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目的:制备叶酸壳寡糖修饰的紫杉醇PLGA纳米粒(F-CS-PLGA-NPs),并考察其对人卵巢癌上皮细胞(SKOV-3)的抑制作用。方法:采用界面沉积法制备F-CS-PLGA-NPs,以30%乙醇作为释放介质考察修饰和未修饰纳米粒的体外释药情况,MTT法比较不同剂型和不同浓度紫杉醇对SKOV-3增殖的抑制作用。结果:F-CS-PLGA-NPs的粒径为(321±0.76)nm,电位为(22.6±0.26)m V,载药量为(5.1±0.25)%,包封率为(41.96±1.96)%。修饰和未修饰纳米粒的体外释药曲线相似,在最初24 h内约有35%药物释放,随后释药速度减慢,纳米粒以近零级方式释放,144 h累计释药率约为75%。细胞实验结果显示,在紫杉醇浓度相同的情况下,F-CS-PLGA-NPs在不同作用时间对细胞的抑制作用均强于紫杉醇溶液组和普通纳米粒组,FCS-PLGA-NPs对SKOVS细胞增殖的抑制作用在一定程度上被游离叶酸减弱。结论:叶酸壳寡糖的修饰增加了纳米粒对SKOVS-3细胞的靶向性。
OBJECTIVE: To prepare folic acid chitooligosaccharides modified paclitaxel PLGA nanoparticles (F-CS-PLGA-NPs) and investigate its inhibitory effect on human ovarian epithelial cells (SKOV-3). Methods: F-CS-PLGA-NPs were prepared by the interface deposition method. The release of modified and unmodified nanoparticles was investigated by using 30% ethanol as the release medium. MTT assay was used to compare the proliferation of SKOV-3 with different dosage forms and paclitaxel Inhibition. RESULTS: The diameter of F-CS-PLGA-NPs was (321 ± 0.76) nm, the potential was (22.6 ± 0.26) mV, the drug loading was (5.1 ± 0.25)% and the encapsulation efficiency was (41.96 ± 1.96) %. The in vitro release profiles of modified and unmodified nanoparticles were similar, with about 35% drug release in the first 24 h, followed by a slow release rate and near zero order release of nanoparticles, with a cumulative drug release rate of approximately 75% at 144 h . The results of cell experiments showed that the inhibitory effect of F-CS-PLGA-NPs on paclitaxel-treated cells was stronger than that of paclitaxel-treated and paclitaxel-treated groups at the same concentration of paclitaxel. The proliferation of SKOVS cells was inhibited by FCS-PLGA-NPs The inhibition was somewhat attenuated by free folate. CONCLUSION: Modification of folic acid chitooligosaccharides enhances the targeting of the nanoparticles to SKOVS-3 cells.