Evaluation of a combined emulsion process to encapsulate methylene blue into PLGA nanoparticles

The delivery of photosensitizer compounds using biodegradable nanoparticles could improve dosage, controlled release and its bioavailability. In this study, methylene blue (MB) loaded PLGA nanoparticles (MB-PNP) are prepared by a new approach combining single and double emulsification techniques. Comparisons of MB-PNP obtained with the combined and the individual techniques are presented. Nanoparticles are characterized by dynamic light scattering, laser Doppler electrophoresis and scanning electron microscopy. Particles prepared by the combined technique presented hydrodynamic diameters of 186 nm. The sizes of MB-PNP obtained from the single emulsion technique are similar to the combined technique, while the diameter of particles prepared by double emulsion increased from 201 nm to 287 nm as the TDL increased. MB-PNP displayed an average zeta potential between -21 mV and -28 mV for all formulations. MB loading ranges between 0.3-1.4%, while the encapsulation efficiency ranges from 8-14%, both depending on the TDL and the preparation technique. In vitro release studies show a monophasic release profile that was analyzed by considering the mechanisms of initial burst, drug diffusion and a combination of them. Experimental results could be better described using a mathematical model of release that simultaneously combines the mechanisms of initial burst and drug diffusion. The approach presented to encapsulate MB and also to analyze the drug release could be extended to other drugs with partial solubility.