Development of PEG-PLA/PLGA microparticles for pulmonary drug delivery prepared by a novel emulsification technique assisted with amphiphilic block copolymers.
Development of PEG-PLA/PLGA microparticles for pulmonary drug delivery prepared by a novel emulsification technique assisted with amphiphilic block copolymers.
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DOI：
10.1016/j.colsurfb.2011.06.004
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发表时间：
2011-10
期刊：
影响因子：
--
通讯作者：
T. Takami;Y. Murakami
中科院分区：
文献类型：
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作者：
T. Takami;Y. Murakami
我们开发了一种新的“喷雾干燥”方法，通过“嵌段共聚物辅助”乳化/蒸发制备表面修饰的颗粒，用于肺部给药。该方法包括三个步骤：(1)通过水和含聚合物的有机溶剂的乳化得到同时含有疏水聚合物和两亲性嵌段共聚物的O/W乳状液；(2)用雾化器雾化O/W乳状液；(3)用加热器干燥乳状液雾。这样，在有机溶剂从O/W乳液中蒸发的过程中，疏水聚合物和两亲性嵌段共聚物的疏水部分逐渐缠绕在一起。因此，在粒子表面引入了亲水性高分子链。虽然疏水聚合物分子中不存在活性基团，但颗粒表面很容易修饰。通过控制嵌段共聚物和疏水聚合物的质量比，成功地制得了干燥的聚乙二醇聚乳酸/聚乳酸微球。在颗粒表面引入聚乙二醇酯会增加颗粒的Zeta电位。有趣的是，获得了直径约为2μm的“凹陷”微粒。这种“凹陷”的微粒可以作为肺部给药的药物载体，因为这种微粒具有较大的表面积。我们希望这种新的表面修饰技术能够有效地制造药物输送系统中的颗粒。
We developed a novel “spray dry-based” method for preparing surface-modified particle via “block copolymer-assisted” emulsification/evaporation for pulmonary drug delivery. The method included three steps: (1) o/w emulsion containing both hydrophobic polymers and amphiphilic block copolymers was obtained by emulsification of water and a polymer-containing organic solvent, (2) the o/w emulsion was misted with a nebulizer, and (3) the emulsion mists were dried by a heater. In this way, the hydrophobic polymers and the hydrophobic part of the amphiphilic block copolymers gradually tangled during the evaporation of organic solvents from the o/w emulsion. Consequently, the hydrophilic polymer chain was introduced on the particle surface. The particle surface can be easily modified although there are no reactive groups in the hydrophobic polymer molecules. We successfully obtained dry PEG–PLA/PLGA microparticles by controlling the weight ratio of the block copolymer and the hydrophobic polymer. The introduction of PEG to the particle surface involves an increase in the Zeta potential of the particles. Interestingly, the “dimpled” microparticles having a diameter of approximately 2μm were obtained. The “dimpled” microparticles can serve as drug carriers for pulmonary drug delivery, because the particles have a large surface area. We expect that this novel surface-modification technique will enable efficient fabrication of particles in drug delivery systems.