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目的:制备载天门冬酰胺酶(asparaginase,AN)自组装透明质酸-聚乙二醇(hyaluronic acid-graft-poly(ethylene glycol),HA-g-PEG)/γ-环糊精(γ-cyclodextrin,γ-CD)纳米囊(HA-g-PEG/γ-CD nanocapsules loaded with AN,AHRPs),并对AHRPs及游离AN在体外的活性及稳定性进行研究。方法:采用自组装法制备了AHRPs,考察了AHRPs的透射电镜、粒径、Zeta电位、最适温度和最适p H,并通过贮存稳定性、抗胰蛋白酶水解能力、抗部分金属离子及有机化合物、热稳定性、酸碱稳定性和血浆稳定性等实验,对游离AN与AHRPs体外稳定性差异进行了一定的考察。结果:AHRPs的粒径为(410.30±3.20)nm,Zeta电位为(-31.40±1.65)m V,AHRPs和游离AN的最适温度分别为50℃和60℃,最适p H值均为7.5。稳定性实验结果显示,相同条件下,AHRPs的贮存稳定性、抗胰蛋白酶水解能力、抗金属离子和有机化合物、热稳定性、酸碱稳定性和血浆稳定性均优于游离AN。结论:AHRPs能同时提高游离AN在体外的活性及稳定性。
OBJECTIVE: To prepare self-assembled hyaluronic acid-graft-poly (ethylene glycol) (HA-g-PEG) / γ-cyclodextrin (γ- The activity and stability of AHRPs and free AN in vitro were studied in vitro by using cyclodextrin and γ-CD nanocapsules loaded with AN (AHRPs). Methods: AHRPs were prepared by self-assembly method. The transmission electron microscopy, particle size, Zeta potential, optimum temperature and optimal pH of AHRPs were investigated. The storage stability, antitrypsin hydrolytic ability, anti-partial metal ions and organic Compounds, thermal stability, acid-base stability and plasma stability experiments to investigate the differences between in vitro stability of free AN and AHRPs. Results: The particle size of AHRPs was (410.30 ± 3.20) nm and the Zeta potential was (-31.40 ± 1.65) mV. The optimum temperature for AHRPs and free AN were 50 ℃ and 60 ℃, respectively. The optimum p H values were 7.5 . The results of stability experiments showed that under the same conditions, the storage stability, antitrypsin hydrolytic ability, anti-metal ions and organic compounds, thermal stability, pH stability and plasma stability of AHRPs were better than those of free AN. Conclusion: AHRPs can improve the activity and stability of free AN in vitro at the same time.