A new melatonin oral delivery platform based on orodispersible films containing solid lipid microparticles.

An innovative delivery system for melatonin, based on the incorporation of solid lipid microparticles in orodispersible films (ODFs) made of maltodextrin, was designed and developed. Lipid microparticles at two different melatonin concentrations (10 and 20% w/w) were produced by the spray congealing technology using two different lipid carrier (tristearin and hydrogenated castor oil) and characterized in terms of size, solid state, drug loading and drug release pattern. Tristearin microparticles were discarded due to a polymorphic modification of the carrier. The incorporation of hydrogenated castor oil microparticles in ODFs by using the casting method did not alter significantly the shape and dimension of the microparticles and the mechanical properties (elasticity and strength) of the films, which remained acceptable for manufacturing and handling. The in vitro release studies performed in saliva, gastric and intestinal simulated media on ODFs containing melatonin loaded in hydrogenated castor oil microaparticles revealed the possibility to combine with an immediate release of the drug and a sustained release over at least 5 h period. In conclusion, the proposed drug delivery system maintains the advantages of ODFs, i.e. the suitability to be swallowed without water, and permits the tuning of drug release according to the clinical needs by modulating the ratio of free and microencapsulated drug in the ODF.