6533b829fe1ef96bd128986a

RESEARCH PRODUCT

Influence of Chemical Enhancers and Iontophoresis on the In Vitro Transdermal Permeation of Propranolol: Evaluation by Dermatopharmacokinetics

María Sebastián-morellóVirginia MerinoM. Begoña Delgado-charroAlicia López-castellanoC. Balaguer-fernándezM.a. Calatayud-pascual

subject

Drugdermatopharmacokineticsmedia_common.quotation_subjectChemical enhancerslcsh:RS1-441Pharmaceutical SciencePropanol - Uso terapéutico.02 engineering and technologyPropranololMedicamentos - Administración.030226 pharmacology & pharmacyArticlelcsh:Pharmacy and materia medicaIonización.03 medical and health sciences0302 clinical medicineIonization.medicineStratum corneumpropranololDermatopharmacokineticsTransdermalmedia_commonchemical enhancersChromatographytransdermal administrationIontophoresisChemistryLaurocapramTransdermal administrationIontophoresisDrugs - Administration.Skin absorption.iontophoresisPermeation021001 nanoscience & nanotechnologyPropranololPropanol - Therapeutic use.In vitromedicine.anatomical_structurePropanol - Pharmacokinetics.Propanol - Farmacocinética.Absorción cutánea.0210 nano-technologymedicine.drug

description

[EN] The aims of this study were to assess, in vitro, the possibility of administering propranolol transdermally and to evaluate the usefulness of the dermatopharmacokinetic (DPK) method in assessing the transport of drugs through stratum corneum, using propranolol as a model compound. Four chemical enhancers (decenoic and oleic acid, laurocapram, and R-(+)-limonene) and iontophoresis at two current densities, 0.25 and 0.5 mA/cm(2) were tested. R-(+)-limonene, and iontophoresis at 0.5 mA/cm(2) were proven to be the most efficient in increasing propranolol transdermal flux, both doubled the original propranolol transdermal flux. Iontophoresis was demonstrated to be superior than the chemical enhancer because it allowed faster delivery of the drug. The DPK method was sufficiently sensitive to detect subtle vehicle-induced effects on the skin permeation of propranolol. The shorter duration of these experiments and their ability to provide mechanistic information about partition between vehicle and skin and diffusivity through skin place them as practical and potentially insightful approach to quantify and, ultimately, optimize topical bioavailability.

https://doi.org/10.3390/pharmaceutics10040265