title: Heparin-appended polycaprolactone core/corona nanoparticles for site specific delivery of 5-fluorouracil.
abstract: The aim of the present work is to formulate heparin-modified-polycaprolactone (HEP) core shell nanoparticles (NPs) of 5-fluorouracil (5-FU). These NPs were characterized for various in vitro parameters like particle size, zeta potential, etc. HEP NPs were found to maintain comparatively slower drug release pattern (98.9% in 96 h) than PCL NPs. Cytotoxicity studies demonstrated a massive cytotoxic potential of 5-FU-loaded HEP NPs in A549, MDA-MD-435, and SK-OV-3 cancer cell lines. Pharmacokinetic parameters were also determined in blood after IV administration of HEP NPs: AUC, Cmax, MRT, and Tmaxvalues are 6096.075 ± 5.90 μg h/mL, 144.38 ± 1.52 μg/L, 58.71 ± 0.25 h, 96 ± 0.50 h, respectively and 117.92 ± 1.78, 45.35 ± 3.00, 1.2 ± 0.25, 0.5 ± 0.02 in plain 5-FU solution.
authors.affiliation: a Department of Pharmaceutics, Drug Delivery and Nanotechnology Laboratories , Guru Ramdas Khalsa Institute of Science and Technology, Pharmacy , Jabalpur , India.
authors.forename: Ashish
authors.initials: A
authors.lastname: Garg
authors.affiliation: a Department of Pharmaceutics, Drug Delivery and Nanotechnology Laboratories , Guru Ramdas Khalsa Institute of Science and Technology, Pharmacy , Jabalpur , India.
authors.forename: Vaibhav
authors.initials: V
authors.lastname: Patel
authors.affiliation: b Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences , Dr. H. S. Gour Vishwavidyalaya , Sagar , Madhya Pradesh , India.
authors.forename: Rajeev
authors.initials: R
authors.lastname: Sharma
authors.affiliation: c Nanotechnology Project Laboratories, Department of Pharmaceutics , Bhagyoday Tirth Pharmacy College , Sagar , Madhya Pradesh , India.
authors.forename: Amit
authors.initials: A
authors.lastname: Jain
authors.affiliation: c Nanotechnology Project Laboratories, Department of Pharmaceutics , Bhagyoday Tirth Pharmacy College , Sagar , Madhya Pradesh , India.
authors.forename: Awesh K
authors.initials: AK
authors.lastname: Yadav
mesh_terms: D000072283:A549 Cells; D016503:Drug Delivery Systems / Q000379:methods*; D005472:Fluorouracil / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D006493:Heparin / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D053758:Nanoparticles / Q000737:chemistry*; D011091:Polyesters / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D011091:Polyesters; C016240:polycaprolactone; D006493:Heparin; D005472:Fluorouracil
keywords: 5-fluorouracil; Cellular cytotoxicity; heparin; nanoparticles; polycaprolactone