Abstract
Drug administration through the transdermal route has optimized for the comfort of patients and easy application. However, the main limitation of transdermal drug delivery is the impermeability of the human skin. Recent advances on improvement of drug transport through the skin include elastic liposomes as a penetration enhancer. Entrapment of ferrofluids in the core of liposomes produces magnetoliposomes, which can be driven by a high-gradient magnetic field. The association of both strategies could enhance the penetration of elastic liposomes. This work relies on the preparation and characterization of elastic-magnetic liposomes designed to permeate through the skin. The incorporation of colloidal magnetite and the elastic component, octaethylene glycol laurate (PEG-8-L), in the structure of liposomes were evaluated. The capability of the elastic magnetoliposomes for permeation through nanopores of two stacked polycarbonate membranes was compared to conventional and elastic liposomes. Magnetite incorporation was dependent on vesicle diameter and size distribution as well as PEG-8-L incorporation into liposomes, demonstrating the capability of the fluid bilayer to accommodate the surfactant without disruption. On the contrary, PEG-8-L incorporation into magnetoliposomes promoted a decrease of average diameter and a lower PEG-8-L incorporation percentage as a result of reduction on the fluidity of the bilayer imparted by iron incorporation into the lipid structure. Elastic liposomes demonstrated an enhancement of the deformation capability, as compared with conventional liposomes. Conventional and elastic magnetoliposomes presented a reduced capability for deformation and permeation.
Acknowledgments
The authors are grateful to the Brazilian agencies, Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) and Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP), for their financial support and to Dr. Leandro Tessler from the State University of Campinas (Brazil) for the project and construction of the HGM system.
Declaration of interest
This research was supported by FAPESP (02/12637–9) and CNPq (150044/2004–6).