Influence of Lamotrigine concentration on physicochemical properties and transdermal release using PBAT/PLA electrospun fibers

• Published in: Colloids and surfaces. A, Physicochemical and engineering aspects Physicochemical and engineering aspects, 2024-04, Vol.686, p.133216, Article 133216
• Main Authors: Cândido, Gabriela Braga Gomes, Fraga, Gabriel Nardi, Rossin, Ariane Regina de Souza, Lourenço, Rebeca Lino, Gibin, Mariana Sversut, Zanuto, Vitor Santaella, Caetano, Josiane, Dragunski, Douglas Cardoso
• Format: Article
• Language: English
• Subjects: biopharmaceuticals; calorimetry; chloroform; class; dermis; dimethylformamide; drug interactions; Ecovio; electron microscopy; Electrospinning; epilepsy; infrared spectroscopy; Lamotrigine; muscles; nanofibers; patients; permeability; polymers; Release kinetic model; solubility; swine; thermogravimetry; transdermal application; Transdermal drug delivery; Weibull statistics; X-ray diffraction
• ISSN: 0927-7757; 1873-4359
• DOI: 10.1016/j.colsurfa.2024.133216

Epilepsy is a disease caused by a change in respiratory signs, which can cause fainting and muscle contractions. Thus, one of the drugs indicated for the treatment of epileptic seizures is Lamotrigine, classified class II in the biopharmaceutical classification system; it has low solubility and high permeability in interstitial fluids; in addition, the pharmaceutical forms currently available have large drug interaction screens. New forms of drug delivery have been investigated, in which transdermal delivery systems have appeared with great prominence. Thus, the present work aims to produce polymeric nanofibers using the electrospinning technique, incorporating the drug Lamotrigine in its structure. For this, the experimental conditions for the production of fibers are evaluated, using the polymeric blend PBAT/PLA to obtain an alternative administration technology so that the patient has fewer interaction effects and also promotes an increase in the solubility of the active. The membranes produced (15% w/v of PBAT/PLA in a solution of 85% chloroform: 15% dimethylformamide and with 5%, 10%, 20%, and 30% w/w of Lamotrigine) were identified by scanning electron microscopy (SEM), infrared spectroscopy (FTIR), thermogravimetry (TGA), differential scanning calorimetry (DSC), X-ray diffraction (DRX), transmission analysis, conductivity, mechanical analysis, release study, and permeation study. The release profiles found were adjusted to different kinetic release models. The Weibull model showed better results for R2 and the Akaike confirmation, demonstrating that the PBAT/PLA/L5 showed better results for release. Ex-vivo permeation in porcine skin demonstrated that the lower concentration of Lamotrigine has better permeation in the dermis and epidermis. [Display omitted] •Lamotrigine electrospinning is performed at different concentrations.•High concentrations of Lamotrigine modify the physical-chemical properties of electrospun matrices.•The drug was released within 180 min.•The permeation study on pig ear skin demonstrated that at lower concentrations, permeability is improved.•The manufactured material can be accredited for the transdermal release of Lamotrigine.