Enhanced Econazole Penetration into Human Nail by 2-n-Nonyl-1,3-dioxolane

Transungual permeation: current insights

“…Hui et al [53] from Maibach's group used SEPA (2-n-Nonyl-1,3-dioxolane) for improving the penetration of econazole from a nail lacquer formulation termed as Econail™. It was found that the addition of SEPA® could increase permeation of econazole 6 times higher than the control.…”

“…The driller precisely drills into the desired layers of the nail and removes the nail powder. The nail powder from the dorsal, ventral, and intermediate layers of the nail can be easily obtained using this instrument and can be analyzed for drug content [2,50,53].…”

An Ex Vivo Toe Model Used to Assess Applicators for the Iontophoretic Ungual Delivery of Terbinafine

“…However, the existing topical formulations are unable to deliver the required therapeutic amount of drug to the deeper infected site because of the hard and impermeable keratinized nail plate (8). There has been intensive effort to increase drug penetration across the nail through the use of chemical enhancers, but that has resulted in limited success (9)(10)(11)(12)(13)(14). Normal human nail plates or nail clippings are most commonly used in the trans-ungual permeation studies.…”

Synthesis of isotopically labelled [3‐14C]‐ and [3,3‐2H2]‐5‐fluoro‐1,3‐dihydro‐1‐hydroxy‐2,1‐benzoxaborole (AN2690), a new antifungal agent for the potential treatment of onychomycosis

“…10 First, in order to study its ability to penetrate human cadaver finger nail plates in vitro, 11 we required a radiolabelled version so we could accurately measure amounts within the nail plate and amounts that had penetrated through and into a collector using previously published methods. 12,13 For this purpose, we designed [3-14 C]-5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, which incorporates the radioisotope into the 3-position of the oxaborole ring. Second, we required a bis-deuterium isotope to use as a reference sample for the mass spectrometry analysis of biological samples during pre-clinical development.…”