特产研究2024，Vol.46Issue(2)：36-46,11.DOI:10.16720/j.cnki.tcyj.2024.042
血根碱壳聚糖微球的制备工艺优化及体内外性能研究
Preparation Process Optimization and in Vitro and in Vivo Properties of Sanguinarine Chitosan Microspheres
摘要
Abstract
To investigate the optimal preparation of sanguinarine chitosan microspheres,and and to characterize the appearance and particle size of the microspheres and study them in vitro and in vivo.An HPLC method for the determination of sanguinarine was established.San-guinarine chitosan microspheres were prepared by emulsion crosslinking method.The formulation was optimized by single factor test and central composite design response surface method with drug loading,encapsulation efficiency and average particle size as evaluation indi-cators.The appearance and morphology of microspheres were observed by microscope and scanning electron microscope,and the particle size and distribution of microspheres were determined by laser particle sizer.Sanguinarine bulk drug solution and sanguinarine chitosan microspheres solution at different time points were obtained by dynamic dialysis method,and the in vitro release rates of the two solutions were investigated.Finally,the pharmacokinetic equation was fitted.Different groups of mice were injected with sanguinarine raw material solution and sanguinarine microsphere solution,and tissue blood was taken at different times for determination to observe the distribution and targeting in vivo.The curve equation of sanguinarine HPLC was y=2.530 0x+43.323 1(R2=0.999 8,linear range 10.0～50.0 μg/mL).The optimal formula was obtained by single factor test and central composite design response surface method:sanguinarine dosage 60 mg,chitosan dosage 70 mg,emulsifier dosage 5％,pentanediol dosage 0.25mL,water oil volume ratio 3:10,acetic acid concentration 2％,stirring speed 500 r/min and crosslinking time 3.5 h.The morphology of sanguinarine chitosan microspheres was observed to be nearly spherical and the surface was smooth,and the average particle size was determined to be(8.17±0.16)μm,with the particle size distribution ranging from 2 to 20 μm.In vitro release showed that sanguinarine chitosan microspheres were released more slowly than haematoxylin API,and the Ritger-Peppas equation fitted better(R2=0.980 8).Sanguinarine microspheres have obvious sustained-release effect in mice,and have different degrees of targeting in lungs and liver.Sanguinarine chitosan microspheres have obvious sustained-release effect in vitro,and the distribution in mice has certain targeting and sustained-release properties.关键词
血根碱/微球/星点设计-响应面法/体外释放/缓释/靶向性Key words
sanguinarine/microspheres/central composite design-response surface method/in vitro release/slow-release/targeting分类
医药卫生引用本文复制引用
李春梅,史彤辉,陈旭,张馨元,周长胜..血根碱壳聚糖微球的制备工艺优化及体内外性能研究[J].特产研究,2024,46(2):36-46,11.基金项目
黑龙江省哲学社会科学研究规划项目(21KSE330) （21KSE330）
2023年度黑龙江省中医药经典普及化专项项目(ZYW2023-077) （ZYW2023-077）
2023年度黑龙江省博士后科研启动金项目(BS0051) （BS0051）
