PHARMACEUTICAL NANOTECHNOLOGYZidovudine-loaded PLA and PLA–PEG blend nanoparticles: Influence of polymer type on phagocytic uptake by polymorphonuclear cells
Section snippets
INTRODUCTION
Poly(lactide acid) (PLA) nanoparticles have been extensively used for the development of controlled drug-delivery systems. PLA nanoparticles, due to their physicochemical properties (size, surface charge, and hydrophobicity), are recognized by polymorphonuclear neutrophils or mononuclear cells, inducing phagocytosis,1,2 after intravenous administration. The neutrophils and mononuclear cells recognize pathogenic microorganisms and also may recognize polymeric surfaces as foreign material,3 and
Materials
The polymers studied were poly(lactide acid) (PLA) (Mw 40–100 kDa) (viscosity 0.15–0.25) from Sigma (St. Louis, MO) and poly(ethylene glycol) (PEG) (Mw 6 kDa). The surfactant used in the emulsification process was polyvinyl alcohol (PVA) (18 kDa—85% hydrolyzed) from Sigma. The organic solvent was methylene chloride (Labsynth Ltd., Diadema, Brazil). Zidovudine was a gift from FURP (Brazil). Distilled water of Milli-Q quality was used as the suspending medium. Luminol, trypan blue solution and
Nanoparticles Characterization
The double emulsion-solvent evaporation method was successful in producing nanoparticles containing AZT. This method is particularly interesting to encapsulate hydrophilic molecules. The results of AZT encapsulation efficiency can be observed in Table 1. It was observed that for a constant PLA concentration, the efficiency encapsulation of AZT on nanoparticles increases with increasing PEG concentration in blend. Modifying the surface characteristics of nanoparticles it is possible to obtain
DISCUSSION
The objective of this study was to analyze the importance of nanoparticlecharacteristics in inducing the oxidative burst of neutrophils monitored by chemiluminescence luminol-dependent. Another aim was to examine if nanoparticles composed of blends containing PEG could have steric properties, and if the PEG ratio could affect the extent of phagocytosis. For copolymers these effect is well characterized and established, but for blends (physical mixture of polymers) not yet, since the forces that
Acknowledgements
The authors are grateful to Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)/Brazil for the financial support.
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