| PLA/MSM缓释微球的制备及生物活性 |
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| 引用本文： | 王鑫众,刘建国,唐宇锋,王宇,章培标,陈学思. PLA/MSM缓释微球的制备及生物活性[J]. 高等学校化学学报, 2013, 34(4): 984-991. DOI: 10.7503/cjcu20121108 |
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| 作者姓名： | 王鑫众 刘建国 唐宇锋 王宇 章培标 陈学思 |
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| 作者单位： | 1. 吉林大学第一医院, 长春 130021;2. 中国科学院长春应用化学研究所, 长春 130022 |
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| 基金项目： | 国家自然科学基金(批准号:51273081,51273195)资助. |
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| 摘 要： | 采用膜乳化-液中干燥法制备出担载二甲基砜(MSM)的聚乳酸(PLA)微球(PLA/MSM), 并研究了膜孔径、 搅拌转速和MSM浓度对载药微球形貌、 尺寸、 载药量、 体外释放及细胞活性的影响; 采用场发射环境扫描电子显微镜(ESEM)观察微球形貌、 尺寸及分布, 用等离子体发射光谱(ICP-AES)法检测PLA/MSM微球载药量、 包封率及体外释放, 采用ESEM观察微球内部结构, 并通过体外细胞培养和噻唑蓝(MTT)法检测MC-3T3-E1细胞的增殖能力. 研究结果表明, 膜乳化法制备的载药微球规整, 呈典型的圆球状, 表面光滑, 内部有多孔结构. 当膜孔径为5.1 μm且搅拌转速为500 r/min时, PLA/MSM微球大小更为均一; 当体系中MSM质量分数为8.6%时, 载药量可达到77.43%. 随着膜孔径减小及药物浓度的增加, 体外释放速率加快, 但初期均无明显的突释现象, 约10 d后累积释放量达到89.2%. 细胞实验结果显示, 在膜孔径为5.1 μm且MSM质量分数为8.6%的条件下, 制备的载药微球在细胞培养7 d时表现出明显的促增殖作用.
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| 关 键 词： | 膜乳化 聚乳酸 二甲基砜 微球 生物活性 |
| 收稿时间： | 2012-12-07 |
Preparation of Controlled-release PLA Microspheres Loading Methylsulfonylmethane and Its Biological Activity |
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| WANG Xin-Zhong,LIU Jian-Guo,TANG Yu-Feng,WANG Yu,ZHANG Pei-Biao,CHEN Xue-Si. Preparation of Controlled-release PLA Microspheres Loading Methylsulfonylmethane and Its Biological Activity[J]. Chemical Research In Chinese Universities, 2013, 34(4): 984-991. DOI: 10.7503/cjcu20121108 |
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| Authors: | WANG Xin-Zhong LIU Jian-Guo TANG Yu-Feng WANG Yu ZHANG Pei-Biao CHEN Xue-Si |
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| Affiliation: | 1. First Hospital, Jilin University, Changchun 130021, China;2. Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China |
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| Abstract: | Polylactic acid(PLA) microspheres carrying methylsulfonylmethane(MSM) were prepared by membrane emulsification. The effects of membrane pore size, stirring speed and MSM concentration on microspheres morphology, size, drug loading and in vitro release, as well as cell biological activity were studied using environmental scanning electron microscope(ESEM), inductively coupled plasma atomic emission spectrometer(ICP-AES), in vitro culture of MC3T3-E1 cell and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenylte-trazolium bromide(MTT) method. The study will provide references for the study of the long-acting release agent of MSM. The results showed that the drug-loaded microspheres prepared with membrane emulsification were typical spherical with smooth surface and the internal porous structure. The size and morphology of the microspheres could be affected by membrane pore size, stirring speed and MSM concentration. The drug-loaded microspheres prepared with the membrane pore size of 5.1 μm and a stirring speed of 500 r/min were more uniform in size than others. When the mass fraction of MSM solution was 8.6%, the drug loading of microspheres could be up to 77.43%. The in vitro release rate of MSM could be sped up when the membrane pore size was reduced and the MSM concentration was increased, but the initial burst release for all samples was not obvious, and it reached up to 89.2% after 10 d. The cell experiments showed that cell proliferation of MC3T3-E1 was improved at 7 d cell culture using MSM-loaded microspheres with the membrane pore size of 5.1 μm and MSM mass fraction of 8.6%. The research indicates that the PLA/MSM drug-loaded microspheres has good controlled release characteristics and biological activity, which can be used as a long-acting release formulation of MSM for the treatment of osteoarthritis and application in bone and cartilage tissue engineering. |
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| Keywords: | Membrane emulsification Polylactic Methylsulfonylmethane Microsphere Biological activity |
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