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Subject Area

Pharmaceutical Technology

Abstract

Introduction: Lornoxicam (LRX), a member of the Oxicam class of non-steroidal anti-inflammatory drugs (NSAIDs), exhibits potent analgesic, anti-inflammatory, and antipyretic properties. Nevertheless, its effectiveness is hampered by high dosage requirements, a short half-life, and low and pH dependent water solubility, necessitating further research for enhanced therapeutic outcomes.

Methodology: This study introduces floating microsponges of LRX to enhance drug release duration and reduce dosing frequency. Microsponges were formulated using quasi-emulsion solvent diffusion with ethyl cellulose and polyvinyl alcohol (PVA) as sustained-release polymers. A 32 factorial design assessed the effects of ethyl cellulose (X1) and PVA (X2) concentrations on key parameters: Entrapment efficiency (%; Y1), In vitro buoyancy (%; Y2), particle size (µm; Y3) and Q12 hrs (%; Y4). Formulation optimization aimed to maximize Y1,Y2 and Y3 while Y4 constraint was set in between 80-85%. Characterization included Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), entrapment efficiency, buoyancy, particle size, dissolution studies, and stability assessments. Effectiveness of developed microsponges was tested by in vitro protein denaturation assay.

Results: The meticulous optimization process through the 32 factorial design yielded a final formulation that showcased impressive attributes. The entrapment efficiency of 83.29 ± 3.12 %, buoyancy reaching 74.28 ± 4.39, a particle size of 38 µm and Q12 hrs (%) of 82.14 ± 4.11 collectively contribute to the robustness of the floating microsponges. Additionally, the spherical nature of the microsponges, as revealed in the SEM study, further supports the reliability and consistency of the formulation. Furthermore, the formulation's performance in stability studies over a 6-month duration demonstrated its resilience to changes, affirming its suitability for long-term storage and use. This stability profile enhances the practical applicability of the developed floating microsponges, emphasizing their potential for reliable and sustained therapeutic effects.

Conclusion: The application of floating microsponges offers a promising approach to enhance LRX therapy.

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