Comparison of Shell-Cross-Linked Micelles with Soft and Glassy Cores as a Drug Delivery Vehicle for Albendazole: Is There a Difference in Performance?

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• 作者：Yoseop Kim ; Elviana D. Liemmawal ; Mohammad H. Pourgholami ; David L. Morris ; Martina H. Stenzel
• 刊名：Macromolecules
• 出版年：2012
• 出版时间：July 10, 2012
• 年：2012
• 卷：45
• 期：13
• 页码：5451-5462
• 全文大小：555K
• 年卷期：v.45,no.13(July 10, 2012)
• ISSN：1520-5835

文摘

The understanding of glass transition temperatures T_g in drug and polymer systems is indispensable for drug encapsulation and delivery. Amphiphilic block copolymers consisting a various ratios of poly(methyl methacrylate) (T_g = 100 掳C) and poly(ethyl acrylate) (T_g = 鈭?2 掳C) as the hydrophobic block have been synthesized via reversible addition鈥揻ragmentation chain transfer (RAFT) polymerization as drug delivery carrier for albendazole (ABZ). Self-assembled micelles with diameters of 25 nm with glassy (PMMA) and soft (PEA) core have been synthesized. Differential scanning calorimetry (DSC) has been used to evaluate crystallinity and miscibility of ABZ with the core-forming polymer. All drug鈥損olymer systems are compatible, but they become less miscible with increasing amount of PMMA. The most noticeable difference was the suppression of the crystallinity of the drug with increasing PEA content, a prerequisite for long shelf life of the drug carrier. Since the different micelles are subject to different thermodynamic stability, shell-cross-linking was carried out. Cell experiments against OVCAR-3 cell lines show a fast and efficient uptake of these nanoparticles. Shell-cross-linked micelles were found to be 2鈥? times more efficient against OVCAR-3 cells at low concentrations. In contrast, there was no significant difference in the IC₅₀ value of drug carriers with glassy and soft cores.