Poly(pseudo)rotaxanes formed by mixed micelles and α-cyclodextrin enhance terbinafine nail permeation to deeper layers

Krawczyk-Santos, Anna Paula; Marreto, Ricardo Neves; Concheiro, Ángel; Taveira, Stephânia Fleury

doi:10.1016/j.ijpx.2022.100118

Cited by 4 publications

(6 citation statements)

References 60 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…35 Consequently, it is reasonable to assume that the vehicle included in this phase III clinical trial has played a role, more as an active pharmaceutical product than as a placebo-controlled group, and it may be explained by the active effect of the technology behind the vehicle. Apart from that, the high level of hydration and solubility showed by the inclusion of cyclodextrins in nail lacquers formulations, [20][21][22][23]28 which promotes quicker healthy nail growth, may have contributed to a more favourable clinical evaluation by the independent investigator during the study and especially in distal onychomycosis.…”

Section: Discussionmentioning

confidence: 99%

“…The Ciclo-Tech® technology is based on the interaction of a solubilising and moisturising agent -hydroxypropyl-𝛽-cyclodextrin-, with a permeability-enhancing substance -sodium lauryl sulfate-, and with a film-forming agent -poloxamer 407-. β-cyclodextrins encapsulate the active ingredient in a hydrophilic medium, 19,20 increasing its diffusion through the keratin of the nail and, at the same time, promoting nail hydration, [21][22][23] and therefore healthy nail replacement. [Correction added on 13 April 2023, after first online publication: "growth and healing' was changed to 'healthy nail replacement' in the preceding sentence.]…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Efficacy and safety of a new medicated nail hydrolacquer in the treatment of adults with toenail onychomycosis: A randomised clinical trial

Zalacain-Vicuña

Nieto

Picas

et al. 2022

Mycoses

View full text Add to dashboard Cite

Background: A new water-soluble formulation with ciclopirox has shown a higher penetration than other ciclopirox nail lacquers currently marketed, thus providing a higher concentration of ciclopirox into the nail.Objective: To evaluate the efficacy and safety of a new ciclopirox nail hydrolacquer compared with its vehicle and an active comparator (hydroxypropyl chitosan-based 80 mg/g ciclopirox nail lacquer) for the treatment of toenail fungal infection.Methods: Phase III, multicenter, randomised, double-blind, clinical trial in patients with distal mild to moderate toenail onychomycosis due to dermatophyte fungi.Patients were randomised to apply topically a ciclopirox nail hydrolacquer, its vehicle or a reference product once daily for 48 weeks with a follow-up period of 4 weeks up to week 52.Results: A total of 381 patients were included. No statistically significant differences were observed between patient groups in the proportion of subjects achieving a complete cure. At week 52, a higher percentage of patients in the ciclopirox nail hydrolacquer group achieved a mycological cure (negative for culture and DTS/KOH test, with results: 32.0% ciclopirox nail hydrolacquer , 23.2% vehicle and 27% reference product, respectively), and similar results were found for improvement (mycological cure and reduction of diseased nail ≥20%, with results: 27.2% ciclopirox nail hydrolacquer, 21.6% vehicle and 20.6% reference product, respectively). Regarding mycological results, only ciclopirox nail hydrolacquer demonstrated significant statistical superiority versus vehicle negativizing dermatophyte culture (p = .039) with no recurrences, relapses or re-infections in a four-week follow-up patients with complete cure. The safety profile was comparable to the vehicle and reference product and consistent with the previously reported.

show abstract

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Efficacy and safety of a new medicated nail hydrolacquer in the treatment of adults with toenail onychomycosis: A randomised clinical trial

Zalacain-Vicuña

Nieto

Picas

et al. 2022

Mycoses

View full text Add to dashboard Cite

show abstract

“…The safety and pharmacokinetics will be also evaluated in the timeframe of 16–52 weeks. A terbinafine-based formulation using poly(pseudo)rotaxanes (PPR) technology to enhance the drug delivery is currently under development [ 41 ]. Terbinafine-based PPRs are water-soluble preparations consisting of micelles, α-cyclodextrin, and Terbinafine.…”

Section: Topical Antifungal Nail Therapies Under Development and Inve...mentioning

confidence: 99%

Novel and Investigational Treatments for Onychomycosis

Gregoriou

Kyriazopoulou

Tsiogka

et al. 2022

JoF

View full text Add to dashboard Cite

Onychomycosis is a common nail disease caused by fungi. The primary pathogens are dermatophytes; however, yeasts, non-dermatophyte moulds, and mixed fungal populations may also contribute to the development of a recalcitrant condition, usually accompanied by difficulties in everyday life and severe emotional stress. Treatment failure and relapse of the infection are the most frequent problems, though new issues have become the new challenges in the therapeutic approach to onychomycosis. Resistance to antifungals, an increasing number of comorbidities, and polydrug use among the ageing population are imperatives that impose a shift to safer drugs. Topical antifungals are considered less toxic and minimally interact with other drugs. The development of new topical drugs for onychomycosis is driven by the unmet need for effective agents with prolonged post-treatment disease-free time and a lack of systemic impact on the patients’ health. Efinaconazole, Tavaborole, and Luliconazole have been added to physicians’ weaponry during the last decade, though launched on the market of a limited number of countries. The pipeline is either developing new products (e.g., ME-1111 and NP213) with an appealing combination of pharmacokinetic, efficacy, and safety properties or reformulating old, well-known drugs (Terbinafine and Amphotericin B) by using new excipients as penetration enhancers.

show abstract

“…This inhibits fungal sterol biosynthesis by decreasing ergosterol levels. On average, this drug results in a 70-79% recovery rate, with complete recovery ranging from 38-59% [9]. After oral administration, terbinafine HCl undergoes the first-pass effect and is extensively bound to the plasma proteins; therefore, a high dose is recommended [10].…”

Section: Introductionmentioning

confidence: 99%

Thermo-Responsive Sol-Gel-Based Nano-Carriers Containing Terbinafine HCl: Formulation, In Vitro and Ex Vivo Characterization, and Antifungal Activity

Bajwa,

Tabassam,

Hameed

et al. 2023

Gels

View full text Add to dashboard Cite

The current research aims to create a sol-gel-based nanocarrier containing terbinafine formulated for transdermal delivery of the drug into the skin. Sol-gel-based nanocarriers were prepared via the cold method using poloxamer-188, poloxamer-407, and distilled water. The prepared formulation was examined for pH, gelation temperature, Fourier transform infrared spectrophotometer (FTIR) analysis, thermal stability analysis, X-ray diffraction (XRD), scanning electron microscopy (SEM), particle size analysis, zeta potential, and anti-microbial activity. The in-vitro drug release study of F1 was found to be 94%, which showed greater drug release as compared to F2 and F3. The pH of the formulation was found to be within the range applicable to the skin. The gelation temperature was detected at 28 °C. The SEM images of formulations have spotted various particles well-segregated from each other. Analysis of formulations showed a mean globule size diameter of 428 nm, zeta potential values of 0.04 mV, refractive index (1.329), and viscosity (5.94 cP). FTIR analysis confirmed various functional groups’ presence in the prepared formulation. Thermal analysis has confirmed the stability of the drug within the prepared formulation. The growth of inhibition was found to be 79.2% in 60 min, which revealed that the prepared formulation has shown good permeation from the membrane. Hence, the sol-gel-based nanocarrier formulation of terbinafine was successfully developed and evaluated.

show abstract

Poly(pseudo)rotaxanes formed by mixed micelles and α-cyclodextrin enhance terbinafine nail permeation to deeper layers

Cited by 4 publications

References 60 publications

Efficacy and safety of a new medicated nail hydrolacquer in the treatment of adults with toenail onychomycosis: A randomised clinical trial

Efficacy and safety of a new medicated nail hydrolacquer in the treatment of adults with toenail onychomycosis: A randomised clinical trial

Novel and Investigational Treatments for Onychomycosis

Thermo-Responsive Sol-Gel-Based Nano-Carriers Containing Terbinafine HCl: Formulation, In Vitro and Ex Vivo Characterization, and Antifungal Activity

Contact Info

Product

Resources

About