Poly(pseudo)rotaxanes formed by mixed micelles and α-cyclodextrin enhance terbinafine nail permeation to deeper layers.
Int J Pharm X
; 4: 100118, 2022 Dec.
Article
de En
| MEDLINE
| ID: mdl-35602759
ABSTRACT
This work aimed to develop water-based formulations for onychomycosis topical treatment using micelles of small pegylated surfactants associated with α-cyclodextrin (αCD) to deliver terbinafine to the nail. Kolliphor® RH40 (RH40) and Gelucire® 48/16 (GEL) single and mixed micelles (RH40GEL 11) were prepared. αCD was added to the surfactants dispersions to form poly(pseudo)rotaxanes (PPR). Formulations were characterized in terms of drug solubilization (3 to 34-fold increase), particle size (9-11 nm) and Z-potential (+0.3 - +1.96 mV), blood compatibility (non-hemolytic), rheological behavior (solid-like viscoelastic properties after 5-10% αCD addition), drug release and interaction with the nail plate. GEL micelles and surfactant-10% αCD PPRs notably hydrated the nail plate. The high viscosity of PPR led to a slower drug release, except for RH40GEL +10% αCD that surprisingly released terbinafine faster. The RH40GEL +10% αCD formulation delivered twice more amount of terbinafine to deeper regions of nail plate compared to other formulations. The results evidenced the potential of PPR formed by small pegylated surfactants as a water-based formulation for nail drug delivery.
CDs, cyclodextrins; GEL, Gelucire® 48/16; Mixed micelles; Nail permeation; Onychomycosis; PEG, polyethylene glycol; PPR, poly(pseudo)rotaxane; PdI, polydispersity index; Poly(pseudo)rotaxanes; RH40, Kolliphor® RH40; RH40:GEL, mixture of RH40 and GEL 1:1; Supramolecular gels; TB, terbinafine hydrochloride; Terbinafine
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Langue:
En
Journal:
Int J Pharm X
Année:
2022
Type de document:
Article
Pays d'affiliation:
Brésil