This work spotlights on fabrication of CD44-tropic, layer-by-layer (LbL) coated, liquid crystalline nanoparticles of rapamycin (Rap-LbL-LCNPs) to enhance its water solubility and enable its anticancer use.Rap-LCNPs were fabricated using hydrotrope method and then coated using LbL self-assembly technique.LbL coating strategy successfully reduced monoolein-induced hemolysis and increased LCNPs serum stability. Lyophilized Rap-LbL-LCNPs were successfully sterilized using γ-radiations. In CD44-overexpressed MDA-MB-231 cells, Rap-LbL-LCNPs demonstrated superior cytotoxicity compared with the nontargeted formulation. Rap-LbL-LCNPs showed 3.35-fold increase in bioavailability compared with free drug. Rap-LbL-LCNPs significantly inhibited tumor growth, enhanced animal survival and reduced nephrotoxic and hyperglycemic effects of Rap.LbL coating strategy of Rap-LCNPs could serve as a promising approach that facilitates Rap use in cancer therapy.

作者：May S, Freag；Yosra Sr, Elnaggar；Doaa A, Abdelmonsif；Ossama Y, Abdallah

来源：Nanomedicine (London, England) 2016 年 11卷 22期