Vassilios Karavelidis1, Dimitrios Bikiaris, Konstantinos Avgoustakis. 1. Laboratory of Polymer Chemistry and Technology, Chemistry Department, Aristotle University of Thessaloniki, Thessaloniki, Greece; Pharmathen S.A., Pharmaceutical Industry, Pallini, Attiki, Greece.
Abstract
OBJECTIVE: New pegylated thermosensitive polymers were developed to study them as drug vehicles in targeting release nanoparticulate systems of anticancer drugs. METHODS: The drug vehicles were prepared in the form of core-shell nanoparticles using novel polymeric materials synthesized by copolymerization of poly(propylene adipate) (PPAd) and methoxy-polyethylene glycol (mPEG) with different molecular weights. The physical and chemical properties of the synthesized mPEG-PPAd copolymers were studied using several techniques, and their cytocompatibility was evaluated. For drug nanoencapsulation, a water in oil (W/O) emulsification and solvent evaporation technique was used and the prepared nanoparticles were studied for their physical properties, morphology, drug release and anticancer efficacy against cancer cell lines. KEY FINDINGS: The size of the nanoparticles lied in a range suitable for tumour targeting. Drug release was affected by the composition of polymer, the temperature and pH of the release medium. The release results obtained indicate that judicious selection of nanoparticles composition may allow for enhanced drug delivery to the tumours following application of local hyperthermia. CONCLUSIONS: The paclitaxel-loaded mPEG-PPAd nanoparticles were found to be cytotoxic against to the human hepatoma HepG2) and the human epithelial (HeLa) cancer cell lines. Enhanced cytotoxicity against the HeLa cells was observed at elevated temperature (42°C compared with 37°C), providing support for the potential usefulness of the mPEG-PPAd nanoparticles for the development of thermo-sensitive anticancer drug delivery systems.
OBJECTIVE: New pegylated thermosensitive polymers were developed to study them as drug vehicles in targeting release nanoparticulate systems of anticancer drugs. METHODS: The drug vehicles were prepared in the form of core-shell nanoparticles using novel polymeric materials synthesized by copolymerization of poly(propylene adipate) (PPAd) and methoxy-polyethylene glycol (mPEG) with different molecular weights. The physical and chemical properties of the synthesized mPEG-PPAd copolymers were studied using several techniques, and their cytocompatibility was evaluated. For drug nanoencapsulation, a water in oil (W/O) emulsification and solvent evaporation technique was used and the prepared nanoparticles were studied for their physical properties, morphology, drug release and anticancer efficacy against cancer cell lines. KEY FINDINGS: The size of the nanoparticles lied in a range suitable for tumour targeting. Drug release was affected by the composition of polymer, the temperature and pH of the release medium. The release results obtained indicate that judicious selection of nanoparticles composition may allow for enhanced drug delivery to the tumours following application of local hyperthermia. CONCLUSIONS: The paclitaxel-loaded mPEG-PPAd nanoparticles were found to be cytotoxic against to the humanhepatoma HepG2) and the human epithelial (HeLa) cancer cell lines. Enhanced cytotoxicity against the HeLa cells was observed at elevated temperature (42°C compared with 37°C), providing support for the potential usefulness of the mPEG-PPAd nanoparticles for the development of thermo-sensitive anticancer drug delivery systems.
Authors: Nikolaos D Bikiaris; Nina Maria Ainali; Evi Christodoulou; Margaritis Kostoglou; Thomas Kehagias; Emilia Papasouli; Emmanuel N Koukaras; Stavroula G Nanaki Journal: Nanomaterials (Basel) Date: 2020-12-11 Impact factor: 5.076