張欣欣;許潔;蔣巖;趙麗艷;張萬明;

• 1:河北北方學院藥學系
• 2:河北省神經藥理學重點實驗室

摘要(Abstract)：

為提高依托泊苷制劑的水溶性和穩定性,采用星點設計-效應面法優化依托泊苷納米混合膠束(ETP mPEG-PLA/P123)的處方工藝。在單因素試驗基礎上,以投藥量、mPEG-PLA所占質量比和水化體積為自變量,以依托泊苷包封率、載藥量以及粒徑為因變量,進行3因素5水平的星點設計-效應面法實驗,采用熒光探針法測定臨界膠束濃度(CMC),并對所制備的膠束制劑進行理化性質和釋放行為的評估。結果表明,ETP mPEG-PLA/P123膠束制劑的最優處方工藝如下:mPEG-PLA與P123質量比為38∶62,投藥量為5 mg,水化體積為6 mL;采用最優處方制得的混合膠束的包封率為87.4%,載藥量為4.19%,粒徑為115.6 nm, PDI為0.216,Zeta電位為-16.3 mV;熒光探針法測定的CMC值為1.7×10~(-3 )g/L,mPEG-PLA/P123膠束穩定性良好;體外釋放實驗中,依托泊苷可從膠束中緩慢而持續地釋放,在48 h內釋放量可達80%。采用優化處方制得的ETP mPEG-PLA/P123納米混合膠束,能顯著增加依托泊苷的溶解度,膠束制劑穩定性好,且有一定的緩釋作用,可為進一步拓寬依托泊苷新型制劑的應用范圍提供理論依據。

關鍵詞(KeyWords)： 藥劑學;依托泊苷;P123;膠束;UPLC;薄膜水化法;星點設計-效應面法

Abstract:

Keywords:

基金項目(Foundation): 國家自然科學基金(81274005);; 河北省教育廳高�；�本科研業務費(JYT2020002);; 河北省衛生健康委科研基金(20180812)

作者(Author): 張欣欣;許潔;蔣巖;趙麗艷;張萬明;

Email:

DOI:

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