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Melatonin Delivery: Transdermal and Transbuccal Evaluation in Different Vehicles
Ana Flo1, Ana C Calpena1, Lyda Halbaut1
1Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of Barcelona, Barcelona, Spain.
Pharmaceutical Research
|March 10, 2016
Summary
Melatonin (MLT) permeation through skin and buccal mucosa varies by vehicle. Carbopol® 940 (C940) and Montanov® 68 (M68) showed high skin permeation, while sodium carboxymethylcellulose (NaCMC) excelled for buccal delivery.
Area of Science:
- Pharmacology and Pharmaceutics
- Drug Delivery Systems
- Dermatology and Oral Medicine
Background:
- Melatonin (MLT) possesses significant antioxidant and anticarcinogenic properties, making it a potential therapeutic agent.
- Understanding drug vehicle interactions is crucial for optimizing delivery and efficacy.
- Buccal and skin routes offer alternative pathways for systemic drug administration.
Purpose of the Study:
- To evaluate the impact of various pharmaceutical vehicles on melatonin permeation.
- To assess melatonin release and stability in different formulations.
- To compare the efficacy of different vehicles for both skin and buccal mucosal delivery.
Main Methods:
- Formulation characterization including rheology and drug release studies.
- In vitro permeation studies using human skin and porcine buccal mucosa.
- Photostability testing of melatonin in various vehicles.
Main Results:
- Montanov® 68 (M68) and Carbopol® 940 (C940) demonstrated high skin permeation for melatonin.
- Sodium carboxymethylcellulose (NaCMC) proved to be the most effective vehicle for buccal permeation.
- Melatonin showed significant degradation in solution and Orabase® (OB), but was stable in most other formulations.
Conclusions:
- Carbopol® 940 (C940) or Montanov® 68 (M68) are suitable for systemic melatonin delivery via skin.
- Sodium carboxymethylcellulose (NaCMC) is recommended for systemic melatonin delivery through the buccal mucosa.
- For local action, Montanov® 68 (M68) or Poloxamer 407 (P407) and Pluronic® lecithin organogel (PLO) are suggested for skin and buccal mucosa, respectively.
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