title: Chitosan nanoparticles of 5-fluorouracil for ophthalmic delivery: characterization, in-vitro and in-vivo study.
abstract: The aim of this investigation was to develop 5-fluorouracil (5-FU) loaded chitosan nanoparticles (CH-DNPs) for ophthalmic delivery. CH-DNPs were fabricated by ionotropic gelation mechanism using chitosan (CH) and a polyanion (TPP). The nanoparticles were smooth and spherical, confirmed by scanning electron microscopy (SEM) and atomic force microscope (AFM). CH/TPP mass ratio and TPP significantly changed the particles size morphology and encapsulation efficiency. The nanoparticles size ranged from approximately 114 to 192 nm and had a positive zeta potential (30±4 mV). The encapsulation efficiency, loading capacity and recovery of DNPs were 8.12-34.32%, 3.14-15.24% and 24.22 to 67% respectively. Physical characterization was done by Fourier transform infrared (FT-IR) and X-ray diffraction (XRD). No interaction was observed in between drug and polymer and crystallinity of drug was not changed in drug loaded nanoparticles. In-vitro release study of DNPs showed diffusion controlled release. Bioavailability study of batch CS9 was studied in rabbit eye and compare to 5-FU solution. 5-FU level was significantly higher in aqueous humor of rabbit eye. Ocular tolerance was studied in the eye of New Zealand rabbits and tested formulation was non-irritant with no sign of inflammation.
authors.affiliation: Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, UP, India. rcnagarwal.rs.phe@itbhu.ac.in
authors.forename: Ramesh Chand
authors.initials: RC
authors.lastname: Nagarwal
authors.forename: Paras Nath
authors.initials: PN
authors.lastname: Singh
authors.forename: Shri
authors.initials: S
authors.lastname: Kant
authors.forename: Pralay
authors.initials: P
authors.lastname: Maiti
authors.forename: Jayanta Kumar
authors.initials: JK
authors.lastname: Pandit
mesh_terms: D000818:Animals; D048271:Chitosan / Q000008:administration & dosage* / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods*; D005123:Eye / Q000187:drug effects; D005260:Female; D005472:Fluorouracil / Q000008:administration & dosage* / Q000737:chemistry; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D010316:Particle Size; D011817:Rabbits; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D048271:Chitosan; D005472:Fluorouracil