Long circulating PEGylated poly(D,L-lactide-co-glycolide) nanoparticulate delivery of Docetaxel to solid tumors.
OBJECTIVE
The aim of this study was to investigate the ability of PEGylated poly(D,L-lactide-co-glycolide) nanoparticles (NPs) to deliver Docetaxel (DTX) (an anticancer agent) to solid tumors.


METHODS
PLGA-mPEG diblock copolymers were synthesized by ring opening polymerization reaction and characterized by (1)H NMR, FT-IR and gel permeation chromatography. NPs, with a smooth spherical shape and near 100 nm size were prepared using the emulsion solvent evaporation technique and characterized. The drug release rate was investigated in acidic and physiological media (phosphate buffer saline, pH 5.0 and 7.4). The therapeutic efficacy and biocompatibility of NP formulations were evaluated for in vitro cytotoxicity by MTT assay using MCF-7 and C26 cell lines. The pharmacokinetic and biodistribution studies were performed on C26 tumor bearing mice. The antitumor efficacy of DTX NP formulations on C26 tumor bearing mice was investigated.


RESULTS
DTX-loaded PEGylated NPs increased the drug's biological half-life while providing substantial accumulation at the solid tumors. PEGylated NPs appear to be a promising alternate carrier for DTX having greater efficacy in inhibiting tumor growth.
Senthilkumar
Murugesan
M
Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr HS Gour University, Sagar, MP, India. senthilsagar@gmail.com
Mishra
Pradeep
P
Jain
Narendra Kumar
NK
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D045744:Cell Line, Tumor; D002850:Chromatography, Gel; D000077143:Docetaxel; D004337:Drug Carriers; D005260:Female; D006207:Half-Life; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles; D009368:Neoplasm Transplantation; D009374:Neoplasms, Experimental / Q000378:metabolism; D010316:Particle Size; D011091:Polyesters; D011092:Polyethylene Glycols / Q000737:chemistry*; D011098:Polyglactin 910 / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D017550:Spectroscopy, Fourier Transform Infrared; D043823:Taxoids / Q000008:administration & dosage / Q000493:pharmacokinetics*; D013997:Time Factors; D014018:Tissue Distribution
D000970:Antineoplastic Agents; D004337:Drug Carriers; D011091:Polyesters; D043823:Taxoids; C558447:methoxypolyethyleneglycol-poly(lactic-co-glycolic acid); D000077143:Docetaxel; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011098:Polyglactin 910; D011092:Polyethylene Glycols