可生物降解的甲氧基聚乙二醇/聚己内酯核壳胶束:姜黄素缓释制剂的制备与表征
Biodegradable m-PEG/PCL Core-Shell Micelles: Preparation and Characterization as a Sustained Release Formulation for Curcumin.
作者信息
Danafar Hossein, Davaran Soodabeh, Rostamizadeh Kobra, Valizadeh Hadi, Hamidi Mehrdad
机构信息
Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran. ; Zanjan Pharmaceutical Nanotechnology Research Center, Zanjan University of Medical Sciences, Zanjan, Iran. ; Department of Medicinal Chemistry, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran.
Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
出版信息
Adv Pharm Bull. 2014 Dec;4(Suppl 2):501-10. doi: 10.5681/apb.2014.074. Epub 2014 Dec 31.
PURPOSE
Among the potent anticancer agents, curcumin is known as a very efficacious against many different types of cancer cells, but its clinical applications has been limited because of hydrophobicity, low gastrointestinal absorption, poor bioavailability and rapid metabolism. In this way, a novel micellar delivery system with mPEG-PCL was synthesized and the release profile of the curcumin from the drug-loaded micelles was evaluated.
METHODS
In this study, curcumin was encapsulated within monomethoxypoly(ethylene glycol)-poly(ε-caprolactone) (mPEG-PCL) micelles through a single-step nano-precipitation method, leading to creation of curcumin-loaded mPEG-PCL (Cur/mPEG-PCL) micelles. Di-block mPEG-PCL copolymers were synthesized and used to prepare micelles. mPEG-PCL copolymer was characterized in vitro by HNMR, FTIR, DSC and GPC techniques. Then, mPEG-PCL copolymers with curcumin were self-assembled into micelles in aqueous solution. The resulting micelles were characterized further by various techniques such as dynamic light scattering (DLS) and atomic force microscopy (AFM).
RESULTS
The findings showed the successful formation of smooth and spherical curcumin-loaded micelles. The encapsulation efficiency of curcumin was 88 ± 3.32%. The results of AFM revealed that the micelles have spherical shapes with size of 73.8 nm. The release behavior of curcumin from micelles was compared in different media. In vitro release of curcumin from curcumin-entrapped micelles was followed remarkably sustained profile. The sustained release of drug was hypothetically due to the entrapment of curcumin in core of micelles.
CONCLUSION
The results indicate the successful formulation of curcumin loaded m-PEG/PCL micelles. From the results, iIt can be concluded that curcumin m-PEG-PCL micelles may be considered as an effective treatment strategy for cancer in the future.
目的
在强效抗癌药物中,姜黄素以对多种不同类型癌细胞具有非常有效的作用而闻名,但其临床应用因疏水性、低胃肠道吸收率、低生物利用度和快速代谢而受到限制。因此,合成了一种新型的聚乙二醇单甲醚-聚己内酯(mPEG-PCL)胶束递送系统,并评估了载药胶束中姜黄素的释放情况。
方法
在本研究中,通过单步纳米沉淀法将姜黄素包裹在聚乙二醇单甲醚-聚己内酯(mPEG-PCL)胶束中,从而制备了载姜黄素的mPEG-PCL(Cur/mPEG-PCL)胶束。合成了二嵌段mPEG-PCL共聚物并用于制备胶束。通过核磁共振氢谱(HNMR)、傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)和凝胶渗透色谱法(GPC)技术对mPEG-PCL共聚物进行体外表征。然后,含姜黄素的mPEG-PCL共聚物在水溶液中自组装成胶束。通过动态光散射(DLS)和原子力显微镜(AFM)等各种技术对所得胶束进行进一步表征。
结果
研究结果表明成功形成了光滑的球形载姜黄素胶束。姜黄素的包封率为88±3.32%。原子力显微镜结果显示胶束呈球形,尺寸为73.8nm。比较了姜黄素在不同介质中从胶束中的释放行为。姜黄素从包封姜黄素的胶束中的体外释放呈现出明显的持续释放曲线。药物的持续释放推测是由于姜黄素被包裹在胶束核心中。
结论
结果表明成功制备了载姜黄素的m-PEG/PCL胶束。从结果可以得出结论,姜黄素m-PEG-PCL胶束未来可能被视为一种有效的癌症治疗策略。