title: 5-Fluorouracil-lipid conjugate: potential candidate for drug delivery through encapsulation in hydrophobic polyester-based nanoparticles.
abstract: The encapsulation of 5-fluorouracil (5-FU) in hydrophobic polymeric materials is made feasible by a lipid-based prodrug approach. A lipid-5-FU conjugate of 5-FU with palmitic acid was synthesized in two-step process. A synthesized dipalmitoyl derivative (5-FUDIPAL) was characterized using Fourier transform infrared spectroscopy and (1)H-nuclear magnetic resonance. The 5-FUDIPAL was encapsulated in polyester-based polymers by the double emulsion-solvent evaporation method. The nanoparticles were characterized by scanning electron microscopy, transmission electron microscopy and dynamic light scattering. The thermal stability was assessed by differential scanning calorimetry data. In vitro release kinetics measurements of the drug from nanoparticles showed the controlled release pattern over a period of time. Cytotoxicity measurements by MTT assay confirmed that dipalmitoyl derivative in nano formulation successfully inhibited the cell growth. Thus the combined physical and biological evaluation of the different polyester-based nanoparticle containing the modified drug showed a facile approach to delivering 5-FU to the tumour site with enhanced efficacy.
authors.affiliation: Chemical Biology, Rajiv Gandhi Centre for Biotechnology, Poojappura, Thiruvananthapuram 695 014, Kerala, India.
authors.forename: N
authors.initials: N
authors.lastname: Ashwanikumar
authors.affiliation: Cancer Research Programme, Rajiv Gandhi Centre for Biotechnology, Poojappura, Thiruvananthapuram 695 014, Kerala, India.
authors.forename: Nisha Asok
authors.initials: NA
authors.lastname: Kumar
authors.affiliation: Cancer Research Programme, Rajiv Gandhi Centre for Biotechnology, Poojappura, Thiruvananthapuram 695 014, Kerala, India.
authors.forename: S
authors.initials: S
authors.lastname: Asha Nair
authors.affiliation: Chemical Biology, Rajiv Gandhi Centre for Biotechnology, Poojappura, Thiruvananthapuram 695 014, Kerala, India. Electronic address: gsvinod@rgcb.res.in.
authors.forename: G S
authors.initials: GS
authors.lastname: Vinod Kumar
mesh_terms: D002152:Calorimetry, Differential Scanning; D016923:Cell Death / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D005472:Fluorouracil / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045325:HCT116 Cells; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D020128:Inhibitory Concentration 50; D019344:Lactic Acid / Q000737:chemistry; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D019308:Palmitic Acid / Q000138:chemical synthesis / Q000737:chemistry; D010316:Particle Size; D011091:Polyesters / Q000138:chemical synthesis / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D066244:Proton Magnetic Resonance Spectroscopy; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
chemical_list: D008055:Lipids; D011091:Polyesters; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019308:Palmitic Acid; D019344:Lactic Acid; D005472:Fluorouracil
keywords: 5-Fluorouracil; Nanoparticles; Palmitic acid; Polyester