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A menthol-based solid dispersion technique for enhanced solubility and dissolution of sulfamethoxazole from an oral

Bibi F Choonara1, Yahya E Choonara, Pradeep Kumar

  • 1Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, 7 York Road, Parktown, 2193, South Africa.

AAPS Pharmscitech
|January 1, 2015
PubMed

Insights

Menthol solid dispersions significantly enhanced the solubility and dissolution of sulfamethoxazole, a poorly soluble antibiotic. This formulation approach improved oral drug delivery by controlling drug release rates.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Materials Science

Background:

  • Sulfamethoxazole, a BCS Class II drug, exhibits poor intrinsic solubility, limiting its oral bioavailability.
  • Developing effective drug delivery systems is crucial for enhancing the therapeutic efficacy of poorly soluble drugs like sulfamethoxazole.

Purpose of the Study:

  • To formulate and characterize menthol-based solid dispersions of sulfamethoxazole to improve its solubility and dissolution.
  • To evaluate the physicochemical properties and in vitro drug release of sulfamethoxazole-loaded matrix tablets.

Main Methods:

  • Preparation of sulfamethoxazole-menthol solid dispersions and hydroxypropyl methylcellulose (HPMC) matrix tablets.
  • Characterization using techniques such as crystallinity, melting point, molecular transitions, and textural analysis.
  • In vitro evaluation of swelling, degradation, solubility, and drug release profiles.

Main Results:

  • Menthol-based solid dispersions significantly improved sulfamethoxazole solubility and dissolution.
  • Matrix tablets demonstrated controlled in vitro drug release, with fractional releases ranging from 0.714 to 0.970.
  • Varying menthol concentrations influenced drug release rates over extended periods (12-56 hours).

Conclusions:

  • Menthol serves as an effective hydrophilic carrier for sulfamethoxazole, acting as a solubilizing and release-retarding agent.
  • Menthol-based solid dispersions offer a promising strategy for enhancing the oral delivery of poorly soluble drugs.
  • The developed matrix tablets show potential for controlled release of sulfamethoxazole, improving its therapeutic profile.

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