EC Pharmacology And Toxicology

Poorly water-soluble drugs like ibuprofen present challenges related to limited absorption and gastrointestinal (GI) side effects. This work aims at preparing asymmetric membrane floating microspheres (AMFM) with the purpose of enhancing the solubility, gastric retention, and therapeutic efficiency of ibuprofen, thereby decreasing its adverse effects. Ibuprofen-AMFM were prepared by a phase inversion technique, which resulted in the formation of microspheres containing a porous inner layer and a non-porous outer membrane as evidenced by scanning electron microscopy. This special structure allowed the microspheres to float in gastric fluid for up to 12 hours, thereby increasing the gastric residence time. The microspheres showed high drug loading of 89.52 ± 1.23% and process yield 74.23 ± 0.65%. In vitro drug release studies indicated that the drug release gets extended up to a period of 12 hours through Fickian diffusion and Higuchi kinetics. In vivo anti-inflammatory studies also demonstrated increased efficacy of ibuprofen-AMFM, with an increase in inflammation inhibition of about 85.34%, compared to 60.92% with pure ibuprofen. All the above observations indicated that ibuprofen-AMFM was one of the most efficient ways to improve drug bioavailability and patient compliance, hence being a prospective delivery system for poorly soluble drugs.

 Keywords: Ibuprofen; Asymmetric Membrane; Floating; Kinetics; Phase Inversion

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