Preparation and cellular uptake study of anemoside B4 and PD-L1 siRNA co-delivered cRGD-modified targeting liposomes
- VernacularTitle:白头翁皂苷B4和PD-L1siRNA共递送cRGD修饰靶向脂质体的制备及体外细胞摄取研究
- Author:
Anping WAN
1
;
Jing ZHANG
2
;
Xiong ZHOU
1
;
Yulin FENG
1
;
Jun LIU
1
;
Yao HE
1
,
2
;
Xiang LI
1
Author Information
1. National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine，Jiangxi University of Chinese Medicine，Nanchang 330006，China
2. Key Laboratory of Modern Preparation of TCM of Ministry of Education，Jiangxi University of Chinese Medicine，Nanchang 330004，China
- Publication Type:Journal Article
- Keywords:
anemoside B4;
PD-L1;
siRNA;
liposome;
cellular uptake
- From:
China Pharmacy
2023;34(1):18-22
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To prepare anemoside B4 （AB4） and programmed cell death ligand 1 （PDL1） siRNA （siP） co- delivered cRGD-modified targeting liposomes （AB4/siP-c-L）， and to study the cellular uptake in vitro. METHODS The cRGD- modified AB4-loaded targeted liposomes （AB4-c-L） were prepared by ethanol injection. AB4-c-L was mixed with 20 nmol/L siP in the same volume and AB4/siP-c-L was obtained through electrostatic adsorption. The particle size， Zeta potential， morphology， encapsulation efficiency and drug content， in vitro release behavior and serum stability of AB4/siP-c-L were investigated by laser scattering particle size tester， transmission electron microscopy， ultrafiltration centrifugation， dialysis and agar-gel electrophoresis block test. Cellular uptake of AB4/siP-c-L by Lewis lung cancer cells LLC and its intracellular localization were evaluated by flow cytometry and confocal laser scan technique. RESULTS The average particle size of AB4/siP-c-L was （187.4±3.1） nm， and the Zeta potential was （33.5±1.4） mV. AB4/siP-c-L was spheroidal in shape. The encapsulation efficiency and content of AB4 were （95.2±0.4） % and （1.0±0.2） mg/mL， respectively. AB4/siP-c-L could better package siP， and exhibited good serum stability， obvious pH sensitivity and sustained release property. The uptake rate of AB4/siP-c-L by LLC cells was significantly higher than that of free drug， and was able to accumulate in cytoplasm. CONCLUSIONS AB4/siP-c-L can effectively realize the co-loading of AB4 and gene drug siP， which has certain in vitro targeting to LLC cells.
