Formulation and technology of oxymatrine-astragaloside IV coloaded liposomes based on quality by design
10.16438/j.0513-4870.2023-0515
- VernacularTitle:基于质量源于设计 (QbD) 理念的氧化苦参碱-黄芪甲苷共载脂质体处方工艺研究
- Author:
Liang-yin WEI
1
;
Xia LI
1
;
Hong WANG
1
;
Lin-qing HUANG
1
;
Cong-yan LIU
1
;
Yan CHEN
1
Author Information
1. Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing 210028, China; Multi-component of Traditional Chinese Medicine and Microecology Research Center, Jiangsu Provincial Academy of Chinese Medicine, Nanjing 210028, China
- Publication Type:Research Article
- Keywords:
quality by design;
liposome;
high-pressure homogenization;
astragaloside IV;
oxymatrine
- From:
Acta Pharmaceutica Sinica
2024;59(1):232-242
- CountryChina
- Language:Chinese
-
Abstract:
To optimize the formulation and technology of oxymatrine-astragaloside IV coloaded liposomes (Om-As-Lip) based on quality by design (QbD) principles, and further to verify the feasibility of its amplification process, Om-As-Lip was prepared by ethanol injection combined with pH gradient method. The critical material attributions of Om-As-Lip were evaluated by dual-risk analysis tools and Plackett-Burman design (PBD). The formulation of Om-As-Lip was further optimized with the Box-Behnken design (BBD). The design space was also established based on the contour plots of BBD. In order to further investigate the amplification process of Om-As-Lip, the critical process parameters of high-pressure homogenization (HPH) were optimized by single-factor test, and the quality of the final product was also evaluated. The results of risk analysis and PBD confirmed that the astragaloside concentration, cholesterol concentration, and phospholipid ratio (HSPC∶SPC) were the ctitical material attributes. The model established by BBD had a good predictability, and the optimized mass ratio of As to phospholipids was 1∶40, cholesterol to phospholipids was 1∶10, HSPC to SPC was 51∶9. The design space of Om-As-Lip was as follows: the ratio of cholesterol to phospholipids was 1∶12-1∶5 and HSPC to SPC was 1∶7-17∶3. The optimized high-pressure homogenization pressure was 600 bar, temperature was 4 ℃, and cycle times was 6 times for HPH-Om-As-Lip. The quality of Om-As-Lip prepared based on the QbD concept can meet the expected CQAs, and the formulation and technology established can provide a reliable experimental basis for its future development and applications.
