Stomach-specific drug delivery of 5-fluorouracil using ethylcellulose floating microspheres.
A multiple-unit-type oral floating dosage form (FDF) of 5-Fluorouracil (5-FU) was developed to prolong gastric residence time for the treatment of stomach cancer. The floating microspheres were prepared by solvent evaporation method. The prepared microspheres were characterized for their micromeretic properties, floating behavior and entrapment efficiency; as well by Fourier transform infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD), thin layer chromatography (TLC) and scanning electron microscopy (SEM). The in vitro release studies and floating behavior were performed in HCl buffer pH 1.2, Phosphate buffer pH 4.5 and in Simulated Gastric Fluid (SGF). The best fit release kinetics was achieved with Higuchi plot. The yields of preparation were very high and low entrapment efficiencies were noticed with larger particle size for all the formulations. Mean particle size, entrapment efficiency and production yield were highly influenced by polymer concentration. It was concluded from the present investigation that porous Ethylcellulose microspheres are promising controlled release as well as stomach targeted carriers for 5-FU.
Vaghani
Subhash
S
Department of Pharmaceutics, PES College of Pharmacy, Hanumanthnagar, Bangalore, India. subhashvaghani@gmail.com
Vasanti
S
S
Chaturvedi
Kiran
K
Satish
C S
CS
Jivani
N P
NP
D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry*; D005472:Fluorouracil / Q000008:administration & dosage* / Q000493:pharmacokinetics; D005753:Gastric Mucosa / Q000378:metabolism; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D008863:Microspheres; D010316:Particle Size; D016062:Porosity
D000964:Antimetabolites, Antineoplastic; D003692:Delayed-Action Preparations; D005079:Excipients; C013517:ethyl cellulose; D002482:Cellulose; D005472:Fluorouracil