Preparation and evaluation of novel purine derivative F7 thermosensitive liposome
- VernacularTitle:新型嘌呤衍生物F7热敏脂质体的制备和评价研究
- Author:
Chun-Yang DU
1
;
Long ZHAO
;
Na GUO
;
Guang-Yu GAO
;
Yu-Ou TENG
;
Ying WANG
;
Ming-Yuan LI
;
Peng YU
Author Information
1. 天津科技大学生物工程学院 300457 天津
- Keywords:
thermosensitive liposome;
pH gradient drug loading method;
entrapment efficiency;
cytotoxicity
- From:
Journal of International Pharmaceutical Research
2018;45(9):714-722
- CountryChina
- Language:Chinese
-
Abstract:
Objective To prepare F7 thermosensitive liposome and evaluate its physicochemical properties, then investigate its cytotoxicity against tumor cells in vitro. Methods The F7 thermosensitive liposome was prepared by the pH gradient active drug loading method using dipalmitoyl phosphatidylcholine myristoyl lyso-phosphocholine and 1, 2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy (polyethylene glycol)-2000 as membrane materials. The encapsulation efficiency and drug loading were determined for the F7 thermosensitive liposome by HPLC. The phase transition temperature of F7 thermosensitive liposome was investigated by differential scanning calorimetry;the liposome morphology was observed by atomic force microscopy;the drug release of liposome was examined by dialysis;and the particle size and zeta potential were measured through Malvern particle size analyzer. The cytotoxicity of F7 and F7 thermosensitive liposome was determined by the MTT method, and the freeze-drying process was optimized using the designexpert software. Results The encapsulation efficiency of F7 thermosensitive liposomes was (97.56±0.22) ％, and the drug loading ratio was (1.51±0.01) ％. The phase transition temperature of F7 thermosensitive liposome was 39.9℃, the zeta potential was (-15.10±0.85) mV, the particle size was (86.94±1.21) nm, and the poly disperse coefficient was 0.17±0.01. Compared with the F7 injection, the F7 thermosensitive liposomes showed a stronger, dose-dependent inhibitory effect on the growth of lung cancer H1299 and breast cancer MCF-7 cells. The freeze-dried powder of liposomes dissolved well with the encapsulation efficiency of 95％ and the particle size of approximately 130 nm. Conclusion The F7 thermosensitive liposome prepared by the pH gradient active drug loading method has high encapsulation efficiency and good stability. The preparation method is simple and feasible for further development of the F7 preparation.
