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高等学校化学研究 ›› 2016, Vol. 32 ›› Issue (5): 848-853.doi: 10.1007/s40242-016-6155-x

• Articles • 上一篇    下一篇

Effects of the Molecular Weight of PLGA on Degradation and Drug Release In vitro from an mPEG-PLGA Nanocarrier

LIU Rui2, WANG Yan1, MA Yudan1,4, WU Yi3, GUO Yi1, XU Li1   

  1. 1. Key laboratory for Molecular Enzymology and Engineering, Ministry of Education, National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun 130012, P. R. China;
    2. Department of Endocrinology, China-Japan Union Hospital, Jilin University, Changchun 130033, P. R. China;
    3. College of Pharmacy, Jilin University, Changchun 130021, P. R. China;
    4. Jilin Research Institute of Sports Science, Changchun 130022, P. R. China
  • 收稿日期:2016-04-22 修回日期:2016-08-12 出版日期:2016-10-01 发布日期:2016-08-15
  • 通讯作者: GUO Yi, WU Yi E-mail:guoyi@jlu.edu.cn;wuyi@jlu.edu.cn
  • 基金资助:

    Supported by the National Natural Science Foundation of China(Nos.81271697, 81571791, 31571017).

Effects of the Molecular Weight of PLGA on Degradation and Drug Release In vitro from an mPEG-PLGA Nanocarrier

LIU Rui2, WANG Yan1, MA Yudan1,4, WU Yi3, GUO Yi1, XU Li1   

  1. 1. Key laboratory for Molecular Enzymology and Engineering, Ministry of Education, National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun 130012, P. R. China;
    2. Department of Endocrinology, China-Japan Union Hospital, Jilin University, Changchun 130033, P. R. China;
    3. College of Pharmacy, Jilin University, Changchun 130021, P. R. China;
    4. Jilin Research Institute of Sports Science, Changchun 130022, P. R. China
  • Received:2016-04-22 Revised:2016-08-12 Online:2016-10-01 Published:2016-08-15
  • Contact: GUO Yi, WU Yi E-mail:guoyi@jlu.edu.cn;wuyi@jlu.edu.cn
  • Supported by:

    Supported by the National Natural Science Foundation of China(Nos.81271697, 81571791, 31571017).

摘要:

We successfully synthesized four kinds of copolymers with varying molecular weights of poly(lactide-co-glycolide)(PLGA) to yield methoxy-poly(ethylene glycol)-block-poly(lactide-co-glycolide)(mPEG-PLGA) nanocarriers:mPEG-PLGA(3k), mPEG-PLGA(9k), mPEG-PLGA(11k) and mPEG-PLGA(16k). An antitumor drug, 10-hydroxycamptothecin(HCPT), was encapsulated into the mPEG-PLGA nanocarrier cores by self-assembly in dialysis. The lower molecular weight nanocarriers degraded more quickly, resulting in mass loss, pH decline, and a rapid HCPT release rate in vitro. The degradation and drug release of the nanocarriers were dependent on the PLGA molecular weight. However, the larger molecular weight nanocarriers could not increase the loading content and encapsulation efficiency. Considering the antitumor effect of these nanocarriers, the mPEG-PLGA(9k) nanocarrier, which had the highest drug loading content[(7.72±0.57)%] and a relatively high encapsulation efficiency[(22.71±5.53)%], is an optimum agent for drug delivery.

关键词: Poly(lactide-co-glycolide), 10-Hydroxycamptothecin, Nanocarrier, Drug delivery

Abstract:

We successfully synthesized four kinds of copolymers with varying molecular weights of poly(lactide-co-glycolide)(PLGA) to yield methoxy-poly(ethylene glycol)-block-poly(lactide-co-glycolide)(mPEG-PLGA) nanocarriers:mPEG-PLGA(3k), mPEG-PLGA(9k), mPEG-PLGA(11k) and mPEG-PLGA(16k). An antitumor drug, 10-hydroxycamptothecin(HCPT), was encapsulated into the mPEG-PLGA nanocarrier cores by self-assembly in dialysis. The lower molecular weight nanocarriers degraded more quickly, resulting in mass loss, pH decline, and a rapid HCPT release rate in vitro. The degradation and drug release of the nanocarriers were dependent on the PLGA molecular weight. However, the larger molecular weight nanocarriers could not increase the loading content and encapsulation efficiency. Considering the antitumor effect of these nanocarriers, the mPEG-PLGA(9k) nanocarrier, which had the highest drug loading content[(7.72±0.57)%] and a relatively high encapsulation efficiency[(22.71±5.53)%], is an optimum agent for drug delivery.

Key words: Poly(lactide-co-glycolide), 10-Hydroxycamptothecin, Nanocarrier, Drug delivery