化工进展 ›› 2021, Vol. 40 ›› Issue (2): 998-1007.DOI: 10.16085/j.issn.1000-6613.2020-0608

• 生物与医药化工 • 上一篇    下一篇

具有梯级释药性能的核壳型双重载药微球

尹微虹1(), 巨晓洁1,2(), 谢锐1,2, 汪伟1,2, 刘壮1,2, 褚良银1,2   

  1. 1.四川大学化学工程学院,四川 成都 610065
    2.四川大学高分子材料工程国家重点实验室,四川 成都 610065
  • 收稿日期:2020-04-17 修回日期:2020-05-07 出版日期:2021-02-05 发布日期:2021-02-09
  • 通讯作者: 巨晓洁
  • 作者简介:尹微虹(1993—),女,硕士研究生,研究方向为智能化药物控释系统。E-mail:1301462304@qq.com
  • 基金资助:
    四川省青年科技基金杰出青年科技人才项目(2017JQ0027);霍英东教育基金会高等院校青年教师基金(151070)

Dual drug-loaded core-shell microspheres for programmed sequential release

Weihong YIN1(), Xiaojie JU1,2(), Rui XIE1,2, Wei WANG1,2, Zhuang LIU1,2, Liangyin CHU1,2   

  1. 1.School of Chemical Engineering, Sichuan University, Chengdu 610065, Sichuan, China
    2.State Key Laboratory of Polymer Materials Engineering, Sichuan University, Chengdu 610065, Sichuan, China
  • Received:2020-04-17 Revised:2020-05-07 Online:2021-02-05 Published:2021-02-09
  • Contact: Xiaojie JU

摘要:

分别利用单轴和同轴静电喷雾法成功制备出以聚乳酸-羟基乙酸共聚物(PLGA)为内核基质、聚乙烯吡咯烷酮(PVP)为外壳基质的核壳型双重载药微球,其中,抗菌药物盐酸万古霉素(VA)被包封于微球外壳,促成骨药物地塞米松(DA)被负载于微球内核。对载药微球的形貌结构、物理性质和体外释药性能进行了表征和分析。结果表明,当电喷前体PVP浓度为80g/L时,单轴和同轴静电喷雾方法均可得到大小均一、球形良好的核壳型微球。X射线衍射(XRD)和差示扫描量热(DSC)结果表明,DA晶体被成功包封于核壳型微球后转变为无定形状态。基于PVP的水溶性和PLGA的缓慢降解特性,两种核壳型载药微球都实现了壳层VA快速释放、内核DA缓慢释放的梯级释药性能。本文制备得到的具有梯级释药性能的核壳型载药微球在药物控释、组织工程等领域有很好的应用前景。

关键词: 核壳型微球, 单轴静电喷雾, 同轴静电喷雾, 双重载药, 梯级释药

Abstract:

Dual drug-loaded core-shell microspheres were successfully prepared by single and coaxial electrostatic spraying methods under mild conditions with poly(lactic acid-co-glycolic acid) (PLGA) as the core matrix and poly(vinylpyrrolidone) (PVP) as the shell matrix. Vancomycin hydrochloride (VA) as an antibacterial model drug was loaded into the PVP shell and osteogenic dexamethasone (DA) as an osteogenic model drug was loaded into the PLGA core. The results showed that when PVP concentration is 80g/L, both single and coaxial electrostatic spraying methods could obtain core-shell microspheres with good spherical shape and distinct core-shell structure. The results of X-ray diffraction (XRD) and differential scanning calorimeter (DSC) showed that DA is amorphous when it is encapsulated into the microspheres. Based on the water-solubility of PVP and the slow degradation of PLGA, these core-shell microspheres can achieve the rapid-release of VA and the sustained-release of DA. The programmed sequential release behavior of these dual drug-loaded core-shell microspheres endows them with potential applications in the drug controlled-release and tissue engineering.

Key words: core-shell microspheres, single electrostatic spraying, coaxial electrostatic spraying, dual drug-loading, programmed sequential release

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