Preparation and evaluation of in vitro properties of naproxen microspheres prepared with sodium alginate

Abstract

Background: Naproxen is a nonsteroidal anti-inflammatory drug (NSAID). Naproxen is cyclooxygenase (COX) inhibitor and reduces prostaglandin and shows its anti-inflammatory, ant-pain and exhibits gastrointestinal side effects. Objective: The present work was undertaken to formulate microparticles of naproxen with the objective of improving the therapeutic efficacy, patient compliance and bioavailability. Methods: Ionotropic gelation was used to entrap naproxen into sodium alginate (Na Alg) microspheres as a potential drug carrier for the oral drug delivery system. Microparticles with different drug to polymer ratios were prepared and characterized for encapsulation efficiency, particle size, DSC (Differential Scanning Calormetriy), FTIR (Fourier transform infara red) and drug release profiles. Results: The best drug to polymer ratio for microparticles was 1:4 (F3) with 200 mg naproxen and 800 mg Na Alg. The microparticles formulation F1 (200 mg drug and 200 mg Na Alg), F2 (200 mg drug and 400 mg Na Alg) and F3 showed loading efficiency of 61.93%, 77.86% and 85.50%, production yields of 100% (for all of formulations) and mean particle size of 1219.17, 1427.62 and 1737.80 µm respectively. The DSC showed stable character of naproxen in the drug loaded microparticles and also revealed amorphous form. The FTIR results suggest that the drug maintain its chemical stability during the encapsulation process. The results were found that microparticles of F3 prepared had slower and low release than the microparticles of F1, F2 and naproxen powder untreated (p <o.o5). The drug release rate had decrease by an increase in alginate sodium polymer concentration. Conclusions: It was concluded that the alginate formulations exhibit promising properties of a sustained release form for naproxen drug and that they provide distinct tissue protection in the stomach.