模板剂法与致孔剂法对多孔麦芽糊精结构及药物递送影响研究

Effects of template and pore-forming agent method on the structure and drug delivery of porous maltodextrin

本研究以麦芽糊精为原料、1%~5%聚乙烯比咯烷酮K30为模板剂、1%~5%碳酸氢铵为致孔剂、姜黄素和布洛芬为模型药物,分别采用模板剂法和致孔剂法制备多孔麦芽糊精,对不同工艺制备多孔麦芽糊精结构和药物递送行为进行全面表征。结果显示,致孔剂法制备多孔麦芽糊精具有更大比表面积(6.4494 m^(2)·g^(-1))和孔径(32.8042 nm),明显优于模板剂法(3.6702 m^(2)·g^(-1),15.2785 nm)。致孔剂法制备多孔麦芽糊精吸附姜黄素过程符合准一级吸附动力学模型,吸附布洛芬过程则符合准二级吸附动力学模型,而模板剂法制备多孔麦芽糊精吸附两种模型药物过程均符合准一级吸附动力学模型。溶出行为表明两种工艺制备多孔麦芽糊精均可显著改善难溶性药物溶出行为,且药物释放均符合Peppas释放动力学模型和扩散机制,但模板剂法制备多孔麦芽糊精具有更快释药速率。喷嘴口径改变对多孔麦芽糊精吸附模型药物过程和药物释放行为均无明显影响。综上,两种不同工艺制备多孔麦芽糊精均有利于难溶性药物的递送,其中以模板剂法制备多孔麦芽糊精对难溶性药物的递送效果最优。该研究可为多孔粒子的制备提供理论依据,促进多孔粒子在难溶性药物中的应用,提高难溶性药物的生物利用度。

This study using maltodextrin as raw material,1%−5%polyvinylpyrrolidone K30 as template agent,1%−5%ammonium bicarbonate as pore-forming agent,curcumin and ibuprofen as model drugs.Porous maltodextrin was prepared by template and pore-forming agent methods,respectively.The structure and drug delivery behavior of porous maltodextrin prepared by different technologies were comprehensively characterized.The results showed that the porous maltodextrin prepared by pore-forming agent method had larger specific surface area(6.4494 m^(2)·g^(-1))and pore size(32.8042 nm),which was significantly better than that by template agent method(3.6702 m^(2)·g^(-1),15.2785 nm).The adsorption kinetics between porous maltodextrin prepared by pore-forming agent method and curcumin were suitable for quasi-first order adsorption kinetic model,and that between porous maltodextrin and ibuprofen were suitable for quasi-second order adsorption kinetic model.While the adsorption kinetics between porous maltodextrin prepared by template agent method and two model drugs were both suitable for the quasi-first order adsorption kinetic model.In addition,the dissolution behavior analysis showed that the porous maltodextrin prepared by the two technologies can significantly improve the dissolution behavior of insoluble drugs,and the drug release was both carried out by diffusion mechanism,which suitable for the Peppas kinetic release model,but the porous maltodextrin prepared by template agent method had a faster release rate.The change of nozzle diameter had no significant effect on the adsorption process and drug release behavior of porous maltodextrin.In conclusion,the porous maltodextrins prepared by two different technologies were both beneficial to the delivery of insoluble drugs,and the template agent method was the best for delivery of insoluble drugs.This study can provide theoretical basis for the preparation of porous particles,promote the application of porous particles in insoluble drugs,and improve the bioavailability of insoluble drugs.