Optimization of preparation technology of baicalin lipid nano foam aerosol
- VernacularTitle:黄芩苷脂质纳米泡沫气雾剂的制备工艺优化
- Author:
Hongfang YU
1
;
Renjie WU
1
;
Jiafeng ZOU
2
;
Jiazhen ZHU
3
;
Wendong YAO
1
;
Zheng SHI
1
Author Information
1. Dept. of Pharmacy，the First Affiliated Hospital of Zhejiang Chinese Medical University，Hangzhou 310018，China
2. Hangzhou SoliPharma Limited Liability Company，Hangzhou 310018，China
3. College of Pharmaceutical Science，Zhejiang Chinese Medical Uni versity，Hangzhou 311400，China
- Publication Type:Journal Article
- Keywords:
baicalin;
lipid nano foam aerosol;
Box-Behnken design-response surface methodology;
technology optimization
- From:
China Pharmacy
2022;33(8):943-949
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To optimize the pr eparation technology of the baicalin lipid nano foam aerosol （BC-LN-FA）. METHODS Baicalin lipid nanoparticle （BC-LN）and BC-LN-FA were prepared by the thin film dispersion method and homogeneous emulsification method ，respectively，using baicalin （BC） as the model drug. The preparation technology was optimized by Box-Behnken design-response surface methodology using particle size and encapsulation efficiency （EE）as indexes ，with dosage ， emulsifier dosage ，co-emulsifier dosage and homogenization time as factors. The morphology ，particle size ，polymerdispersity index（PDI），EE，the viscosity ，the foam dissolution rate and in vitro transdermal release of BC-LN-FA were characterized. RESULTS The optimal technology included 25 mg BC ，40 mg emulsifier （mass ratio of stearic acid-soybean lecithin-glycerol was 1∶1∶1），30 mg co-emulsifier （mass ratio of octadecanol-lactic acid was 1∶1），homogenization time of 20 min. Results of 3 times of validation tests showed that particle size of prepared BC-LN-FA was （151.70±2.40）nm，EE was （68.62±1.16）％；the deviation of them from the predicted value （particle size of 150.80 nm，EE of 67.02％）were 0.60％ and 2.39％ respectively. The BC-LN-FA prepared by the optimal process was light yellow opalescence ，uniform in particle size and round-like in shape. The viscosity，the foam dissolution rate ，the content of BC and PDI were （122.92±5.09）mPa·s，（65.32±3.22）％，（7.01±0.12）％ and（0.199±0.006），respectively. At 48 h，the cumulative release rates of BC-LN-FA in phosphate buffer saline （PBS）at pH 7.4， 6.8，5.0 were（54.12±2.69）％，（57.85±4.25）％ and（59.47±1.83）％，respectively；those of free BC in PBS at pH 7.4 was only （15.04±1.43）％. CONCLUSIONS The optimized technology is stable and feasible. Prepared BC-LN-FA has a uniform particle size，high digestion rate and certain viscosity.
