Successful delivery of docetaxel to rat brain using experimentally developed nanoliposome: a treatment strategy for brain tumor.
Successful delivery of docetaxel to rat brain using experimentally developed nanoliposome: a treatment strategy for brain tumor.
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使用实验开发的纳米脂质体成功地将多西紫杉醇递送至大鼠大脑：脑肿瘤的治疗策略。
DOI：
10.1080/10717544.2016.1253798
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发表时间：
2017-11
期刊：
影响因子：
6
通讯作者：
Mandal M
中科院分区：
文献类型：
--
作者：
Shaw TK;Mandal D;Dey G;Pal MM;Paul P;Chakraborty S;Ali KA;Mukherjee B;Bandyopadhyay AK;Mandal M
多西紫杉醇（DTX）在体外对胶质瘤细胞有很好的抑制作用。然而，由于药物的物理化学和药理学特性，DTX通过BBB的体内通道极其困难。现有的制剂在这方面都不成功。因此，在本研究中，通过开发载有DTX的纳米脂质体，努力将DTX通过血脑屏障（BBB）发送到脑，以治疗诸如脑实体瘤（神经胶质瘤）的疾病。通过FTIR光谱法评价主要药物-辅料相互作用。采用脂质层水化法制备了载药纳米脂质体（L-DTX），并对其进行了理化表征。研究了C6胶质瘤细胞的体外细胞摄取。FTIR数据表明，所选药物和辅料具有化学相容性。单层囊泡大小小于50 nm，表面光滑。L-DTX体外释药缓慢，持续性好。药代动力学数据显示，L-DTX在实验大鼠中的作用比游离药物和泰索帝®更持久。与Taxotere®相比，L-DTX的DTX在4 h内使脑中药物浓度增加100%。因此，纳米脂质体作为媒介物可能是一种令人鼓舞的策略来治疗神经胶质瘤与DTX。
Docetaxel (DTX) is found to be very effective against glioma cell in vitro. However, in vivo passage of DTX through BBB is extremely difficult due to the physicochemical and pharmacological characteristics of the drug. No existing formulation is successful in this aspect. Hence, in this study, effort was made to send DTX through blood–brain barrier (BBB) to brain to treat diseases such as solid tumor of brain (glioma) by developing DTX-loaded nanoliposomes. Primarily drug-excipients interaction was evaluated by FTIR spectroscopy. The DTX-loaded nanoliposomes (L-DTX) were prepared by lipid layer hydration technique and characterized physicochemically. In vitro cellular uptake in C6 glioma cells was investigated. FTIR data show that the selected drug and excipients were chemically compatible. The unilamellar vesicle size was less than 50 nm with smooth surface. Drug released slowly from L-DTX in vitro in a sustained manner. The pharmacokinetic data shows more extended action of DTX from L-DTX in experimental rats than the free-drug and Taxotere®. DTX from L-DTX enhanced 100% drug concentration in brain as compared with Taxotere® in 4 h. Thus, nanoliposomes as vehicle may be an encouraging strategy to treat glioma with DTX.
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影响因子：
2.6
作者：
Banks WA
通讯作者：
Banks WA
影响因子：
8
作者：
Hu K;Cao S;Hu F;Feng J
通讯作者：
Feng J
影响因子：
1.8
作者：
Kuppens, IELM;van Maanen, MJ;Beijnen, JH
通讯作者：
Beijnen, JH
影响因子：
3
作者：
Dey, Niladri Shekhar;Mukherjee, Biswajit;Satapathy, Bhabani Sankar
通讯作者：
Satapathy, Bhabani Sankar
影响因子：
5.6
作者：
Sánchez-Moreno P;Boulaiz H;Ortega-Vinuesa JL;Peula-García JM;Aránega A
通讯作者：
Aránega A