Optimization of preparation techniques for poly(lactic acid-co-glycolic acid) nanoparticles
Optimization of preparation techniques for poly(lactic acid-co-glycolic acid) nanoparticles
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DOI：
10.1023/a:1010038908767
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发表时间：
2000-06-01
影响因子：
2.5
通讯作者：
Brannon-Peppas, Lisa
中科院分区：
文献类型：
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作者：
Birnbaum, Duane T.;Kosmala, Jacqueline D.;Brannon-Peppas, Lisa
聚（乳酸-羟基乙酸）（PLAGA）的微粒和纳米颗粒由于其生物可降解性而成为许多药物化合物控释的优良候选物。亚微米PLAGA颗粒的制备提出了制备微粒时不一定存在的严重挑战。我们已经评估了PLAGA纳米颗粒制剂中使用的有机溶剂和表面活性剂的几种组合。关键因素，如从表面活性剂分离的能力，冷冻干燥后，配方产量和纳米粒子的大小重新悬浮的纳米粒子的能力进行了研究。使用十二烷基硫酸钠和乙酸乙酯的表面活性剂/溶剂组合获得最小的颗粒（65 nm），使用聚（乙烯醇）和二氯甲烷获得最大的颗粒（466 nm）。然而，最佳的纳米粒子使用丙酮或乙酸乙酯作为有机溶剂和聚（乙烯醇）或人血清白蛋白作为表面活性剂。这是因为这些纳米颗粒的性能的最关键的测量被证明是它们在冷冻干燥后重新悬浮的能力。
Microparticles and nanoparticles of poly(lactic acid-co-glycolic acid) (PLAGA) are excellent candidates for the controlled release of many pharmaceutical compounds because of their biodegradable nature. The preparation of submicron PLAGA particles poses serious challenges that are not necessarily present when preparing microparticles. We have evaluated several combinations of organic solvents and surfactants used in the formulation of PLAGA nanoparticles. Critical factors such as the ability to separate the nanoparticles from the surfactant, the ability to re-suspend the nanoparticles after freeze-drying, formulation yield and nanoparticle size were studied. The smallest particles were obtained using the surfactant/solvent combination of sodium dodecyl sulfate and ethyl acetate (65 nm) and the largest particles were obtained using poly(vinyl alcohol) and dichloromethane (466 nm). However, the optimal nanoparticles were produced using either acetone or ethyl acetate as the organic solvent and poly(vinyl alcohol) or human serum albumin as the surfactant. This is because the most critical measure of performance of these nanoparticles proved to be their ability to re-suspend after freeze-drying.