Enhanced oral bioavailability and anticancer efficacy of fisetin by encapsulating as inclusion complex with HPβCD in polymeric nanoparticles.
Enhanced oral bioavailability and anticancer efficacy of fisetin by encapsulating as inclusion complex with HPβCD in polymeric nanoparticles.
复制标题
通过将 HPβCD 封装在聚合物纳米颗粒中，提高非瑟酮的口服生物利用度和抗癌功效。
DOI：
10.1080/10717544.2016.1245366
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发表时间：
2017-11
期刊：
影响因子：
6
通讯作者：
Sistla R
中科院分区：
文献类型：
--
作者：
Kadari A;Gudem S;Kulhari H;Bhandi MM;Borkar RM;Kolapalli VR;Sistla R
鱼腥草素(FST)是一种有效的抗癌植物成分，其水溶性差，生物利用度低。本研究的目的是通过将聚丙交酯-羟基乙醇酸纳米粒(PLGA-NPs)作为HP-βCD(羟丙基-β-环糊精)的络合物，提高FST的口服生物利用度，并评价其对乳腺癌细胞的抗癌活性。制备了FSt-HP-βCD包合物，并用红外光谱、差示扫描量热法、X射线衍射仪和核磁共振氢谱对超分子包合物的形成进行了表征。制备了FHIC-PLGA纳米粒(FHIC-PNP)，并研究了其对人乳腺癌细胞MCF-7的体外抗肿瘤活性、细胞摄取、细胞凋亡和活性氧产生的影响。以纯FST和FHIC-PNP为对照，测定FST在C57BL6小鼠体内的相对生物利用度。结果表明，FHIC-PNP不仅增强了FST对MCF-7细胞的抗癌活性和细胞凋亡率，而且还提高了其口服生物利用度，表现为峰浓度和总吸收药物浓度的增加。
Fisetin (FST), a potent anticancer phytoconstituent, exhibits poor aqueous solubility and hence poor bioavailability. The aim of the present study is to improve the oral bioavailability of FST by encapsulating into PLGA NPs (poly-lactide-co-glycolic acid nanoparticles) as a complex of HPβCD (hydroxyl propyl beta cyclodextrin) and to assess its anti-cancer activity against breast cancer cells. FST-HPβCD inclusion complex (FHIC) was prepared and the supramolecular complex formation was characterized by FTIR, DSC, PXRD and 1H NMR. FHIC encapsulated PLGA nanoparticles (FHIC-PNP) were prepared and were studied for in vitro anticancer activity, cellular uptake, apoptosis and reactive oxygen species generation in MCF-7 human breast cancer cells. Comparative bioavailability of FST was determined after oral administration in C57BL6 mice as pure FST and FHIC-PNP. The results revealed that FHIC-PNP not only enhanced the anti-cancer activity and apoptosis of FST against MCF-7 cells but also improved its oral bioavailability, as demonstrated by increased peak plasma concentration and total drug absorbed.
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影响因子：
--
作者：
Maurya BK;Trigun SK
通讯作者：
Trigun SK
影响因子：
11.2
作者：
Hu, Liandong;Zhang, Hailei;Hu, Qiaofeng
通讯作者：
Hu, Qiaofeng
影响因子：
6.6
作者：
Bothiraja, Chellampillai;Yojana, Bhagwat D.;Thorat, Uday H.
通讯作者：
Thorat, Uday H.
影响因子：
9.7
作者：
Jang, Ki Young;Jeong, Soo-Jin;Kim, Sung-Hoon
通讯作者：
Kim, Sung-Hoon
DOI：
10.1016/j.ijbiomac.2014.05.035
发表时间：
2014-08-01
影响因子：
8.2
作者：
Pooja, Deep;Bikkina, Dileep J. Babu;Tiwari, Ashok K.
通讯作者：
Tiwari, Ashok K.