Transferrin-conjugated polyphosphoester hybrid micelle loading paclitaxel for brain-targeting delivery: Synthesis, preparation and in vivo evaluation

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• 作者：Pengcheng Zhang^a ; ¹ ; Luojuan Hu^b ; ¹ ; Qi Yin^a ; Zhiwen Zhang^a ; Linyin Feng^b ; ^{lyfeng@mail.shcnc.ac.cn} ; Yaping Li^a ; ^{ypli@mail.shcnc.ac.cn}
• 关键词：Blood&ndash ; brain barrier (BBB) ; Transferrin ; Polyphosphoester ; Micelle ; Glioma
• 刊名：Journal of Controlled Release
• 出版年：2012
• 期刊代码：25_01683659
• 类别：pha
• 出版时间：10 May, 2012
• 卷：159
• 期：3
• 页码：429-434
• 文件大小：648 K

摘要

The successful treatment of central nervous system (CNS) disorders is hampered by inefficient drug delivery across the blood-brain barrier (BBB). Transferrin (Tf) could facilitate the transcytosis of coupled nanocarriers through Tf receptor (TfR) mediated pathway. In this study, Tf-modified paclitaxel-loaded polyphosphoester hybrid micells (TPM) was prepared and evaluated for its in vitro and in vivo brain-targeting efficiency. The polyphosphoester hybrid micelle formed a core-shell structure in aqueous solution, and demonstrated high drug entrapping efficiency (89.9 卤 3.4%). In addition, the micelle showed negligible hemolysis even at 2.0 mg/mL. The TPM was 87.85 卤 2.32 nm with 味 potentials 鈭?#xA0;12.33 卤 1.46 mV, and PTX showed sustained release from TPM. TPM demonstrated enhanced cellular uptake and brain accumulation, which were 2 and 1.8-fold of PM, respectively. TPM exhibited strongest anti-glioma activity, and the mean survival time of mice bearing intracranial U-87 MG glioma treated with TPM (39.5 days) was significantly longer than those treated with Taxol庐 (33.6 days). These results indicated that Tf conjugated micelle could be a promising carrier for brain-targeting drug delivery.