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聚乳酸/羟基乙酸磁性微球的制备及其姜黄素负载

Preparation of Polylactic Acid/Glycolic Acid Magnetic Microspheres and Their Loading of Curcumin

  • 摘要: 以聚乳酸/羟基乙酸(PLGA)共聚物为药物装载材料、油酸改性的四氧化三铁(Fe3O4@OA)纳米颗粒为磁性功能材料,制备姜黄素/PLGA磁性微球,考察了乳化方法、高速均质速度、水油相体积比、PLGA用量、水相聚乙烯醇(PVA)质量分数、Fe3O4@OA用量和姜黄素用量对磁性微球粒径的影响,并通过光学显微镜、激光粒度仪、紫外分光光度计、振动样品磁强计、热重分析仪等对其形貌及理化性能进行分析。研究结果显示:姜黄素/PLGA磁性微球的最佳制备工艺为选用搅拌-均质两步乳化法、高速均质15 000 r/min、水油相体积比10∶1、PLGA用量100 mg、水相PVA质量分数1%、Fe3O4@OA用量40 mg和姜黄素用量40 mg,此条件下制备的微球表面光滑,粒径较均一,多分散性指数(PDI)为0.38,平均粒径为3.60 μm,微球的磁感应强度为14.12(A·m2)/kg,含磁量约为27.98%。载药微球的包封率为97.09%,载药率为6.40%,在体外释放实验中表现出明显的缓释效果。

     

    Abstract: The curcumin/polylactic acid/glycolic acid(PLGA) magnetic microsphere was innovatively prepared by a stirring-homogenization two-step emulsification method using PLGA copolymer as drug loading material and oleic acid-modified triiron tetraoxide(Fe3O4@OA) nanoparticles as the magnetic functional material. Impacts of the emulsification method, high-speed homogenization speed, water oil volume ratio, PLGA dosage, mass fraction of aqueous polyvinyl alcohol(PVA), the dosage of Fe3O4@OA and curcumin on the particle size of magnetic microspheres were examined. The morphology and physicochemical properties of curcumin/PLGA magnetic microspheres were analyzed by optical microscope, laser particle sizer, ultraviolet spectrophotometer, vibrating sample magnetometer and thermogravimetric analyzer, respectively. The results showed that the optimal preparation process for curcumin/PLGA magnetic microspheres was the stirring homogenization two-step emulsification method, with a high-speed homogenization speed of 15 000 r/min, a water oil phase volume ratio of 10∶1, a PLGA dosage of 100 mg, a water phase PVA mass fraction of 1%, the Fe3O4@OA dosage of 40 mg and the dosage of 10 mg curcumin. Under these conditions, the surface of the microspheres was smooth, the particle size was homogeneous, the polydispersity index(PDI) was 0.38, the average particle size was 3.60 μm, the magnetic induction strength of the microspheres was 14.12 (A·m2)/kg, and the magnetic content was about 27.98%. The encapsulation rate of drug-laden microspheres was 97.09%, and the drug loading was 6.40%, which showed a significant sustained release effect in the in vitro release assay.

     

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