Synthesis of paclitaxel palmitate and the formulation optimization of its liposomes
10.12206/j.issn.2097-2024.202404062
- VernacularTitle:紫杉醇棕榈酸酯的合成及其脂质体的制备与处方研究
- Author:
Bingchen CHEN
1
;
Sizhen WANG
;
Beibei GUO
;
Feng YANG
Author Information
1. 海军军医大学:第一附属医院肛肠外科,上海 200433
- Keywords:
paclitaxel;
palmitic acid;
liposomes;
prodrug;
pharmaceutical research
- From:
Journal of Pharmaceutical Practice and Service
2024;42(9):379-384,410
- CountryChina
- Language:Chinese
-
Abstract:
Objective To improve the cellular uptake efficiency and the therapeutic effect through the structural modification of paclitaxel(PTX)and the preparation of corresponding liposomes.Methods The prodrug of paclitaxel,PTX-PA,was prepared by esterification reaction,and the quantitative detection method of PTX-PA was established.Next,the optimal formulation and preparation of PTX-PA/Lip was obtained through single factor screening based on their appearance,particle size,and encapsulation efficiency.Results The PTX-PA was successfully synthesized,and the established HPLC quantitative analysis method for PTX-PA met the methodological requirements.After the optimal preparation and formulation research through single factor screening,the particle size of optimized PTX-PA/Lip was(62.75±1.81)nm with a PDI of(0.076±0.02),while the drug encapsulation rate reached more than 90%.Conclusion This research successfully prepared palmitic acid modified paclitaxel liposomes based on nanotechnology,enhancing the drug delivery efficiency of paclitaxel and laying the foundation for the pharmacodynamics research of PTX-PA.
