Improving ex vivo skin permeation of non-steroidal anti-inflammatory drugs: Enhancing extemporaneous transformation of liposomes into planar lipid bilayers

• Published in: International journal of pharmaceutics Vol. 461; no. 1-2; pp. 427 - 436
• Main Authors: Vázquez-González, Martha L., Bernad, Rafael, Calpena, Ana C., Domènech, Oscar, Montero, M.T., Hernández-Borrell, Jordi
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 30-01-2014
• Subjects: Administration, Cutaneous; AFM; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics; Chemistry, Pharmaceutical - methods; Drug Delivery Systems; Enhancers; Female; Humans; Ibuprofen; Ibuprofen - administration & dosage; Ibuprofen - pharmacokinetics; Lipid Bilayers - metabolism; Liposomes; Microscopy, Atomic Force; Skin - metabolism; Skin Absorption; Surface-Active Agents - chemistry; Transdermal drug delivery; AFM; Transdermal drug delivery; Enhancers; Ibuprofen (PubChem CID: 3672); Liposomes; Ibuprofen
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2013.12.009

•Ibuprofen is encapsulated in liposomes for topic application.•Surfactant enhancers increase transdermal permeation of encapsulated ibuprofen.•Enhancers transform liposomes into planar structures.•Lipid bilayer-like structures are observed onto the skin by AFM.
Transdermal delivery of active principles is a versatile method widely used in medicine. The main drawback for the transdermal route, however, is the low efficiency achieved in the absorption of many drugs, mostly due to the complexity of the skin barrier. To improve drug delivery through the skin, we prepared and characterized liposomes loaded with ibuprofen and designed pharmaceutical formulations based on the extemporaneous addition of penetration enhancer (PE) surfactants. Afterwards, permeation and release studies were carried out. According to the permeation studies, the ibuprofen liposomal formulation supplemented with PEs exhibited similar therapeutic effects, but at lower doses (20%) comparing with a commercial formulation used as a reference. Atomic force microscopy (AFM) was used to investigate the effect caused by PEs on the adsorption mechanism of liposomal formulations onto the skin. Non-fused liposomes, bilayers and multilayered lipid structures were observed. The transformation of vesicles into planar structures is proposed as a possible rationale for explaining the lower doses required when a liposome formulation is supplemented with surfactant PEs.