Abstract
Purpose: This article describes the preparation and characterization of folate conjugated nanoparticles using poly(lactide-co-glycolide)-poly(ethylene glycol)-folate (PLGA-PEG-FOL) polymer for targeted delivery of anticancer agents. Methods: PLGA-PEG-FOL was synthesized by coupling di-block copolymer (PLGA-PEG-NH2) with folic acid. PLGA-PEG-FOL polymer was characterized by 1H NMR, GPC and FTIR. PLGA-PEG-FOL polymer was employed in the preparation of doxorubicin (DOX) loaded nanoparticles by double emulsion solvent evaporation (DESE), single emulsion solvent evaporation (SESE) and dialysis methods. Nanoparticles were characterized for size, morphology, entrapment efficiency, in vitro release and folate content. The presence of folate on nanoparticle surface was also confirmed using transmission electron microscopy. Qualitative uptake and cell viability studies were carried out in FOL receptor-positive ovarian cancer cells (SKOV3). Results: DESE and SESE methods resulted in folate conjugated nanoparticles with an average size of 200 nm and entrapment efficiencies of 24.5 and 51.9% respectively. However, dialysis method resulted in microparticles with an average size of 2.5 μm. Folate conjugated nanoparticles exhibited higher uptake and cytotoxicity in SKOV3 cells in comparison with the pure DOX and unmodified nanoparticles. Conclusion: PLGA-PEG-FOL can be utilized in the preparation of surface modified nanoparticles for targeted delivery of anticancer agents to FOL-receptor-positive cancer cells.
Highlights
Nanoparticles are colloidal particulate systems with particle sizes ranging between 10-1000 nm
PLGA polymers, i.e. PLGA 65:35 (d,l-lactide : glycolide), molecular weight 40,000-75,000 Da, polyvinyl alcohol (PVA), folic acid, dialysis tubing made of cellulose membrane, mouse anti-folic acid, goat antimouse IgG labeled with gold nanoparticles (10 nm) were procured from Sigma Chemicals (St Louis, MO)
In the present study we have proposed a relatively easy strategy for the preparation of folate conjugated PLGA nanoparticles for both hydrophilic and hydrophobic drug molecules
Summary
Nanoparticles are colloidal particulate systems with particle sizes ranging between 10-1000 nm. Polymeric nanoparticles have gained lot of attention due to their versatile properties including: long shelf stability, high drug loading capacity, and their ability to deliver both hydrophilic and hydrophobic drug molecules via peroral, transmucosal and inhalation routes [1,2]. They are made up of biocompatible and biodegradable polymers obtained from either natural (chitosan, albumin, sodium alginate and gelatin) or synthetic (poly (lactic acid), poly (D,L-glycolide), poly (lactide-coglycolide), poly (caprolactones) and poly (cyanoacrylates)) sources [3]. These linkers prevent the uptake of nanoparticles by ReticuloEndothelial System (RES) and thereby increase the circulation time in blood [5]
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