Faculty of Chemistry, University of Warsaw, Pasteura 1 Str., PL-02-093 Warsaw, Poland.
Faculty of Chemistry, Warsaw University of Technology, Noakowskiego 3 Str., PL-00-664 Warsaw, Poland.
Int J Mol Sci. 2020 Aug 14;21(16):5832. doi: 10.3390/ijms21165832.
This work presents a new look at the application of cyclodextrins (CD) as a drug nanocarrier. Two different cyclodextrins (CD, CD) were covalently conjugated to branched polyethylenimine (PEI), which was additionally functionalized with folic acid (PEI-CD-CD-FA). Here, we demonstrated that the combination of CD and CD enabled to load and control release of two anticancer drugs: doxorubicin (DOX) and beta-lapachone (beta-LP) (DOX in -CD and beta-LP into -CD) via host-guest inclusion. The PEI-CD(DOX)-CD-FA nanoconjugate was used to transport anticancer drugs into A549 lung cancer cells for estimation the cytotoxic and antitumor effect of this nanoconjugate. The presence of FA molecules should facilitate the penetration of studied nanoconjugate into the cell. Whereas, the non-cellular experiments proved that the drugs are released from the carrier mainly in the pH 4.0. The release mechanism is found to be anomalous in all studied cases.
本工作重新审视了环糊精(CD)作为药物纳米载体的应用。两种不同的环糊精(CD、CD)被共价连接到支化聚乙烯亚胺(PEI)上,PEI 还被叶酸(PEI-CD-CD-FA)功能化。在这里,我们证明了 CD 和 CD 的结合能够通过主客体包合来装载和控制两种抗癌药物:阿霉素(DOX)和β-拉帕醌(β-LP)(DOX 在 -CD 中,β-LP 在 -CD 中)的释放。PEI-CD(DOX)-CD-FA 纳米复合物被用于将抗癌药物输送到 A549 肺癌细胞中,以评估该纳米复合物的细胞毒性和抗肿瘤作用。FA 分子的存在应该有助于研究的纳米复合物进入细胞。然而,非细胞实验证明,药物主要在 pH 4.0 从载体中释放。在所有研究的情况下,都发现释放机制是异常的。