Transmucosal delivery of melatonin-encapsulated niosomes in a mucoadhesive gel.

Aim: A transmucosal niosome gel was developed to improve the pharmacokinetics of exogenous melatonin.

Materials & Methods: The melatonin niosomes (MN) gel was characterized and melatonin levels were determined in healthy volunteers.

Results: Micron-sized MN in a gel, mean ex vivo residence time of more than 3 h with maximum adhesiveness at 25 and 37°C showed similar in vitro release but different in vitro permeation to melatonin gel. Oral transmucosal MN gels, at 2.5, 5 and 10 mg, topically applied in 14 healthy volunteers in a randomized double-blinded crossover design with 7-day washout, gave dose-proportional pharmacokinetics, with improved absorption and prolonged systemic circulation.

Conclusion: The transmucosal MN gel provides a topical option for melatonin administration with substantial prolonged systemic delivery.