黄芩苷
体内
Zeta电位
化学
体外
生物利用度
细胞毒性
牛血清白蛋白
药理学
纳米颗粒
癌细胞
IC50型
核化学
材料科学
生物化学
癌症
纳米技术
医学
色谱法
生物
内科学
高效液相色谱法
生物技术
作者
Fanning Meng,Fengjie Liu,Meng Lan,Tengteng Zou,Lihong Li,Tiange Cai,Yu Cai
标识
DOI:10.1016/j.jddst.2021.102603
摘要
Baicalin (BA) has been shown to be one of the natural compounds with anti-proliferative activity against numerous cancer cell lines, but its application is restricted due to its rapid metabolism and non-targeting to specific tissues. This study exploited folic acid (FA)-conjugated bovine serum albumin (BSA) nanoparticles (NPs) loaded with baicalin (FA-BSANPs/BA) by desolvation crosslinking method to improve its bioavailability and therapeutic efficacy. The optimized FA-BSANPs/BA showed spherical shape and uniform distribution. The average particle size, zeta potential, encapsulation efficiency (EE) and drug loading (DL) of FA-BSANPs/BA were 228.41 ± 2.36 nm, −32.70 ± 1.27 mV, 76.88 ± 0.59% and 7.41 ± 0.23%, respectively. X-ray diffraction (XRD) and thermogravimetric (TG) analysis exhibited that the drug was amorphous in the particles. The results of drug release behavior in vitro demonstrated that FA-BSANPs/BA releases BA slowly and continuously. In vitro cytotoxicity test results suggested that the IC50 of FA-BSANPs/BA and BA on MCF-7 cells was 16.7 and 75.96 μg/mL, respectively. The uptake efficiency of FA-BSANPs was significantly higher than that of BSANPs, which leads to a stronger potential for apoptosis. In vivo antitumor studies showed that FA-BSANPs/BA can greatly inhibit tumor growth compared with BA and exhibited the ability to target tumors in MCF-7 xenograft tumor-bearing nude mice. In conclusion, FA-BSANPs/BA improves therapeutic efficacy of BA and reduces side effects by targeting tumors, providing a promising strategy for breast cancer therapy.
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