Deformable Liposomal Hydrogel for Dermal and Transdermal Delivery of Meloxicam

• Published in: International journal of nanomedicine Vol. 15; pp. 9319 - 9335
• Main Authors: Zhang, Zhang Julia, Osmałek, Tomasz, Michniak-Kohn, Bozena
• Format: Journal Article
• Language: English
• Published: New Zealand Dove Medical Press Limited 01.01.2020; Taylor & Francis Ltd; Dove
• Subjects: Administration, Cutaneous; Administration, Topical; Alzheimer's disease; Animals; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; Anti-Inflammatory Agents, Non-Steroidal - metabolism; Arthritis; Bioflavonoids; Chromatography; Drug dosages; Flavones; Flavonoids; Health aspects; High performance liquid chromatography; Humans; Hydrogels; Hydrogels - chemistry; Hydrophobic and Hydrophilic Interactions; Instrument industry; Lipids; Liposomes - chemistry; Male; Mechanical Phenomena; Meloxicam; Meloxicam - administration & dosage; Meloxicam - metabolism; Original Research; Particle Size; Permeability; Skin; Skin - metabolism; Skin Absorption; Swine; Viscosity; New York; United States; United States > US; poloxamer P407; ex vivo skin permeation; flavonoid; flavosome; transfersome
• ISSN: 1178-2013; 1176-9114; 1178-2013
• DOI: 10.2147/IJN.S274954

Meloxicam (MX) is a potent hydrophobic non-steroidal anti-inflammatory drug used to reduce inflammation and pain. However, its oral dosage form can cause many adverse gastrointestinal effects. In the present study, a poloxamer P407 based hydrogel system containing transfersomes or flavosomes has been prepared as a potential therapeutic vehicle for the topical delivery of MX. In this study, MX was encapsulated in conventional liposomes, transfersomes, and flavosomes. The obtained liposomal vesicles were characterized in terms of size, drug entrapment efficiency, zeta potential, and stability. These MX-loaded liposomal formulations were further incorporated into a poloxamer P407 gel and evaluated using rheological properties, a stability study and an ex vivo permeation study through human cadaver skin by both HPLC analysis and confocal laser scanning microscopy (CLSM). The developed deformable liposomes exhibited homogeneous vesicle sizes less than 120 nm with a higher entrapment efficiency as compared to conventional liposomes. The deformable liposomal gel formulations showed improved permeability compared to a conventional liposomal gel and a liposome-free gel. The enhancement effect was also clearly visible by CLSM. These deformable liposomal hydrogel formulations can be a promising alternative to conventional oral delivery of MX by topical administration. Notably, flavosome-loaded gel formulations displayed the highest permeability through the deeper layers of the skin and shortened lag time, indicating a potential faster on-site pain relief and anti-inflammatory effect.