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Rheological Characterization, In Vitro and Ex Vivo Drug Release, Therapeutic Effectiveness and Safety Studies of Diclofenac Sodium, Loaded with Micronized Fumed Silicon Dioxide Gel

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Chemistry for a Clean and Healthy Planet (ICPAC 2018)

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Abstract

The present research has been undertaken with the aim to develop a topical gel formulation of diclofenac sodium using a micronized fumed silicon dioxide (Aerosil) gelled with a liquid paraffin (non-polar vehicle). The two gels, 8% (formulation A) and 10% (formulation B) were prepared from hydrophilic colloidal silicon dioxide (Aerosil 200) and their physicochemical characterization and efficacy as oleaginous ointment bases were investigated. They were evaluated for physicochemical properties such as homogeneity, grittiness, viscosity, pH, spreadability, drug content, skin irritancy, in vitro drug and ex vivo drug release. Compatibility studies were carried out using FT-IR spectroscopy. Developed gels were found to be comparable to marketed products in all physicochemical aspects tested. No significant changes in the peak pattern of IR spectra of pure diclofenac sodium implies that no chemical incompatibility between drug and excipients used in the formulations. Drug permeation through the rat abdominal skin membrane was slow as compared to the synthetic membrane for all the formulations tested. Permeation data for all the tested formulations were found to follow zero-order kinetics with Fickian diffusion mechanism, indicating that drug permeations were independent of the drug concentrations in the gels. The prepared gels showed significant analgesic activity in rats as compared to the control value. Also, the application of gels showed no skin irritation throughout the entire observation period. Based on the results of this investigation, formulation A with 8% aerosil gel base in liquid paraffin was found to be a promising formulation for further clinical investigations.

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Acknowledgements

The authors are thankful to the Dean College of Pharmacy and Health Sciences, Ajman University, Ajman, UAE for providing research facilities.

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences, College of Pharmacy, Ajman University, Ajman, UAE

    Mohammad W. Islam & Abd Elazim A. Ali

  2. Ministry of Health, Dubai, UAE

    Abdullah K. Alkindi

  3. Department of Pharmaceutics, Dubai Pharmacy College for Girls, Dubai, UAE

    Aliasgar Shahiwala

Authors
  1. Mohammad W. Islam
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  2. Abd Elazim A. Ali
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  3. Abdullah K. Alkindi
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  4. Aliasgar Shahiwala
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Corresponding author

Correspondence to Mohammad W. Islam .

Editor information

Editors and Affiliations

  1. Department of Chemistry, Faculty of Science, University of Mauritius, Reduit, Mauritius

    Ponnadurai Ramasami

  2. Dept of Chemistry, Faculty of Scien, University of Mauritius, Reduit, Mauritius

    Minu Gupta Bhowon

  3. Dept. of Chemistry, Faculty of Scie, University of Mauritius, Reduit, Mauritius

    Sabina Jhaumeer Laulloo

  4. Dept. of Chem., Fac. of Science, University of Mauritius, Reduit, Mauritius

    Henri Li Kam Wah

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Islam, M.W., Ali, A.E.A., Alkindi, A.K., Shahiwala, A. (2019). Rheological Characterization, In Vitro and Ex Vivo Drug Release, Therapeutic Effectiveness and Safety Studies of Diclofenac Sodium, Loaded with Micronized Fumed Silicon Dioxide Gel. In: Ramasami, P., Gupta Bhowon, M., Jhaumeer Laulloo, S., Li Kam Wah, H. (eds) Chemistry for a Clean and Healthy Planet. ICPAC 2018. Springer, Cham. https://doi.org/10.1007/978-3-030-20283-5_26

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