳酸/乙醇酸共聚物(PLGA)低聚物,就其生物降解和药物递送应用进行了进一步研究。PLGA低聚物具有快速生物降解特性。它们在恒定pH值的介质中以31.43 - 40.68毫克/天的速率降解为水溶性物质,即乳酸和乙醇酸,在非恒定pH值的介质中以28.04 - 37.87毫克/天的速率降解。生物降解速率受PLGA低聚物的组成和孵育介质的pH值影响。低聚物中乙醇酸部分的含量越高,生物降解速率越快。孵育介质的pH值越低,PLGA低聚物的生物降解越慢。基于PLGA低聚物的缓释药物递送系统通过将PLGA低聚物与药物热混合制成可注射微颗粒。阿司匹林用作模型药物。该低聚物微颗粒具有易于制备、药物负载效率高、易于给药和快速生物降解的优点。这种热混合制备方法具有超过90%的高负载效率。PLGA低聚物微颗粒可根据低聚物组成在9至13天内释放药物。药物释放速率和释放持续时间均受低聚物组成的影响。PLGA低聚物基质具有保护阿司匹林不被水解的能力。乳酸/乙醇酸低聚物微颗粒在缓释药物递送方面具有潜在用途。