Inderscience Publishers

The doxorubicin–entrapped lipoparticles: preparation, characterisation, and efficacy of cellular uptake in human Caco–2 cell

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Doxorubicin–loaded polyethylene glycol (PEG)–modified lipoparticles with high doxorubicin entrapment has been developed. The preparation technique, characteristics, release profile, cell cytotoxicity, and cellular internalisation of the lipoparticles were evaluated. The PEG–modified lipoparticles prepared by ethanol injection extrusion (100 nm pore size) achieve a population of blank liposomes with a mean size of 125 ± 2.3 nm and a zeta potential of −12.4 ± 1.5 mV. The optimum doxorubicin–loaded lipoparticles system used doxorubicin nanoparticles as core interactions with a 20 : 1 ratio of core and lipid formula consisting of distearoyl phosphatidylcholine/cholesterol/distearoyl phosphoethanolamine–PEG2000)/docosahexaenoic acid at a ratio of 44/36/5/15 and lipid (mg)/ethanol (ml)/water (ml) at a ratio of 25/1/9. The average particle size of the doxorubicin–loaded lipoparticles was 157.7 ± 5.6 nm with a zeta potential of +13.3 mV. Lipoparticle conformation was determined using transmission electron microscopy and field–emission scanning electron microscopy. The doxorubicin encapsulation efficiency was 75.6% for lipoparticles. In vitro release tests indicated that the 50% release time for the doxorubicin–loaded lipoparticles was 7.9 h. A Caco–2 cell model used for evaluating the cytotoxicity and cell uptake efficiency of the doxorubicin–loaded lipoparticles caused significantly less cellular cytotoxicity than doxorubicin solution (p <0.01) and was significantly taken up into cells within 60 min (p < 0.01).

Keywords: formulation, doxorubicin nanoparticles, cellular uptake, doxorubicin–entrapped lipoparticles, human Caco–2 cells, polyethylene glycol, PEG, cell cytotoxicity, nanotechnology, release time

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