Design, development and characterization of transdermal patch of methadone

• Published in: Journal of drug delivery science and technology Vol. 42; pp. 255 - 260
• Main Authors: Muñoz, M.D., Castán, H., Ruiz, M.A., Morales, M.E.
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.12.2017
• Subjects: Chronic pain; Enhancer; Methadone; Transdermal patch; Methadone; Enhancer; Transdermal patch; Chronic pain
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2017.04.011

The methadone has been the standard treatment for opioid addiction since the 1960s. In addition, methadone antagonizes the NMDA receptor and inhibits the reuptake of serotonin and norepinephrine. The methadone effects are in the central nervous system (CNS) and peripheral, its agonist μ action gives analgesic activity and its NMDA action and the inhibitions over monoamines can has a relevant paper in neuropathic pain treatment. Transdermal patch of methadone was prepared to improve adherence by the patient and it could be an alternative in the treatment of the chronic pain. Therefore, the aim of this research study was to design a bio-adhesive monolayer system to be applied like methadone deposit. For this purpose, we tested a copolymer that is plastoid® and PVA. The prepared formulations were evaluated for various parameters like film thickness, content uniformity, water vapour permeability (WVP), microphotographic study, calorimetric analysis, in vitro release study and in vitro permeation study. However, problems were detected relating to drug transfer through the skin. These were solved by incorporating enhancers into the patch formulation. The chosen enhancer was DMSO, since it increased Methadone permeation by up to 70% in comparison with patches with no enhancer. [Display omitted] •Transdermal patch of methadone was could be an alternative in the treatment of the chronic pain.•Study of characterization, release, dissolution and permeation of transdermal systems.•The film obtained was characterized by being transparent, homogeneous and flexible.•Results indicate that the system studied allows an adequate permeation of methadone.