负载盐酸阿霉素的氯化壳聚糖-海藻酸微粒的制备及释药性能
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安徽省自然科学基金项目(2208085MB32);安徽省重点研究与开发计划项目(202004a06020021);安徽省高校自然科学研究重点项目(KJ2020A0049);国家自然科学基金项目(21606002);绿色高分子材料安徽省重点实验室资助项目(2022KF009)


Preparation and Drug Release Performance of Chitosan Hydrochloride-Alginate Microparticles Loaded with Doxorubicin Hydrochloride
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    摘要:

    采用均质乳化法制备了氯化壳聚糖-海藻酸微粒,以盐酸阿霉素为模型药物,分别以Ca2+,Zn2+和Cu2+ 3 种金属阳离子为交联剂,探究了3 种交联剂形成的微粒对药物装载能力及释放性能的影响。研究表明,负载有盐酸阿霉素的氯化壳聚糖-海藻酸钙、氯化壳聚糖-海藻酸锌、氯化壳聚糖-海藻酸铜3 种微粒,其形貌圆整,大小均一,平均粒径分别为2.56 μm,2.78 μm 和1.81 μm,包封率分别为97.22%,98.01%和41.29%。在pH=6.8 的PBS 溶液中恒温恒速进行药物释放,3 组微粒都具有明显的缓释特征,且金属阳离子的种类对包封率及缓释效果都具有显著性影响。研究表明,3 种金属阳离子均可用作制备微粒的交联剂,考虑到毒性,以Ca2+和Zn2+为交联制得的微粒适宜作为药物微载体,可为盐酸阿霉素药物载体的设计提供良好的思路。

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    Chitosan hydrochloride-alginate microparticles were prepared by homogeneous emulsification method. Choosing doxorubicin hydrochloride as model drug, three types of microparticles were fabricated using three kinds of metal cations (Ca2+, Zn2+, Cu2+) as cross-linkers respectively, the effects of different metal cations on the drug loading capacity and drug release efficiency of microparticles were investigated. The results manifest that chitosan hydrochloride- calcium alginate, chitosan hydrochloride- zinc alginate and chitosan hydrochloride- copper alginate microparticles loaded with doxorubicin hydrochloride are round in shape and uniform in size, the average microparticles size is 2.56 μm, 2.78 μm and 1.81 μm, and the entrapment efficiency is 97.22%, 98.01% and 41.29%, espectively. The drug release was simulated in PBS (pH= 6.8) at constant temperature and speed, and it is confirmed that the types of metal cations have significant effects on the entrapment efficiency and drug release property. These results indicate that all three groups of metal cations could be used as cross-linking agents for the preparation of the microparticles. Considering of toxicity, the microparticles that cross-linked by Ca2+, Zn2+ could be more suitable used as micro- drug carriers, which could provide a new strategy in designing doxorubicin hydrochloride- loaded drug vehicles.

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刘彩霞,吴志,夏智超,吴庆喜.负载盐酸阿霉素的氯化壳聚糖-海藻酸微粒的制备及释药性能[J].高分子材料科学与工程,2022,38(9):7-15.

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  • 在线发布日期: 2022-11-23
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