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

作　　者：王鲁豫 季珂 李如梦 田雨冬[2] 关延彬[1,3] 孙彦君 WANG Luyu;JI Ke;LI Rumeng;TIAN Yudong;GUAN Yanbin;SUN Yanjun(School of Pharmacy,Henan University of Chinese Medicine,Henan Zhengzhou 450040,China;Department of Urology Surgery,First Affiliated Hospital,Zhengzhou University,Henan Zhengzhou 450052,China;Henan Research Center for Special Processing Technology of Chinese Medicine,Henan Zhengzhou 450040,China)

机构地区：[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]河南省中药特色炮制技术工程研究中心,河南郑州450040

出　　处：《中国医院药学杂志》2024年第19期2223-2229,共7页Chinese Journal of Hospital Pharmacy

基　　金：河南省高等学校重点科研项目(编号:23A320005);河南中医药大学2022年度研究生科研创新能力提升计划(编号:2022KYCX002);河南省科技攻关项目(编号:182102310096);河南省中医药科学研究专项课题(编号:20-21ZY2150)。

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。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 process for F127/SWCNTs-COOH/Ber was as follows:ratio of carrier to drug was 1∶1,ultrasonic power 200 W and ultrasonic frequency 30 times.Average particle size and Zeta potential were(182.3±11.64)nm and(–3.44±0.17)mV;encapsulation efficiency and drug loading 81.09%and 38.86%;cumulative dissolution rates within 30 min in simulated intestinal fluid and simulated gastric fluid 94.02%and 76.69%.The absorption of berberine in F127/SWCNTs-COOH followed the pseudo-secondorder 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 

分 类 号：R283.6[医药卫生—中药学] R943[医药卫生—中医学]