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Optimization of topical erythromycin formulations by ion pairing
S Matschiner1, R Neubert, W Wohlrab
1College of Pharmacy, Martin Luther University, Halle/Saale, Germany.
Skin Pharmacology : the Official Journal of the Skin Pharmacology Society
|January 1, 1995
Summary
Improving topical acne treatment, ion pairing significantly enhances erythromycin (ERY) penetration into skin follicles. This allows for lower antibiotic dosages, offering a more effective and potentially safer acne vulgaris therapy.
Area of Science:
- Dermatology
- Pharmaceutics
- Drug Delivery
Background:
- Acne vulgaris treatment often relies on topical antibiotics like erythromycin (ERY).
- Effective treatment requires ERY to penetrate sebaceous follicles to reduce microbial load.
- Improving ERY's lipophilicity is crucial for enhanced follicular penetration.
Purpose of the Study:
- To enhance the lipophilicity of erythromycin (ERY) through ion pairing.
- To develop an optimized formulation for improved ion pair penetration.
- To compare the optimized formulation against ethanol-based formulations and a commercial product (Zineryt).
Main Methods:
- Lipophilicity was assessed using partition coefficients (PC).
- ERY penetration was evaluated using a modified multilayer membrane system (MMS).
- Formulations were compared based on ERY penetration efficacy.
Main Results:
- Ion pairing ERY with octadecansulfonate increased its penetration into a lipophilic system threefold compared to ERY base alone.
- Optimized vehicle formulation significantly enhanced ion pair penetration.
- Reduced antibiotic dosage is achievable with optimized ion pair vehicle.
Conclusions:
- Ion pairing is an effective strategy to improve ERY lipophilicity and follicular penetration for acne treatment.
- Optimized formulations can enhance topical antibiotic delivery, potentially reducing required dosages.
- This approach offers a promising avenue for more effective topical acne vulgaris therapy.