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透明质酸修饰的地塞米松核壳纳米粒的制备及表征

王静, 甘莉, 甘勇, 刘建平

王静, 甘莉, 甘勇, 刘建平. 透明质酸修饰的地塞米松核壳纳米粒的制备及表征[J]. 中国药科大学学报, 2013, 44(2): 117-123. DOI: 10.11665/j.issn.1000-5048.20130204
引用本文: 王静, 甘莉, 甘勇, 刘建平. 透明质酸修饰的地塞米松核壳纳米粒的制备及表征[J]. 中国药科大学学报, 2013, 44(2): 117-123. DOI: 10.11665/j.issn.1000-5048.20130204
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WANG Jing, GAN Li, GAN Yong, LIU Jianping. Preparation and characterization of hyaluronic acid-modified dexamethasone core-shell liponanoparticles[J]. Journal of China Pharmaceutical University, 2013, 44(2): 117-123. DOI: 10.11665/j.issn.1000-5048.20130204
Citation: WANG Jing, GAN Li, GAN Yong, LIU Jianping. Preparation and characterization of hyaluronic acid-modified dexamethasone core-shell liponanoparticles[J]. Journal of China Pharmaceutical University, 2013, 44(2): 117-123. DOI: 10.11665/j.issn.1000-5048.20130204
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透明质酸修饰的地塞米松核壳纳米粒的制备及表征

  • 1.

    中国药科大学药剂学教研室

  • 2.

    中国科学院上海药物研究所

基金项目: 国家自然科学基金资助项目(No.81102387);上海市自然科学基金资助项目(No.11ZR1444700)

Preparation and characterization of hyaluronic acid-modified dexamethasone core-shell liponanoparticles

摘要

    摘要
  • 摘要: 探讨透明质酸修饰的地塞米松核壳纳米粒的制备方法，并对其理化性质及释药行为等进行考察。首先采用薄膜分散水化-挤膜法制备核壳纳米粒（LCS-NPs），单因素研究多种处方组成对LCS-NPs性质的影响。随后用透明质酸（HA）与二油酰磷脂酰乙醇胺（DOPE）的键合物（HA-DOPE）修饰LCS-NPs，制得HA-LCS-NPs。采用粒度仪和投射电镜分别考察HA-LCS-NPs的粒径、电位、微观形态和结构组成。以地塞米松为模型药物，考察载药HA-LCS-NPs的包封率和体外释药行为。HA-LCS-NPs在透射电镜下呈现清晰的核壳结构，平均粒径为（189±10.3）nm。HA-LCS-NPs对地塞米松的包封率和载药量分别为27.4%和5.9%，72 h累积释放率低于40%。结果表明，薄膜分散水化-挤膜法制备的LCS-NPs经HA-DOPE修饰，可得到具有明显核壳结构的纳米载体，并实现有效的药物包裹和良好的缓释特征。
    Abstract: The aim of this study was to prepare hyaluronic acid-modified dexamethasone-loaded core-shell liponanoparticles and to investigate their physicochemical properties as well as in vitro drug release behavior.Chitosan nanoparticles (CS-NPs) were prepared by ionic gelation,and then the freshly prepared CS-NPs suspension was used to hydrate the dry lipid film to form core-shell liponanoparticles (LCS-NPs).Hyaluronic acid (HA) was conjugated with 1,2-dioleoyl-sn-glycero-3-phosphor-ethanolamine (DOPE) to form HA-DOPE,which was then incubated with LCS-NPs to get HA-modified LCS-NPs (HA-LCS-NPs).The particle size,Zeta potential,morphology,and composition of HA-LCS-NPs were evaluated.In vitro drug release of HA-LCS-NPs was investigated using dexamethasone as the model drug.Encapsulation efficiency and drug loading capacity of dexamethasone loaded HA-LCS-NPs were detected via ultracentrifugation.HA-LCS-NPs exhibited clear core-shell structure as can be seen in the TEM images,average size distribution of which was (189±10.3) nm.The encapsulation efficiency and drug loading capacity of dexamethasone-loaded HA-LCS-NPs were 27.4% and 5.9%,respectively. The cumulative release of dexamethasone from HA-LCS-NPs was less than 40% at 72 h.The core-shell liponanoparticles could be successfully prepared by hydrating dry lipid film with suspension of chitosan nanoparticles,followed by modification with HA-DOPE.Dexamethasone could be successfully encapsulated in the HA-LCS-NPs and exhibited sustained release behavior.
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  • 刊出日期:  2013-04-24

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