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

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.