摘要
目的制备鼻用雷公藤内酯醇纳米脂质体温敏凝胶(TP-NLS-TG),并进行离体黏膜渗透性研究。方法采用高压均质法制备雷公藤内酯醇纳米脂质体(TP-NLS);以泊洛沙姆407(P-407)与泊洛沙姆188(P-188)质量比(A)、氮酮用量(B)和溶胀时间(C)为考察因素,胶凝温度(GT)及TP-NLS-TG的均匀度为评价指标,优选处方,制备TP-NLS-TG。以牛蛙腹部皮肤模拟人体鼻腔黏膜,建立离体黏膜渗透模型,考察TP-NLS-TG的黏膜渗透作用。结果 TP-NLS-TG最优处方中P-407、P-188和氮酮的用量分别为12%、10%、3%,溶胀4 h后,所制备的TP-NLS-TG的GT为32.0℃,均匀度值为0.005,前8.0 h单位面积累积渗透量(Q8)为(9.296 3±0.614 7)μg/cm^2,释放曲线符合Higuchi数学模型。结论按最佳工艺制备的TP-NLS-TG的GT准确,载药均匀,具有较好的黏膜渗透性,可通过蛙皮吸收。
Objective To prepare nasal triptolide nano liposome thermosensitive gel（TP-NLS-TG） and investigate the in vitropenetrability through nasal mucosa. Methods The triptolide nanoliposomes were prepared by high pressure homogenization method, and the ratio of poloxamer 407（P-407） and poloxamer 188（P-188） was selected, using the azone dosage and stirring time as investigation factors. Gelation temperature（GT） and homogeneity of TG（RSD） were used as evaluation indexes, and TP-NLS-TG was prepared by optimized prescription. An isolated mucosal permeability model was established by frog abdominal skin to carry out the in vitro permeation test of TP-NLS-TG in nasal mucosa. Results The best prescription was 12% P-407, 10% P-188, and 3% azone, and swelling time was 4 h. The TP-SLN gelation temperature of the gel was 32 ℃, and the RSD was 0.005%. In the first 8 h, the cumulative infiltration volume per unit area was（9.296 3 ± 0.614 7） μg/cm^2, and the release curve in line with the Higuchi mathematical model. Conclusion The triptolide nano liposome gel prepared by the optimum technology has an accurate gelling temperature, and uniform content, which has good permeability, can be absorbed through the frog skin.
出处
《中草药》
CAS
CSCD
北大核心
2017年第17期3517-3522,共6页
Chinese Traditional and Herbal Drugs
基金
福建省科技计划(重点)项目(社会发展引导性项目)(2014Y0051)
福建省自然科学基金项目(2017J01141
2017J01142)
福建省省属公益类科研院所基本科研专项(2015R1031-4
2016R1029-3)
福建省医学创新科研项目(2017-CX-12
2017-CXB-4)
福建省中医药科研项目(2017FJZYZY101)
关键词
雷公藤内酯醇
纳米脂质体
温敏凝胶
胶凝温度
黏膜渗透
均匀度
triptolide
nano liposome
thermosensitive gel
gelation temperature
penetrability
content uniformity
作者简介
通信作者 陈洪，副主任医师。Tel：18060618866E-mail：chenhong_ls@sina．com
通信作者 林馁 Tel：13605948318E-mail：linsui_syy@sina．com．cn
