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负载小檗碱单壁碳纳米管递药系统的制备及体外评价

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目的:制备负载小檗碱单壁碳纳米管递药系统(F127/SWCNTs-COOH/Ber),并考察其对前列腺肿瘤的抑制作用.方法:采用超声法制备将小檗碱(berberine,Ber)负载于功能化羧基单壁碳纳米管(F127/SWCNTs-COOH)上,以包封率和载药量为指标,通过单因素试验考察优化处方制备工艺.对F127/SWCNTs-COOH/Ber的粒径及Zeta电位、体外溶出度及吸附特性等进行考察;采用人前列腺癌PC-3细胞进行体外细胞毒性评价.结果:最佳处方制备工艺,药物与载体投料比为1∶1,探超功率为200 W,探超次数为30次.制备的F127/SWCNTs-COOH/Ber平均粒径与电位分别为(182.3±11.64)nm、(-3.44±0.17)mV;包封率与载药量分别为81.09%、38.86%;30 min内在人工肠液和人工胃液中累积溶出率分别为94.02%、76.69%.F127/SWCNTs-COOH对小檗碱的吸附符合准二级吸附动力学模型.MTT实验与细胞摄取实验结果表明,F127/SWCNTs-COOH/Ber对PC-3细胞的增殖抑制作用显著高于单独使用小檗碱,可以更有效地将负载的小檗碱递送进入肿瘤细胞发挥治疗作用.结论:F127/SWCNTs-COOH/Ber递药系统制备成功,可提高小檗碱对前列腺肿瘤PC-3细胞的增殖抑制作用及细胞摄取效率,为前列腺癌治疗提供了一种潜在的递送载体.
Preparation and in vitro evaluation of a berberine-loaded single-walled carbon nanotubes drug delivery system
OBJECTIVE To prepare a drug delivery system of a single-walled carbon nanotubes loaded berberine(F127/SWCNTs-COOH/Ber)and explore the inhibitory effect on prostate cancer.METHODS Berberine was loaded onto F127/SWCNTs-COOH by ultrasonic method and formulation process was optimized by single-factor test using encapsulation efficiency and drug loading as parameters.Particle size,Zeta potential,in vitro dissolution and adsorption characteristics of F127/SWCNTs-COOH/Ber were explored.And cytotoxicity was evaluated in PC-3 cells.RESULTS The optimal formulation pro-cess for F127/SWCNTs-COOH/Ber was as follows:ratio of carrier to drug was 1∶1,ultrasonic power 200 W and ultrasonic fre-quency 30 times.Average particle size and Zeta potential were(182.3±11.64)nm and(-3.44±0.17)mV;encapsulation effi-ciency and drug loading 81.09%and 38.86%;cumulative dissolution rates within 30 min in simulated intestinal fluid and simu-lated gastric fluid 94.02%and 76.69%.The absorption of berberine in F127/SWCNTs-COOH followed the pseudo-second-order model.Anti-cancer activity of F127/SWCNTs-COOH/Ber was significantly higher than that of berberine alone,thereby enabling a more effective delivery of loaded berberine into tumor cells for therapeutic purposes.CONCLUSION F127/SWCNTs-COOH/Ber has successfully prepared,demonstrating its potential of enhancing the inhibitory effect on the proliferation of PC-3 cells in PC and cell uptake efficiency.This provides a promising delivery vector for treating prostate cancer.

berberineSWCNTs-COOHdrug delivery systemprostate cancer

王鲁豫、季珂、李如梦、田雨冬、关延彬、孙彦君

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河南中医药大学药学院,河南郑州 450040

郑州大学第一附属医院泌尿外科,河南郑州 450052

河南省中药特色炮制技术工程研究中心,河南郑州 450040

小檗碱 羧基单壁碳纳米管 递药系统 前列腺肿瘤

河南省高等学校重点科研项目河南中医药大学2022年度研究生科研创新能力提升计划河南省科技攻关项目河南省中医药科学研究专项课题

23A3200052022KYCX00218210231009620-21ZY2150

2024

中国医院药学杂志
中国药学会

中国医院药学杂志

CSTPCD北大核心
影响因子:1.198
ISSN:1001-5213
年,卷(期):2024.44(19)