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A Novel Approach for the Availability and Ocular Delivery of Tenoxicam Potassium: Synthesis, Characterization, and In Vivo Application

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Abstract

Tenoxicam (TX) is a non-steroidal anti-inflammatory agent that can be used to control pain in various ophthalmic lesions like cataracts, refractive surgery, and corneal abrasion. TX has a very slightly aqueous solubility of 0.072 mg/mL resulting in difficulty to be formulated in ophthalmic solutions. This study aims to improve TX solubility by converting it into its potassium salt to achieve a target of 10 mg/mL (1%w/v) concentration of TX in the desired aqueous medium for the formulation of aqueous ophthalmic solutions. The synthesized TX salt was characterized by different evaluation parameters such as solubility studies, 1H NMR, IR, and elemental analyses. Different TX potassium solutions were formulated at concentrations of 0.5% and 1% w/v using different viscosity-imparting agents. The prepared solutions were characterized for their physicochemical properties including visual inspection, pH, rheological, in vitro release, and kinetic behavior. Also, the formulations were biologically evaluated in vivo using male albino rabbits. The obtained results showed the successful synthesis of TX salt, as indicated by IR and NMR, and elemental analysis. The solubility study showed that the solubility of TX was improved hugely to 18 mg/mL (250-fold). In addition, the results showed that the prepared formulations showed acceptable physicochemical properties. The highest release rate was obtained with formula F1, which contains no viscosity-imparting agents. While as, the lowest release rate was obtained in the case of formula F9, composed of Pluronic F127 (12% w/v). The in vivo results showed that TX optimized ophthalmic solutions F8 and F9 inhibited the redness and edema in an extended or sustained manner.

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Acknowledgements

The authors are thankful to the Researchers Supporting Project number (RSP2023R516) at King Saud University, Riyadh, Saudi Arabia. Also, the authors would like to thank the Deanship of Scientific Research at Shaqra University for supporting this work.

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Authors and Affiliations

  1. Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Al-Azhar University, Assiut, 71524, Egypt

    Shaaban K. Osman, Ahmed M. Mohammed, Ahmed A. Abdellatif & Mohammed A. Ibrahim

  2. Department of Pharmaceutical Technology, Faculty of Pharmacy, Minofia University, Minofia, Egypt

    Taher M. Yassin

  3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Assiut, 71524, Egypt

    Abdallah M. Alfayomy

  4. Department of Pharmaceutics, College of Pharmacy, Qassim University, Qassim, 51452, Saudi Arabia

    Ahmed A. Abdellatif

  5. Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, 11451, Saudi Arabia

    Wael A. Mahdi & Sultan Alshehri

  6. Department of Pharmaceutical Sciences, College of Pharmacy, Shaqra University, Shaqra, 11961, Saudi Arabia

    Mohamed A. El Hamd

  7. Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, South Valley University, Qena, 83523, Egypt

    Mohamed A. El Hamd

  8. Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt

    Hatem Sarhan

Authors
  1. Shaaban K. Osman
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Contributions

Conceptualization, S.K. Osman, and M.A. Ibrahim; Data curation, T.M. Yassin, A.M. Mohamed, A.M. Alfayomy, and S.K. Osman; Formal analysis, A.M. Mohammed, T.M. Yaseen, A.M. Alfayomy, and S.K. Osman; Investigation, A.A.H. Abdellatif and S.K. Osman; Methodology, S.K. Osman, T.M. Yassin, and A.M. Mohamed; Project administration, M.A. El Hamd, A.A.H. Abdellatif, M.A. Ibrahim, and S.K. Osman; Resources, A.A.H. Abdellatif, H. Sarhan, and S.K. Osman; Software, A.M. Mohammed, W.A. Mahdi, S. Alshehri, and M.A. Ibrahim; Validation, M.A. El Hamd, A.A.H. Abdellatif and A.M. Alfayomy; Visualization, T.M. Yaseen, M.A. Ibrahim, and S.K. Osman; Writing—original draft, A.M. Mohammed, T.M. Yassin, and S.K. Osman; Writing—review and editing, H. Sarhan, A. H. Abdellatif, W.A. Mahdi, S. Alshehri, and S. K. Osman.

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Correspondence to Shaaban K. Osman or Mohamed A. El Hamd.

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Osman, S.K., Yassin, T.M., Mohammed, A.M. et al. A Novel Approach for the Availability and Ocular Delivery of Tenoxicam Potassium: Synthesis, Characterization, and In Vivo Application. AAPS PharmSciTech 24, 44 (2023). https://doi.org/10.1208/s12249-022-02487-3

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