负载小檗碱单壁碳纳米管递药系统的制备及体外评价
Preparation and in vitro evaluation of a berberine-loaded single-walled carbon nanotubes drug delivery system
王鲁豫 1季珂 1李如梦 1田雨冬 2关延彬 3孙彦君1
作者信息
- 1. 河南中医药大学药学院,河南郑州 450040
- 2. 郑州大学第一附属医院泌尿外科,河南郑州 450052
- 3. 河南中医药大学药学院,河南郑州 450040;河南省中药特色炮制技术工程研究中心,河南郑州 450040
- 折叠
摘要
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.
Abstract
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.
关键词
小檗碱/羧基单壁碳纳米管/递药系统/前列腺肿瘤Key words
berberine/SWCNTs-COOH/drug delivery system/prostate cancer引用本文复制引用
基金项目
河南省高等学校重点科研项目(23A320005)
河南中医药大学2022年度研究生科研创新能力提升计划(2022KYCX002)
河南省科技攻关项目(182102310096)
河南省中医药科学研究专项课题(20-21ZY2150)
出版年
2024
NETL
NSTL
万方数据