Bicellar systems as new delivery strategy for topical application of flufenamic acid

• Published in: International journal of pharmaceutics Vol. 444; no. 1-2; pp. 60 - 69
• Main Authors: Rubio, L., Alonso, C., Rodríguez, G., Cócera, M., López-Iglesias, C., Coderch, L., De la Maza, A., Parra, J.L., López, O.
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 28.02.2013
• Subjects: absorption; Administration, Topical; Animals; Anti-Inflammatory Agents - administration & dosage; Anti-Inflammatory Agents - chemistry; ATR-FTIR; Bicellar systems; collagen; Drug delivery; Drug Delivery Systems; drugs; DSC; Female; Flufenamic acid; Flufenamic Acid - administration & dosage; Flufenamic Acid - chemistry; FS-TEM; In vitro percutaneous absorption; In Vitro Techniques; inflammation; microstructure; Nanostructures - administration & dosage; Nanostructures - chemistry; phospholipids; Phospholipids - administration & dosage; Phospholipids - chemistry; SAXS-SR; Skin - metabolism; Skin Absorption; Swine; topical application; transmission electron microscopy; X-radiation; FFA; C; D; ATR-FTIR; E; Drug delivery; L; FSTEM; SC; BSA; SPP; DSC; DHPC; Tm; Bicellar systems; Perc. Abs; DPPC; PBS; TEWL; CD; OR; FS-TEM; Flufenamic acid; SAXS-SR; In vitro percutaneous absorption; RF; HEX
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2013.01.034

In this work, bicellar systems, bilayered disc-shaped nanoaggregates formed in water by phospholipids, are proposed as a novel strategy for delivery of the anti-inflammatory flufenamic acid (FFA) to the skin. A comparative percutaneous penetration study of this drug in bicellar systems and other vehicles was conducted. The effects induced on the skin by the application of FFA in the different vehicles were analyzed by attenuated total reflectance-fourier transform infrared (ATR-FTIR). Additionally, using the microscopic technique freeze-substitution transmission electron microscopy (FSTEM) and X-ray scattering technique using synchrotron radiation (SAXS-SR), we studied the possible microstructural and organizational changes that were induced in the stratum corneum (SC) lipids and the collagen of the skin by the application of FFA bicellar systems. Bicellar systems exhibited a retarder effect on the percutaneous absorption of FFA with respect to the other vehicles without promoting disruption in the SC barrier function of the skin. Given that skin disruption is one of the main effects caused by inflammation, prevention of disruption and repair of the skin microstructure should be prioritized in anti-inflammatory formulations.