【摘要】：目的:以甲氧基聚乙二醇-聚乳酸(m PEG-PLA)為載體,研制紫杉醇共聚物膠束(PM-PTX),并評(píng)估其體外性能。方法:采用薄膜水化法制備,對(duì)PM-PTX的理化性質(zhì)進(jìn)行表征,檢測(cè)藥物的體外釋放,MTT法考察PM-PTX對(duì)Hep-2細(xì)胞株的體外細(xì)胞毒性。結(jié)果:制得的PM-PTX溶液無(wú)色透明,透射電鏡觀察膠束呈類圓形,膠束的包封率為(83.04±1.96)%,載藥量為(15.01±0.28)%,平均粒徑為(87.74±2.3)nm,多分散指數(shù)(PDI)為(0.259±0.014),Zeta電位為(-1.22±0.133)m V,CMC值為0.158 mg·L-1。在3種p H值(5.8,7.2和7.4)環(huán)境下,96 h藥物的累積釋放率分別為(92.19±3.17)%,(88.37±5.62)%和(86.04±2.16)%,無(wú)明顯差異(P0.05)。與紫杉醇針劑相比,PM-PTX對(duì)Hep-2細(xì)胞株的體外細(xì)胞毒性相對(duì)較弱,但膠束組細(xì)胞毒性的劑量和時(shí)間依賴性更明顯。結(jié)論:PM-PTX粒徑滿足淋巴靶向要求,具備緩釋性,劑型的改變有利于提高藥物抗癌活性。該新劑型對(duì)于惡性腫瘤的淋巴化療具有應(yīng)用前景。
[Abstract]:Aim: to prepare paclitaxel copolymer micelle (PM-PTX) with methoxy polyethylene glycol (m PEG-PLA) as carrier and evaluate its performance in vitro. Methods: the physicochemical properties of PM-PTX were characterized by membrane hydration method, and the drug release in vitro was detected. The cytotoxicity of PM-PTX to Hep-2 cell line was investigated by MTT method. Results: the PM-PTX solution was colorless and transparent. The micelles were round by transmission electron microscope. The encapsulation efficiency was (83.04 鹵1.96)%, the drug loading was (15.01 鹵0.28)%, and the average particle size was (87.74 鹵2.3) nm,. The polydispersity index (PDI) was (0.259 鹵0.014), Zeta potential (-1.22 鹵0.133) MV, the CMC value was 0.158 mg L ~ (-1). The cumulative release rates at 96 h were (92.19 鹵3.17)%, (88.37 鹵5.62)% and (86.04 鹵2.16)% under three pH values (5.87.2and 7.4), respectively (P0.05). Compared with paclitaxel injection, the cytotoxicity of PM-PTX to Hep-2 cell line was relatively weak in vitro, but the dose and time dependence of the cytotoxicity of micelle group was more obvious than that of paclitaxel injection. Conclusion: the particle size of PM-PTX can meet the requirement of lymphoid target, and it has the ability to release slowly. The change of dosage form is helpful to improve the anticancer activity of the drug. The new formulation has a promising application in lymphatic chemotherapy of malignant tumors.
【作者單位】： 復(fù)旦大學(xué)附屬眼耳鼻喉科醫(yī)院上海市頭頸外科重點(diǎn)學(xué)科;復(fù)旦大學(xué)藥學(xué)院藥劑學(xué)教研室;
【基金】：上海市衛(wèi)生計(jì)生委委級(jí)科研項(xiàng)目(20124038)
【分類號(hào)】：R943

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