Injectable long acting chitosan/tripolyphosphate microspheres for the intra-articular delivery of lornoxicam: Optimization and in vivo evaluation.
Chitosan microspheres were formulated for the intra-articular delivery of lornoxicam in knee osteoarthritis, to minimize associated side-effects after prolonged oral administration. Ionotropic-gelation technique was employed using tripolyphosphate as anionic cross-linker. Full-factorial design experiment was conducted to optimize lornoxicam entrapment-efficiency%. Formulations were assessed for their particle size, in-vitro drug release, Scanning electron microscopy, Differential-scanning-calorimetry and Fourier transform infra-red spectroscopy studies. Changing independent variables, chitosan pH, TPP pH and lornoxicam concentration resulted in different values of entrapment-efficiency% ranging from 13.5%±0.35 to 59.5%±2.2. Particle size ranged from 3.57μm±0.02 to 6.12μm±0.00 and lornoxicam%release was prolonged for up to 8days. SEM results showed spherical shape of the microspheres. FTIR and DSC studies confirmed the crosslinking of chitosan with tripolyphosphate. In-vivo therapeutic effect of lornoxicam microspheres was investigated using Monosodiumiodoacetate (MIA) induced osteoarthritis model in rats. Optimized formula showed long-term in-vivo anti-inflammatory effect relative to lornoxicam solution injected intra-articularly with significant reduction of histological, inflammatory and biochemical parameters of osteoarthritis.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Abbassia, Cairo, Egypt.
Hend
H
Abd-Allah
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Abbassia, Cairo, Egypt. Electronic address: amany.kamel@yahoo.com.
Amany O
AO
Kamel
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Abbassia, Cairo, Egypt.
Omaima A
OA
Sammour
D000818:Animals; D048271:Chitosan / Q000008:administration & dosage / Q000737:chemistry*; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D065546:Drug Liberation; D007267:Injections; D007596:Joints / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D008863:Microspheres; D010710:Phosphates / Q000737:chemistry*; D010894:Piroxicam / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D051381:Rats
D004337:Drug Carriers; D010710:Phosphates; D010894:Piroxicam; D048271:Chitosan; C059451:lornoxicam
Chitosan; Intra-articular; Lornoxicam; Microspheres; Monoiodoacetate; Tripolyphosphate