摘要
目的制备一种载中药天花粉蛋白(Tk)的可示踪荧光纳米颗粒,提高药物水溶性和生物利用度及增强其免疫调节功能。方法使用FITC标记Tk用于观察药物作用部位。以聚乙二醇(PEG)-聚乳酸羟基乙酸(PLGA)为纳米载体,分别用逆相蒸发法、单乳法、复乳法构建PEG-PLGA-Tk-FITC纳米颗粒(Nano-Tk),通过粒径、电位、包封率和载药量筛选最佳制备方法。构建小鼠脾脏淋巴细胞体外诱导体系,流式检测Nano-Tk诱导调节性T细胞的功能。结果本研究成功建立了FITC-Tk荧光标记体系,标记效率高且定位于细胞质,筛选确认复乳法为Nano-Tk的最佳制备方法。与Tk直接给药比较,Nano-Tk能提高CD4^(+)Treg和CD8^(+)Treg的体外诱导效率(P<0.05)。结论本研究建立了可示踪荧光纳米颗粒Nano-Tk的制备方法,既提高了药物水溶性,又增强了其负向免疫调节功能,为最大程度发挥Tk抗炎活性,提高生物利用度开辟新思路。
Objective To prepare traceable fluorescent nanoparticles loaded with trichosanthin(Tk)of traditional Chinese medicine,and to improve the water solubility and bioavailability of the drug and enhance its immunomodulatory function.Methods FITC labeled Tk was used to observe the site of action of the drug.PEG-PLGA-Tk-FITC nanoparticles(Nano-Tk)were prepared by reverse evaporation method,single emulsion method,and double emulsion method with PEG-PLGA as nanocarrier.The optimal preparation method was screened by particle size,potential,encapsulation efficiency,and drug loading.The in vitro induction system of mouse spleen lymphocytes was constructed,and the function of Nano-Tk induced regulatory T cells was detected by flow cytometry.Results In this study,FITC-Tk fluorescent labeling system was successfully established with high labeling efficiency and localization in cytoplasm.Double emulsion method was screened and confirmed as the best preparation method of Nano-Tk.Compared with direct administration of Tk,Nano-Tk can significantly improve the induction efficiency of CD4^(+)Treg and CD8^(+)Treg in vitro(P<0.05).Conclusion In this study,the preparation method of traceable fluorescent nanoparticle Nano-Tk is established,which not only improved the water solubility of the drug,but also enhanced its negative immunomodulatory function,and opened up new ideas for maximizing the anti-inflammatory activity of Tk and improving bioavailability.
作者
丁旭苹
王克凡
曾聪
路丽明
DING Xuping;WANG Kefan;ZENG Cong;LU Liming(Department of Immunology and Microbiology,Shanghai Institute of Immunology,Shanghai Jiao Tong University School of Medicine,Shanghai 200025,China)
出处
《中国医药导报》
2025年第24期28-33,共6页
China Medical Herald
基金
上海市科学技术委员会科技计划项目(22490760400)
中央本级重大增减支项目(2060302)。
