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苦参碱/壳聚糖/羧甲基壳聚糖载药膜的制备及其体外释放行为分析

摘要:目的 以苦参碱、壳聚糖和羧甲基壳聚糖分别为药物和载体材料制备口腔粘膜溃疡膜剂。方法 常温下通过溶液浇铸法和正交实验法,制备了新型的苦参碱/壳聚糖载药膜和苦参碱/壳聚糖/羧甲基壳聚糖载药膜。通过拉伸试验、SEM、溶胀测试和体外释放等表征了载药膜的力学性能、表面形貌和载药量,确定载药膜制备的最佳条件。结果 当壳聚糖相对分子质量为65万,壳聚糖/甘油质量比为1∶1.4时,载药膜的力学强度最大,拉伸模量高达0.7875 MPa。扫描电镜观察到苦参碱聚集分布在膜的底面,呈不对称分布。体外释放结果表明,载药膜具有较高的载药量和长效缓释性能。随着壳聚糖相对分子质量增大,苦参碱释放时效越长,当壳聚糖的相对分子质量为65万时,载药膜的苦参碱释放时间长达23 h;在载药膜的底面涂覆浓度为1%羧甲基壳聚糖,载药膜的释放时间增加至108 h。结论 载药膜的基质材料天然、绿色、无毒、可降解,制备方法简单易行,避免了大量有机溶剂的使用,可以作为口腔粘膜溃疡膜剂的载体材料,能够显著延长药物的释放时间。

英文摘要:Objective To prepare a drug-loading film using chitosan and carboxymethyl chitosan as the carrier materials for delivering matrine to oral ulcers. Methods Matrine-loading films using chitosan or carboxymethyl chitosan as the carrier materials were prepared by solution casting method and orthogonal experiment at room temperature. The mechanical properties, surface morphology and drug-loading capacity of the drug-loading film were characterized using tensile test, scanning electron microscopy (SEM), swelling test and in vitro drug release test. Results When the molecular weight of chitosan was 650 000 and the mass ratio of chitosan/glycerol was 1∶1.4, the prepared film had the maximum mechanical strength and tensile modulus reaching 0.7875 MPa. SEM observation showed that matrine aggregated at the bottom of the drug-loading film with an asymmetrical distribution. The in vitro drug release test showed that the film had a high drug-loading capacity and a sustained drug release property. The duration of drug release from the drug-loading film was prolonged as the molecular weight of chitosan increased, reaching 23 h when the molecular weight of chitosan was 650 000. The duration of drug release was further increased to 108 h when the bottom of the drug-loading film was coated with a layer of 1% carboxymethyl chitosan. Conclusion The matrix materials of the drug-loading film are natural, green, nontoxic and biodegradable, and the preparation of the film is simple without using large quantities of organic solvents. The novel drug-loading film can obviously prolong the duration of drugs release for better local drug delivery to oral ulcers in a sustained manner.

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[V1] 2017-12-27 12:40:28 chinaXiv:201712.00902V1 下载全文
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