Design and development of gliclazide-loaded chitosan for oral sustained drug delivery: in vitro/in vivo evaluation.
Gliclazide (GLZ)/Chitosan microparticles were prepared with tripolyphosphate (TPP) by ionic cross-linking. The particle sizes of TPP-chitosan microparticles were in the range 675-887 µm and the loading efficiencies of drug was more than 94.0%. Chitosan concentration, TPP solution pH and glutaraldehyde volume added to the TPP cross-linking solution had an effect on the drug release characteristics. The microparticles were examined with scanning electron microscopy and infrared spectroscopy. Furthermore, pectin can interact with cationic chitosan on the surface of these TPP/chitosan microparticles to form a polyelectrolyte complex film for the improvement of the drug sustained-release performances. In vivo testing of the GLZ-chitosan microparticles in diabetic albino rabbits demonstrated significant antidiabetic effect of GLZ/chitosan microparticles after 8 h which lasts for 18 h, compared with GLZ powder which produced maximum hypoglycaemic effect after 4 h, suggesting that GLZ/chitosan microparticles are a valuable system for the long-term delivery of GLZ.
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11495, PO Box 22452, Kingdom of Saudi Arabia. nsybarakat@yahoo.com
Nahla S
NS
Barakat
Alanood S
AS
Almurshedi
D000284:Administration, Oral; D000818:Animals; D048271:Chitosan / Q000737:chemistry* / Q000494:pharmacology; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy; D016503:Drug Delivery Systems; D005907:Gliclazide / Q000737:chemistry* / Q000494:pharmacology; D005976:Glutaral / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000494:pharmacology; D008297:Male; D010316:Particle Size; D051381:Rats
D007004:Hypoglycemic Agents; D048271:Chitosan; D005907:Gliclazide; D005976:Glutaral