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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
Published on: July 27, 2022
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Topical delivery of roxithromycin solid-state forms entrapped in vesicles
Candice Csongradi1, Jeanetta du Plessis1, Marique Elizabeth Aucamp1
1Centre of Excellence for Pharmaceutical Sciences (Pharmacen), North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
Summary
New vesicle systems successfully delivered amorphous roxithromycin to the dermis for acne treatment. Amorphous forms showed improved topical delivery compared to crystalline forms, targeting Propionibacterium acnes effectively.
Area of Science:
- Pharmaceutical Sciences
- Dermatology
- Drug Delivery Systems
Background:
- Acne vulgaris treatment is evolving with interest in novel antibiotic formulations.
- Targeted delivery of antibiotics to the dermis is crucial for efficacy against Propionibacterium acnes.
Purpose of the Study:
- To evaluate the topical delivery of different roxithromycin solid-state forms (crystalline and amorphous) using vesicle systems.
- To determine if amorphous roxithromycin enhances topical delivery for acne treatment.
Main Methods:
- Encapsulation of roxithromycin crystalline and amorphous forms into niosomes, proniosomes, ufosomes, and pro-ufosomes.
- Characterization of vesicles using microscopy, droplet size analysis, pH, zeta-potential, and entrapment efficiency.
- Comparative release and topical diffusion studies to assess delivery to skin layers.
Main Results:
- Vesicle systems were successfully prepared with optimal properties for topical delivery.
- All formulations achieved targeted delivery to the epidermis-dermis, with no drug found in the receptor compartment or stratum corneum.
- Niosomes containing amorphous roxithromycin demonstrated superior topical delivery compared to crystalline forms.
Conclusions:
- Targeted delivery of roxithromycin to the dermis was successfully achieved using vesicle systems.
- Amorphous roxithromycin solid-state forms exhibited improved topical delivery over crystalline forms.
- These findings support the potential of amorphous roxithromycin in advanced vesicle-based topical formulations for acne vulgaris.
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