title: Paclitaxel-loaded SCK nanoparticles: an investigation of loading capacity and cell killing abilities in vitro.
abstract: Block copolymer nanoparticles having two different hydrodynamic diameters (120 nm vs 50 nm) and core diameters (60 nm vs 20 nm) with variable paclitaxel loading (5 to 20 wt % with respect to polymer weight, 4.4 μg/mL to 21.7 μg/mL paclitaxel concentrations in ultrapure water) were prepared for their in vitro cytotoxicity evaluation. Empty nanoparticles did not show any inherent cytotoxicity even at their highest concentration, whereas paclitaxel-loaded nanoparticles resulted in IC50 values that were better than free paclitaxel at 2 h (0.021 μM vs 0.046 μM) incubation periods, and approximately equal to free paclitaxel at 72 h (0.004 μM vs 0.003 μM) continuous incubation. Confocal fluorescence microscopy images demonstrated that the drug-loaded nanoparticles internalized into KB cells within 2 h and released their payload, resulting in cytotoxicity as evident from the fragmented nuclei present. Functionalization of the nanoparticle surfaces with poly(ethylene oxide) (2 kDa PEO, 5 PEO per block copolymer chain) did not affect the loading of paclitaxel or cell kill ability. No free paclitaxel was found in these nanoparticle formulations indicated by analytical assays.
authors: Departments of Chemistry and Chemical Engineering, Texas A&M University, College Station, Texas 77842, United States.
authors: Lily Yun
authors: LY
authors: Lin
authors: Amolkumar
authors: A
authors: Karwa
authors: James G
authors: JG
authors: Kostelc
authors: Nam S
authors: NS
authors: Lee
authors: Richard B
authors: RB
authors: Dorshow
authors: Karen L
authors: KL
authors: Wooley
mesh_terms: D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D053758:Nanoparticles / Q000737:chemistry*; D017239:Paclitaxel / Q000737:chemistry* / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000737:chemistry; D011108:Polymers / Q000737:chemistry
chemical_list: D004337:Drug Carriers; D011108:Polymers; D011092:Polyethylene Glycols; D017239:Paclitaxel