Preparation and characterization of tumor targeting doxorubicin liposomesmodified via click chemistry
10.11665/j.issn.1000-5048.20160613
- VernacularTitle:基于点击化学修饰的肿瘤靶向阿霉素脂质体的制备与表征
- Author:
Yunkai SHANG
1
;
Caoyun JU
;
Daping XIE
;
Can ZHANG
Author Information
1. 中国药科大学新药研究中心，江苏省代谢性疾病重点实验室
- Publication Type:Journal Article
- Keywords:
click chemistry;
liposome;
surface modification;
doxorubicin;
octreotide;
tumor targeting
- From:
Journal of China Pharmaceutical University
2016;47(6):708-713
- CountryChina
- Language:Chinese
-
Abstract:
In this study, octreotide targeting doxorubicin liposome(Dox@Oct-L)was prepared by modifying cholesterol with azide group to prepare azide-modified doxorubicin liposome(Dox@N3-L), followed by click reaction on the vehicle surface with alkyne-modified octreotide. HPLC chromatographic determination showed that octreotide was successfully attached to drug loaded liposome. No significant effect of click modification on the drug loaded within liposome was detected, and the entrapment efficiency of Dox@Oct-L was 99. 8%. Dox@Oct-L showed improved in vitro anti-tumor activity against HepG2 cell when compared with Dox@N3-L, demonstrating that Dox@Oct-L possessed targeting ability against HepG2 cell. Therefore, the click chemistry in modification of drug-loading carrier surface is gentle and efficient, providing the possibility to functional modification in drug-loading carrier surface convieniently.
