苦参碱纳米粒及其麦胚凝集素修饰产物的制备

摘要

目的 制备苦参碱纳米粒及其麦胚凝集素修饰产物.方法 复乳化-溶剂挥发法制备苦参碱纳米粒,以聚乳酸-羟基乙酸共聚物与苦参碱比例、转速和聚乙烯醇浓度为影响因素,粒径、电位、包封率和载药量为评价指标,通过星点设计优化工艺.碳二亚胺法制备麦胚凝集素修饰苦参碱纳米粒,以碳二亚胺与N-羟基琥珀酰亚胺比例、麦胚凝集素加入量和孵化时间为影响因素,粒径、电位和修饰率为评价指标,通过均匀设计优化工艺.结果 苦参碱纳米粒的最佳条件为聚乳酸-羟基乙酸共聚物与苦参碱比例0.594∶1,转速815 r/min,聚乙烯醇浓度为0.46％,平均粒径、电位、包封率和载药量分别为112.04 nm、-15.38 mV、90.05％和27.14％.其麦胚凝集素修饰产物的最佳条件为碳二亚胺与N-羟基琥珀酰亚胺比例2.8∶0.12,麦胚凝集素加入量3 mg,孵化时间14 h,平均粒径、电位和修饰率分别为474.7 nm、-5.2 mV和69.51％.结论 该制备工艺可靠,所得苦参碱纳米粒及其麦胚凝集素修饰产物性质稳定.%AIM To prepare the matrine nanoparticles and their wheat germ agglutinin-modified product.METHODS Double emulsification-solvent evaporation method was employed to prepare matrine nanoparticles.In consideration of influencing factors of ratio of poly (lactic-co-glycolic acid) to matrine,rotational speed and polyvinyl alcohol concentration,as well as the evaluation indices of particle size,potential,encapsulation efficiency and drug load,the preparation was optimized by central composite design.Wheat germ agglutinin-modified matrine nanoparticles were prepared by carbodiimide method.In addition to the influencing factors of ratio of carbodiimide to N-hydroxysuccinimide,wheat germ agglutinin addition and incubation time,evaluation indices of particle size,potential and modification rate were also taken into account in the preparation optimization by uniform design.RESULTS The optimal conditions for matrine nanoparticles were determined to be 0.594 ∶ 1 for ratio of poly (lactic-co-glycolic acid) to matrine,815 r/min for rotational speed,and 0.46％ for polyvinyl alcohol concentration.The average particle size,potential,encapsulation efficiency and drug loading were 112.04 nm,-15.38 mV,90.05％ and 27.14％,respectively.The optimal conditions for their wheat germ agglutinin-modified product were found to be 2.8 ∶ 0.12 for ratio of carbodiimide to N-hydroxysuccinimide,3 mg for wheat germ agglutinin consumption,and 14 h for incubation time.The average particle size,potential and modification rate were 474.7 nm,-5.2 mV and 69.51％,respectively.CONCLUSION The preparation techniques are reliable,and the matrine nanoparticles and their wheat germ agglutinin-modified product show their stable properties.