Polyethyleneimine/poly-(γ-glutamic acid)/poly(lactide-co-glycolide) nanoparticles for loading and releasing antiretroviral drug

Nanoparticles (NPs) with ternary components of polyethyleneimine (PEI), poly-(gamma-glutamic acid) (gamma-PGA), and poly(lactide-co-glycolide) (PLGA) were applied to carry and release saquinavir (SQV). Hydrophobic SQV was encapsulated in the particle core composed of PLGA to form SQV-PLGA NPs, and the surface of SQV-PLGA NPs was grafted successively with hydrophilic gamma-PGA and PEI (PEI/gamma-PGA/SQV-PLGA NPs). The morphological images revealed that PEI/gamma-PGA/SQV-PLGA NPs were spheroid-like, in general. An increase in the concentration of didecyl dimethylammonium bromide and a reduction in the dose of SQV enhanced the entrapment efficiency of SQV in PLGA NPs. In addition, an increment in the molecular weight of gamma-PGA reduced the grafting efficiency of PEI on gamma-PGA/SQV-PLGA NPs. An increase in the weight percentage of PEI enhanced the average particle diameter. However, the grafting efficiency of PEI on gamma-PGA/SQV-PLGA NPs and the dissolution rate of SQV from PEI/gamma-PGA/SQV-PLGA NPs reduced when the weight percentage of PEI increased. PEI/gamma-PGA/SQV-PLGA NPs are an innovative drug delivery system and can be used for antiretroviral trials. (C) 2011 Elsevier B.V. All rights reserved.