PLGA-PEG nanoparticles containing gallium phthalocyanine: Preparation, optimization and analysis of its photodynamic efficiency on red blood cell and Hepa-1C1C7

Poly(lactide-co-glycolide) (PLGA) has been used for the encapsulation of phthalocyanine motived by its biocompatibility and biodegradability. Many studies have already been done to evaluate the influence of parameters used in the PLGA nanoparticle synthesis but without the evaluation of the combinatory interaction between these parameters on the nanoparticulate properties. Ga(III)-phthalocyanine (GaPc) was encapsulated into the PEGlated PLGA-nanoparticles and the individual and combinatory effects of the emulsification time, the method used for the nanoparticle synthesis and the temperature of the aqueous phase was evaluated on the size, entrapment efficiency, efficacy of nanoparticle recovery, residual PVA and zeta potential value using a 23 factorial design (FD). Mathematical models were adjustable to the data and evolutionary operations were performed to optimize the nanoparticle size. The ability of the optimized nanoparticle to decrease the viability of the Hepa-1C1C7 cell and the blood red cell was also evaluated. The FD disclosed the emulsification-diffusion method decreased the residual PVA and the size of PLGA-PEG nanoparticle, but also decreased the entrapment efficiency of GaPc, the zeta potential absolute value and the recovery efficacy of nanoparticles. The combinatory effect between the method used in the nanoparticle preparation and the temperature of aqueous phase influenced four of the five evaluated properties. The viability of Hepa-1C1C7 cells was reduced until 13× when the cells were irradiated in the presence of encapsulated GaPc while it was decreased until 4.7× when the experiment was carried out with the free GaPc. The encapsulated GaPc was also more efficient to cause the haemolysis of the RBC than it was the free GaPc. The optimization of the nanoparticles synthesis increased the efficiency of the GaPc to oxidize the evaluated cells. [Display omitted] •The diffusion method decreased five properties of GaPc-loaded PLGA-PEG nanoparticle.•The synergic effect of two parameters increased four nanoparticulate properties.•GaPc-loaded optimized nanoparticle decreased 13× the viability of the Hepa-1C1C7 cell.•The encapsulated GaPc was 4.6× more efficient to cause photohemolysis than free GaPc.•The photocytotoxicity of free GaPc on the Hepa-1C1C7 cell was concentration dependent.