Formulation and evaluation of injectable in situ forming microparticles for sustained delivery of lornoxicam.
The objective of this study is to formulate biodegradable in situ microparticles (ISM) containing lornoxicam for post-operative and arthritic pain management. ISM emulsions were prepared according to 25full factorial experimental design to investigate the influence of formulation variables on the release profile of the drug. The independent variables studied are the polymer type, polymer inherent viscosity, polymer concentration, oil type and polymer:oil ratio. In vitro drug release, microscopical examination, particle size determination and syringeability measurement were selected as dependent variables. The effect of γ-sterilization on the prepared formulae was also examined. The prepared formulae showed extended drug release over two weeks, and flow time below 5 s/ml. Scanning electron microscope revealed that the prepared microparticles were spherical in shape, with diameter ranging from 3.45 to 22.78 µm. In vivo pharmacokinetic evaluation of two selected optimum formulations in rabbits showed prolonged drug absorption indicated by delayed Tmaxand the extended mean residence time. In conclusion, the prepared injectable ISM could be a promising approach for providing extended delivery of lornoxicam with low initial burst effect.
a Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Cairo University , Cairo , Egypt.
Soad Ali
SA
Yehia
a Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Cairo University , Cairo , Egypt.
Sally Adel
SA
Abdel-Halim
a Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Cairo University , Cairo , Egypt.
Mary Yosry
MY
Aziz
D000818:Animals; D016503:Drug Delivery Systems / Q000379:methods*; D065546:Drug Liberation; D004655:Emulsions / Q000737:chemistry*; D053758:Nanoparticles; D010316:Particle Size; D010894:Piroxicam / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D011817:Rabbits; D014783:Viscosity
D004655:Emulsions; D010894:Piroxicam; C059451:lornoxicam
Biodegradable polymers; factorial design; parenteral sustained release; peanut oil; pharmacokinetic study; sesame oil