CPHI Solutions
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Discover how we achieved enhanced permeation, solubility, and improved antifungal performance.
Study and solution rationale
The efficacy of topical antifungal formulations depends fundamentally on the active ingredient’s ability to penetrate the stratum corneum and reach therapeutic concentrations at the site of infection. Yet conventional formulations frequently face challenges in overcoming this barrier effectively, particularly when delivering lipophilic compounds such as clotrimazole. Clotrimazole is a widely used broad-spectrum antifungal agent indicated for the treatment of dermatophyte infections and candidiasis. However, its poor aqueous solubility and limited penetration through the stratum corneum can restrict drug delivery to the target site, potentially impacting therapeutic performance.
Enhancing dermal permeation represents a key strategy for improving the topical delivery of lipophilic antifungal agents. To explore this approach, IMCD’s Pharmaceutical Technical Centre (PTC) in Mumbai developed and evaluated a series of topical cream formulations designed to improve the release and skin permeation of clotrimazole. The objective of this study was to investigate the effect of formulation composition on the release and permeability of clotrimazole from a 1% w/w cream formulation.
A series of formulations were developed and compared against a marketed clotrimazole cream using in vitro release testing (IVRT). The study evaluated the impact of different formulation approaches on clotrimazole release and permeability to identify strategies to enhance dermal delivery and potentially improve topical antifungal performance.
Target market
This formulation concept is ideally suited for:
- Topical antifungal creams and lotions
- Prescription and over-the-counter dermatology products
- Formulators seeking enhanced delivery of poorly soluble APIs
- Companies developing differentiated topical products for fungal skin infections
- Manufacturers looking to improve topical performance while maintaining formulation flexibility
Formulator benefits
The incorporation of a solubility and permeability enhancer into clotrimazole cream formulations delivered several performance advantages:
- Enhanced release and permeation of clotrimazole
- Concentration-dependent improvement in drug delivery
- Comparable performance to marketed product at low inclusion levels (1.5%)
- Significant increase in release rates at higher concentrations
- Potential to improve drug availability at the site of action
- Wide formulation latitude, with efficacy demonstrated from 1.5% to 10% w/w inclusion levels
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CPHI Solutions
Explore IMCD's CPHI solutions