Combination of lipid nanoparticles and iontophoresis for enhanced lopinavir skin permeation: Impact of electric current on lipid dynamics
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2022
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Nanostructured lipid carriers (NLC)-loaded with lopinavir (LPV) were developed for its iontophoretic transdermal
delivery. Electronic paramagnetic resonance (EPR) spectroscopy of fatty acid spin labels and differential
scanning calorimetry (DSC) were applied to investigate the lipid dynamic behavior of NLC before and after the
electrical current. In vitro release and permeation studies, with and without anodic and cathodic iontophoresis
were also performed. NLC-LPV had nanometric size (179.0 ± 2.5 nm), high drug load (~x223C 4.14%) and
entrapment efficiency (EE) (~x223C 80%). NLC-LPV was chemically and physically stable after applying an
electric current. The electrical current reduced EE after 3 h (67.21 ± 2.64%), resulting in faster LPV in vitro
release. EPR demonstrated that iontophoresis decreased NLC lipid dynamics, which is a long-lasting effect. DSC
studies demonstrated that electrical current could trigger the polymorphic transition of NLC and drug solubilization
in the lipid matrix. NLC-LPV, combined with iontophoresis, allowed drug quantification in the receptor
medium, unlike unloaded drugs. Cathodic iontophoresis enabled the quantification of about 7.9 μg/cm2 of LPV in
the receptor medium. Passive NLC-LPV studies had to be done for an additional 42 h to achieve similar concentrations.
Besides, anodic iontophoresis increased by 1.8-fold the amount of LPV in the receptor medium,
demonstrating a promising antiviral therapy strategy.
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Nanostructured lipid carrier, Electronic paramagnetic resonance, Lopinavir, Transdermal administration Iontophoresis, Antiviral therapy
Citação
MOURA, Rayssa Barbary Pedroza; ANDRADE, Lígia Marquez; ALONSO, Lais; ALONSO, Antonio; MARRETO, Ricardo Neves; TAVEIRA, Stephânia Fleury. Combination of lipid nanoparticles and iontophoresis for enhanced lopinavir skin permeation: impact of electric current on lipid dynamics. European Journal of Pharmaceutical Sciences, Amsterdam, v. 168, e106048, 2022. DOI: 10.1016/j.ejps.2021.106048. Disponível em: https://www.sciencedirect.com/science/article/pii/S092809872100350X?via%3Dihub. Acesso em: 14 abr. 2023.