卢立康唑纳米晶凝胶的制备与评价  

Preparation and evaluation of Luliconazole Nanocrystal Gels

作　　者：姜娟娟 龚拥军 JIANG Juanjuan;GONG Yongjun(Department of Pharmacy,Xiaogan First People's Hospital,Xiaogan 432000,China)

机构地区：[1]孝感市第一人民医院药剂科,孝感432000

出　　处：《西北药学杂志》2023年第3期121-125,共5页Northwest Pharmaceutical Journal

摘　　要：目的 制备卢立康唑纳米晶凝胶,并通过体外透皮实验评价其质量。方法 通过单因素实验确定卢立康唑纳米晶的处方组成,并以碾磨时间(x_(1))和碾磨速度(x_(2))作为自变量,以卢立康唑纳米晶的粒径分布(y)作为因变量,通过2因素3水平中心复合实验设计优化介质碾磨法制备卢立康唑纳米晶的工艺参数;以卡波姆940作为凝胶载体将卢立康唑纳米晶制备成凝胶;考察卢立康唑纳米晶的微观形态,比较卢立康唑纳米晶及其凝胶的体外释药速率;用Franz扩散池法比较卢立康唑纳米晶凝胶与卢立康唑乳膏的体外透皮性能。结果 以聚乙烯醇和聚乙烯己内酰胺-聚醋酸乙烯酯-聚乙二醇接枝共聚物(soluplus^(?))作为稳定剂,选择介质碾磨时间为14 h,碾磨速度为2 400 r·min^(-1),制备的卢立康唑纳米晶的平均粒径为(374.6±9.6) nm,多聚分散系数为(0.298±0.007),Zeta电位为(-10.9±0.5) mV,呈不规则颗粒状分布;体外释放实验结果显示,卢立康唑纳米晶释药迅速,而凝胶中的药物能够持续缓慢释放;体外透皮实验结果显示,卢立康唑纳米晶凝胶在12 h内药物单位面积累积透皮量明显高于卢立康唑乳膏,其在皮肤内的药物滞留量是卢立康唑乳膏的3.1倍。结论 将卢立康唑制备成纳米晶凝胶,可以显著提高药物累积透皮量及在皮肤中的滞留量,有望提高卢立康唑的治疗效果。Objective To prepare Luliconazole Nanocrystal Gels and to evaluate the gels􀆳quality by in vitro transdermal experiment.Methods The formulation composition of luliconazole nanocrystals was determined by single factor experiment.The preparation process parameters of luliconazole nanocrystals prepared by media milling method were optimized by 2 factors and 3 levels“central composite experimental design”with the milling time(x1)and milling speed(x2)as independent variables and the particle size distribution(y)of luliconazole nanocrystals as the dependent variable.The luliconazole nanocrystals were prepared into gels by using carbomer 940 as the gel carriers.The microscopic morphology of the luliconazole nanocrystals was investigated,and the in vitro drug release rates of luliconazole nanocrystals and their gels were compared.The in vitro transdermal properties of luliconazole nanocrystal gels and luliconazole cream were compared by Franz diffusion cell method.Results Luliconazole nanocrystals were prepared by polyvinyl alcohol(PVA)and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer(soluplus􀆿)as stabilizers,the milling time was 14 hours and the milling speed was 2400 r·min-1.The average particle size of luliconazole nanocrystals was(374.6±9.6)nm,the PDI was(0.298±0.007),and the Zeta potential was(-10.9±0.5)mV.The morphology of luliconazole nanocrystals was irregular granular distribution.The in vitro release results showed that luliconazole nanocrystals released rapidly,while luliconazole in the gels could be released continuously and slowly.The in vitro transdermal results showed that the cumulative drug penetration per unit area of Luliconazole Nanocrystal Gels within 12 hours was significantly higher than that of luliconazole cream,and its drug retention in the skin was 3.1 times that of luliconazole cream.Conclusion Luliconazole Nanocrystal Gels could significantly increase the cumulative drug penetration and retention in skin,which was expected to improve the efficacy of

关 键 词：卢立康唑 纳米晶 介质碾磨法 凝胶 透皮性能 

分 类 号：R94[医药卫生—药剂学]