Preparation of Chelerythrine Nanoparticles and Evaluation of Anti-melanoma Activity in vitro
- VernacularTitle:白屈菜红碱纳米粒的制备及体外抗黑色素瘤活性评价
- Author:
Jin YANG
1
;
Wei HAN
1
;
Yongping ZHANG
1
;
Xiaolan CHEN
1
;
Zhe LI
2
,
3
;
Jie LIU
1
;
Jinglan WU
1
Author Information
1. College of Pharmacy，Guizhou University of Traditional Chinese Medicine，Guiyang 550025，China
2. College of Basic Medicine，Guizhou University of Traditional Chinese Medicine，Guiyang 550025，China
3. Innovation Research and Development Center of Veterinary Traditional Chinese Medicine Preparations，Guizhou University of Traditional Chinese Medicine，Guiyang 550025，China
- Publication Type:Journal Article
- Keywords:
Chelerythrine;
Melanoma;
Anti-tumor effect
- From:
China Pharmacy
2021;32(24):2980-2986
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE：To prepare chelerythrine nanoparticles（CHE-NPs），optimize their formulation ，and evaluate its drug release behavior in vitro and its inhibitory effect on melanoma. METHODS ：Using methoxy polyethylene glycol-poly （lactic-co- glycolic acid ）（mPEG-PLGA）as carrier ，CHE-NPs were prepared by the nano-precipitation method. HPLC method and dialysis bag method were used to determine entrapment efficiency and drug loading. The formulation of CHE-NPs was optimized by Box-Behnken response surface design using overall desirability （OD）of them as dependent variables ，CHE dosage ，mPEG-PLGA concentration and poloxamer 188（F68）concentration as independent variables. The particle size and Zeta potential of CHE-NPs prepared by the optimal formulation were detected ；the characteristics of drug release in vitro were investigated ；the effects of CHE and CHE-NPs on survival rate of mice B 16 melanoma cells were compared ，and median inhibition concentrations （IC50）of them were calculated. RESULTS ：The optimal formulation included CHE of 2 mg，mPEG-PLGA of 13 mg/mL，F68 of 1.8％. Average entrapment efficiency rate of CHE-NPs prepared by the optimal formulation was （80.18±1.11）％，average drug loading was （11.36±0.28）％，average OD value was 0.96±0.04 [the relative deviation from predicted value （0.90）of OD was 6.67％]； particle size was （113.1±1.40）nm，and Zeta potential was （－21.6±0.29）mV；polydispersity index was 0.07±0.01（n＝3）； accumulative release rates of CHE control and CHE-NPs were 90.87％ and 68.68％ within 8 h，and drug release behavior in vitro of the latter was in accordance with Weibull kinetic model. Inhibitory effect of CHE-NPs on B 16 melanoma cells was significantly stronger than that of CHE ；the 24 h IC 50 of CHE-NPs and CHEwere 69.35 and 107.36 μg/mL，respectively. CONCLUSIONS ：The prepared CHE-NPs show good sustained-effect and high capacity of drug loading ，and strengthen the inhibitory effect of CHE on melanoma.
