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利用pH敏感材料聚乙二醇单甲醚-聚乳酸-聚组氨酸(mPEG45-PLA18-PHis12)作为载体构建了高良姜素pH敏感胶束(Gal-pHSM),采用单因素实验和响应面法优化了Gal-pHSM的处方工艺，通过UV-Vis、FTIR、XRD等表征了其结构，测试了Gal-pHSM的pH敏感性，并采用噻唑蓝(MTT)法研究了Gal-pHSM对HeLa细胞的抑制作用。结果表明，Gal-pHSM最佳处方工艺为：mPEG45-PLA18-PHis12与高良姜素质量比11.60∶1、高良姜素浓度0.82 mg·mL-1、水化时间1.40 h,在此条件下，包封率为(92.91±1.03)%、载药量为(7.29±0.18)%、粒径为(79.94±6.04) nm、Zeta电位为-(16.43±0.98) mV;高良姜素在Gal-pHSM冻干粉中以无定形态存在，体外释药具有明显的pH敏感性；24、48 h时，高良姜素的半数抑制浓度(IC50)分别为40.72、24.44μg·mL-1,Gal-pHSM的IC50值分别降至26.72、14.82μg·mL-1,Gal-pHSM对HeLa细胞的抑制作用增强。构建的Gal-pHSM具有良好pH敏感性，有望作为抗肿瘤药物载体。
Abstract：Using the pH-sensitive material polyethylene glycol monomethyl ether-poly(lactic acid)-polyhistidine(mPEG45-PLA18-PHis12) as a carrier, we constructed galangin pH-sensitive micelles(Gal-pHSM).Moreover, we optimized the prescription process of Gal-pHSM by single-factor experiments and response surface methodologies, and characterized the structure of Gal-pHSM by UV-Vis, FTIR,and XRD.Furthermore, we tested the pH sensitivity of Gal-pHSM,and studied the inhibitory effect of Gal-pHSM on HeLa cells by Thiazolyl Blue(MTT) assay.The results show that the optimal prescription process of Gal-pHSM is as follows: the mass ratio of mPEG45-PLA18-PHis12 to galangin of 11.60∶1,the galangin concentration of 0.82 mg·mL-1,and the hydration time of 1.40 h.Under above conditions, the encapsulation rate is(92.91±1.03)%,the drug loading is(7.29±0.18)%,the particle size is(79.94±6.04) nm, and the Zeta potential is -(16.43±0.98) mV.Galangin exists in the form of amorphous in the freeze-dried powder Gal-pHSM,and the in vitro drug release exhibits obvious pH sensitivity.At 24 and 48 h, the half-inhibitory concentration(IC50) of galangin is 40.72 and 24.44 μg·mL-1,respectively, and the IC50 value of Gal-pHSM is reduced to 26.72 and 14.82 μg·mL-1,respectively, indicating that the inhibitory effect of Gal-pHSM on HeLa cells is enhanced.The constructed Gal-pHSM has good pH sensitivity and is expected to be used as an anti-tumor drug carrier.
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基本信息:
中图分类号:TQ460.4;R730.5
引用信息:
[1]王丽,高小玲,李思翰,等.高良姜素pH敏感胶束的构建及体外抗肿瘤活性研究[J].化学与生物工程,2026,43(05):57-64.
基金信息:
2023年度河南省高等学校重点科研项目(23B350005)
2026-05-13
2026-05-13