Paclitaxel-tyroserleutide Conjugates Self-assembly into Nanocarrier for Drug Delivery

Author(s): Yongjia Liu, Leilei Shi, Bangshang Zhu*, Yue Su, Hui Li*, Xinyuan Zhu.

Journal Name: Letters in Drug Design & Discovery

Volume 16 , Issue 8 , 2019

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Graphical Abstract:


Background: The drug-drug self-assembly was considered as a simple and efficient approach to prepare high drug loading nano-drug carriers and present new opportunities for cancer therapeutics. The strategy of PTX amphiphiles preparation would be a possible way to solve the poor water solubility of PTX.

Methods: The PTX-YSL conjugate were synthesized and characterized. The PTX-YSL nanocarriers was prepared by a simple self-assembly method. In vitro cell studies and pharmacokinetic studies were evaluated for their in vitro anti-tumor activities and blood retention time.

Results: The structures of PTX-YSL conjugate were confirmed by LC-MS, 1H NMR and FTIR. The size and morphology of the PTX-YSL self-assembled nanocarriers were observed with TEM and DLS. PTX-YSL nanocarriers could facilitate cellular uptake and had low cytotoxicity. PTX-YSL nanocarriers have longer blood retention for enhancing accumulation in the tumor tissues via EPR effect.

Conclusion: This drug delivery system formed by PTX-YSL conjugates constitutes a promising and effective drug carrier in cancer therapy.

Keywords: Paclitaxel, tyroserleutide, self-assembly, nanocarriers, drug delivery, circular dichroism.

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Article Details

Year: 2019
Page: [882 - 891]
Pages: 10
DOI: 10.2174/1570180815666180803124625
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