3种尼古丁囊泡制剂的制备及体外评价  

Preparation and in vitro evaluation of three nicotine transdermal vesicles

作　　者：王慧[1] 邵青 张燕[1] 张玲[2] 吴强驹[1] WANG Hui;SHAO Qing;ZHANG Yan;ZHANG Ling;WU Qiang-ju(Xi'an Mental Health Center,Xi'an 710061,China;Honghui Hospital Afiliated to Xi'an Jiaotong University,Xi'an 710000,China)

机构地区：[1]西安市精神卫生中心,西安710061 [2]西安交通大学附属红会医院,西安710000

出　　处：《中国新药杂志》2024年第10期1043-1049,共7页Chinese Journal of New Drugs

基　　金：陕西省自然科学基金资助项目/陕西省创新能力支撑计划项目(2022PT-03);西安市医学研究项目:基于药物及生化分析技术的抗精神分裂症药物精准化应用评价体系研究(23YXYJ0006);西安市科学技术局科技创新平台建设项目(201805051ZD2CG35)。

摘　　要：目的:制备尼古丁乙醇脂质体、二元醇脂质体和传递体,并对其进行皮肤渗透性比较,筛选最佳经皮转运囊泡,优化药物的经皮转运。方法:注入法制备尼古丁乙醇脂质体及二元醇脂质体,薄膜分散法制备传递体,以粒径的形态、粒径大小、Zeta电位值及包封率为考察指标,采用Franz扩散池对3种囊泡进行处方优化及筛选,最终筛选出透皮力最强的二元醇脂质体(乙醇∶丙二醇=5∶5,w/w),共聚焦激光扫描显微镜(CLSM)比较3种脂质囊泡经小鼠皮肤的透皮深度。结果:当乙醇∶丙二醇=5∶5(w/w)时,二元醇脂质体最稳定,包封率最高(86.13±1.40)%,粒径最小(106.00±11.0)nm,透皮深度最大(180μm),且乙醇脂质体、二元醇脂质体和传递体在皮肤24 h累计渗透百分数分别为脂质体(对照品)的4.07(P<0.05),8.62(P<0.01)和2.83(P>0.05)倍,CLSM实验表明,该二元醇脂质体对罗丹明B的穿透深度和荧光强度远大于乙醇脂质体和传递体。结论:该二元醇脂质体与乙醇脂质体及传递体相比,能更有效地携带药物通过皮肤,而传递体能显著增加药物的皮内滞留量。Objective:To prepare nicotine-ethanol liposomes,diol liposomes and transporters,compare their skin permeability,screen the best transdermal transport vesicles and optimize the transdermal transport of drugs.Methods:Nicotine-ethanol liposomes and diol liposomes were prepared by injection method,and the transfer bodies were prepared by thin film dispersion method.Based on the morphology,size of particle size,zeta potential value and encapsulation rate,the prescriptions of three kinds of vesicles were optimized and screened by Franz diffusion cell,and confocal laser scanning electron microscopy(CLSM)was used to compare the transdermal depth of three lipid vesicles.Results:When ethanol:propylene glycol=5:5(w/w),the diol liposome was the most stable,the encapsulation rate was the highest(86.13±1.40)%,the particle size was the smallest(106.00±11.0)nm,the transdermal depth was the largest(180μm).The 24 h cumulative penetration percentages of the ethanol liposome,diol liposome(ethanol:propylene glycol=5:5,w/w)and transporters in the skin were 4.07(P<0.05),8.62(P<0.01)and 2.83(P>0.05)times of that of the standard liposomes,respectively.The CLSM experiment showed that the penetration depth and fluorescence intensity of Rhodamine B in ethanol:propylene glycol=5:5(w/w)diol liposomes were much higher than those in ethanol liposomes and transporters.Conclusion:Diol liposomes.(ethanol:propylene glycol=5:5,w/w)carry drugs through the skin more efficiently than ethanol liposomes and transporters,which significantly increase the dermal retention of drugs.

关 键 词：尼古丁 乙醇脂质体 二元醇脂质体 共聚焦激光扫描显微镜 经皮转运 

分 类 号：R943[医药卫生—药剂学]