本文選題：替尼泊苷　切入點(diǎn)：多層包衣白蛋白納米粒　出處：《沈陽(yáng)藥科大學(xué)學(xué)報(bào)》2017年09期 　論文類型：期刊論文

【摘要】：目的以人血清白蛋白為載體包載替尼泊苷,經(jīng)過(guò)包衣修飾后制備包載替尼泊苷的多層包衣納米粒(teniposide-encapsulated multilayer nanoparticles,P-CS-NP),以期降低藥物的不良反應(yīng)并改善其體外抗腫瘤活性。方法以粒徑、多分散指數(shù)和載藥率為評(píng)價(jià)指標(biāo),采用單一因素法篩選出替尼泊苷白蛋白納米粒的最優(yōu)處方工藝,通過(guò)加入殼聚糖和聚谷氨酸聚乙二醇共聚物進(jìn)一步制備多層包衣白蛋白納米粒,篩選得到最優(yōu)包衣量。以游離的替尼泊苷作為參比,用MTT法測(cè)定納米粒對(duì)人肺癌A549細(xì)胞的體外細(xì)胞毒性,并用流式細(xì)胞儀和共聚焦顯微鏡測(cè)定和觀察多層包衣納米粒的細(xì)胞攝取率和細(xì)胞攝取行為。結(jié)果確定了多層包衣納米粒的處方及制備工藝。多層包衣納米粒的體外細(xì)胞毒性比游離的替尼泊苷小,攝取具有時(shí)間依賴性,與殼聚糖共孵育的納米粒的細(xì)胞攝取量增加,入胞后納米粒主要分布在細(xì)胞質(zhì)。結(jié)論白蛋白納米粒能被殼聚糖和聚谷氨酸聚乙二醇共聚物包衣修飾,多層包衣納米�？梢宰鳛樘婺岵窜盏乃幬镞f送載體,其體外細(xì)胞毒性降低。
[Abstract]:Objective to prepare teniposide-coated multilayer nanoparticles-P-CS-NPP coated with human serum albumin (HSA) as carrier and coated with teniposide-apsulated nanoparticles-P-CS-NPP, in order to reduce adverse drug reactions and improve its antitumor activity in vitro. The polydispersity index and drug loading rate were used as the evaluation indexes. The optimal formulation process of teniposide albumin nanoparticles was selected by single factor method. The multilayer coated albumin nanoparticles were prepared by adding chitosan and poly (ethylene glycol glutamate) copolymers, and the optimal coating amount was obtained. The free teniposide was used as the reference. The cytotoxicity of nanoparticles to human lung cancer A549 cells in vitro was determined by MTT assay. The cell uptake rate and cell uptake behavior of multilayer coated nanoparticles were measured and observed by flow cytometry and confocal microscopy. The formulation and preparation process of multilayer coated nanoparticles were determined. The extracellular toxicity was less than that of free teniposide. The uptake was time-dependent, and the uptake of the nanoparticles incubated with chitosan increased, and the nanoparticles mainly distributed in the cytoplasm. Conclusion Albumin nanoparticles can be coated with chitosan and poly (glutamic acid) polyethylene glycol copolymers. Multilayer coated nanoparticles can be used as drug delivery carriers of teniposide, and their cytotoxicity is decreased in vitro.
【作者單位】： 沈陽(yáng)藥科大學(xué)藥學(xué)院;
【分類號(hào)】：R943;R96

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本文編號(hào)：1596931