呋喃西林纳米混悬凝胶剂的制备及体外透皮评价  

Preparation of nanosuspension-based gel of nitrofurazone and evaluation of transdermal penetration in vitro

作　　者：刘肖[1,2] 庞建云[1] 刘娟[1] 申宝德[2] 沈成英[2] 连王权 胡春晓[1] 李小芳[1] 袁海龙[2] 

机构地区：[1]成都中医药大学药学院,成都611137 [2]空军总医院药学部,北京100142

出　　处：《中国新药杂志》2017年第24期3003-3008,共6页Chinese Journal of New Drugs

基　　金：全军重大科研计划基金项目[军后综(2016)450号];国家自然科学基金项目(81573697)

摘　　要：目的:制备呋喃西林纳米混悬凝胶剂(nanosuspension-based gel of nitrofurazone,NTZ-nanogel),并进行离体透皮评价。方法:采用微介质研磨法制备呋喃西林纳米混悬剂(nanosuspension of nitrofurazone,NTZ-NS),并进一步制成NTZ-nanogel。以NTZ-nanogel复溶后的粒径(particle size,PS)和多分散指数(polydispersity index,PDI)以及24 h后大鼠离体皮肤滞留量为评价指标,采用正交实验设计对NTZ-nanogel处方中的卡波姆940(载体)、甘油(保湿剂)和NTZ-NS用量进行优化。比较最优NTZ-nanogel和市售凝胶剂的24 h后离体药物累积渗透量和皮肤滞留量。结果:以最优处方工艺:2.0 m L NTZ-NS、0.2 g卡波姆940、2.0 g甘油制得NTZ-nanogel,复溶后PS为(337±12)nm,PDI为(0.268±0.008);24 h后离体药物累积渗透量和皮肤滞留量分别为(212.521±2.285)和(108.375±4.057)μg·cm-2,明显高于市售凝胶(60.567±1.564)和(10.731±0.630)μg·cm^(-2)。结论:将NTZ制成NTZ-nanogel,能显著增加其在体外透皮实验中的累积渗透量和皮肤滞留量,从而提高在局部皮肤的生物利用度。Objective： To prepare nanosuspension-based gel of nitrofurazone （NTZ-nanogel） and investigate its transdermal penetration in vitro. Methods： Nanosuspension of nitrofurazone （NTZ-NS） was prepared by media milling technique and then transformed into gel. The amounts of matrix （ Carbomer 940）, humectant （glycerol） and NTZ-NS in the formulation of NTZ-nanogel were optimized by orthogonal design method, with particle size （PS） and polydispersity index （PDI） after redispersal and the amount of NTZ in the skin after applying NTZ- nanogel for 24 h as evaluation indexes. The in vitro percutaneous permeation and skin deposition of NTZ-nanogel were studied and compared with those of commercial NTZ gel. Results： The PS and PDI of the NTZ-nanogel, prepared by the optimal formulation （2.0 mL of NTZ-NS, 0.2 g of carbomer 940, 2.0 g of glycerol） were （337 ± 12） nm and （0. 268 ±0. 008）, respectively. The amounts of NTZ penetrating skin and depositing in skin after applyingNTZ-nanogelfor 24 h were （212. 521 ±2. 285） and （108. 375 ±4. 057） μg·cm^-2, which were significantly higher than those of the commercial NTZ gel [ （60. 567 ± 1. 564） and （10. 731 ±0. 630） μg·cm^-2].Conclusion： The NTZ-nanogel can increase the amounts of percutaneous permeation and skin deposition of NTZ, thus improving the bioavailability of NTZ in topical skin.

关 键 词：呋喃西林 纳米混悬剂 凝胶剂 体外透皮 

分 类 号：R943[医药卫生—药剂学]