Mefenamic Acid-loaded Solid SMEDDS: An Innovative Aspect for Dose Reduction and Improved Pharmacodynamic Profile

Abstract

Aim: The current investigation is focused on solid self-microemulsifying drug-delivery systems (S-SMEDDS) of mefenamic acid (MFA) for improving pharmacodynamic activity. Methodology & results: Solubility assessment in various lipid excipients and optimization of pseudoternary plots were carried out for development of liquid SMEDDS. The optimized liquid SMEDD formulation was spray dried to solid dosage form and observed with enhanced amorphization or molecular dispersion of MFA in S-SMEDDS, as evident from x-ray diffractometry and differential scanning calorimetry studies. Enhanced in vitro dissolution rate of optimized formulation was observed, resulting in multifold enhancement in absorption profile of MFA, as compared with pure drug and marketed product. These studies further substantiate the dose reduction in SMEDDS by gaining equivalent therapeutic profile with marketed product. Enhanced analgesic and anti-inflammatory activity was observed with S-SMEDD formulations in acetic acid-induced writhings and carrageenan-induced paw edema models, respectively. Conclusion: The optimized S-SMEDD formulation holds great promise for enhancement of its physiochemical and biological attributes.

Keywords:

• analgesic activity
• bioavailability
• dose reduction
• mefenamic acid
• solubility

Supplementary data

To view the supplementary data that accompany this paper please visit the journal website at:www.tandfonline.com/doi/full/10.2217/epi-2016-0184

Acknowledgments

The authors are highly thankful to Avenue Remedies, India for providing gift sample of mefenamic acid for our research work. Emerging Life Sciences Facility in Guru Nanak Dev University for carrying out characterization studies is highly acknowledged.

Financial & competing interests disclosure

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart. This includes emplyment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

No writing assistance was utilized in the production of this manuscript.

Ethical conduct of research

The authors state that they have obtained approval from the Institutional Animals Ethics Committee of the Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, India (226PO/Re/CPCSEA/07).