CAJ | 학술논문

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)mV,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,F-CS-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SK-OVS-3细胞的靶向性。
목적：：제비협산각과당수식적자삼순PLGA납미립(F-CS-PLGA-NPs),병고찰기대인란소암상피세포(SKOV-3)적억제작용。방법：채용계면침적법제비F-CS-PLGA-NPs,이30%을순작위석방개질고찰수식화미수식납미립적체외석약정황, MTT법비교불동제형화불동농도자삼순대SKOV-3증식적억제작용。결과： F-CS-PLGA-NPs적립경위(321±0.76) nm,전위위(22.6±0.26)mV,재약량위(5.1±0.25)%,포봉솔위(41.96±1.96)%。수식화미수식납미립적체외석약곡선상사,재최초24 h내약유35%약물석방,수후석약속도감만,납미립이근령급방식석방,144 h루계석약솔약위75%。세포실험결과현시,재자삼순농도상동적정황하,F-CS-PLGA-NPs재불동작용시간대세포적억제작용균강우자삼순용액조화보통납미립조,F-CS-PLGA-NPs대SKOVS세포증식적억제작용재일정정도상피유리협산감약。결론：협산각과당적수식증가료납미립대SK-OVS-3세포적파향성。
Objective:To prepare PLGA nanoparticles modified with folic acid conjugated chitosan oligosaccharide containing pa-clitaxel (F-CS-PLGA-NPs) and study the inhibitory effect on SKOV-3. Methods:F-CS-PLGA-NPs were prepared by an interface dep-osition method, 30% ethanol was used as the release medium for the in vitro release profiles of nanoparticles, and MTT was adopted to evaluate the inhibitory effect of paclitaxel with different formulations and concentrations on SKOV-3. Results:The particle size and zeta potential of F-CS-PLGA-NPs was (321 ± 0. 76) nm and (22. 6 ± 0. 26) mV, respectively, the drug loading was (5. 1 ± 0. 25)%, and the encapsulation efficiency was (41. 96 ± 1. 96)%. F-CS-PLGA-NPs had a similar in vitro release profiles with the ordinary nanoparti-cles ( PLGA-NPs) . About 35% of paclitaxel was released from the nanoparticles in the initial 24 h, and then a near zero order release at a relative slow rate was shown, and the cumulative release rate in 144 h was about 75%. The results of cell experiments suggested that at the same paclitaxel concentration, the inhibition effect of F-CS-PLGA-NPs group was stronger than that of the PLGA-NPs group and the solution group. The inhibition effect of F-CS-PLGA-NPs could be reduced by free folic acid. Conclusion:PLGA nanoparticles modified with folic acid conjugated chitosan oligosaccharide can increase the targeting efficiency in SKOVS-3 tumor cells.