黏膜粘附性缺氧响应型壳聚糖胶束的制备与性能
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南昌大学

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国家自然科学基金项目 (No.21965021 )、江西省自然科学基金(20202BAB204010)


Preparation and properties of mucoadhesive and hypoxia-responsive chitosan micelles
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Nanchang University

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The National Natural Science Foundation of China (No.21965021 )

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    摘要:

    以2-硝基咪唑和6-溴己酸乙酯为原料,合成了缺氧响应型6-(2-硝基咪唑)己酸(NIHA),将其接枝改性壳聚糖合成了取代度分别为3.9%、6.3%和8.9%的两亲性壳聚糖-g-6-(2-硝基咪唑)己酰胺衍生物(CS-NID)。利用1HNMR、UV和FTIR表征了CS-NID的化学结构。CS-NID在水中能自组装形成纳米胶束,并采用DLS、Zeta电位和UV对胶束进行了表征。结果表明,CS-NID胶束的平均粒径为165~190 nm,粒径随NIHA取代度增加而减小。胶束具有优良的储存稳定性、黏膜粘附性、pH响应性和缺氧响应性。阿霉素(DOX)通过疏水相互作用被装载进胶束内,最大载药率(DLC)可达13.3%,最大包封率(DLE)可达44.3%。体外药物释放研究表明,CS-NID胶束具有明显的缺氧响应的药物释放行为,在正常生理环境(常氧,pH 7.4)中24h最大药物释放量仅为42%,而在缺氧的酸性(pH 5.4)条件下,2h内药物释放量高达65%,24h内药物释放量超过92%。

    Abstract:

    The hypoxia-responsive 6-(2-nitroimidazole) hexanoic acid (NIHA) was synthesized using 2-nitroazole and 6-bromohexanoic acid ethyl ester. The amphiphilic chitosan-g-6-(2-nitroimidazole) hexanamide derivatives (CS-NID) with substitution degrees of 3.9%, 6.3% and 8.9% were obtained by grafting NIHA onto the chitosan macromolecule. The structure of CS-NID conjugates was confirmed by 1H NMR, UV and FT-IR. The micelles were obtained by the self-assembly of CS-NID in aqueous solution and characterized by DLS, Zeta potential and UV. The average size of CS-NID micelles was about 165-190 nm and decreased with increasing the substitution degrees of NIHA. The CS-NID micelles exhibited excellent storage stability, mucoadhesion and hypoxia responsiveness. Doxorubicin (DOX) was encapsulated in micelles by the hydrophobic interaction, and the maximum drug loading content (DLC) and loading efficiency (DLE) of CS-NID micelles were 13.3% and 44.3% respectively. In vitro drug release showed that DOX was released from CS-NID micelles with a distinctly hypoxia-responsive manner. Only 42% of loaded Dox was released from the CS-NID micelles under normoxic conditions over 24h. Notably, about 65% of loaded DOX was released from the CS-NID micelles under hypoxic conditions in 2h, and over 92% DOX was released within 24 h under hypoxic conditions.

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袁帆,廖曦,陈献煌,彭志平.黏膜粘附性缺氧响应型壳聚糖胶束的制备与性能[J].精细化工,2022,39(10):

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  • 收稿日期:2022-02-22
  • 最后修改日期:2022-05-19
  • 录用日期:2022-06-06
  • 在线发布日期: 2023-08-14
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