Antifungal efficacy of liquid poloxamer 407-based emulsions loaded with sertaconazole nitrate

Kracht, Tobias; Müller‐Goymann, Christel C.

doi:10.1016/j.ijpharm.2020.119400

Cited by 13 publications

(7 citation statements)

References 25 publications

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“…Therefore, in the present study, a precursor solution of the cubic phase was prepared by choosing 80:20 as the fixed ratio (% w / w ) between GMO and water; then, a transition to the cubic phase was performed by adding an excess of aqueous medium. The same operative conditions were employed during the preparation of precursor solution loaded with sertaconazole nitrate ( Figure 1 b), a highly lipophilic drug (logP = 6.23) characterized by extremely poor aqueous solubility [ 18 , 19 ].…”

Section: Resultsmentioning

confidence: 99%

In Situ Swelling Formulation of Glycerol-Monooleate-Derived Lyotropic Liquid Crystals Proposed for Local Vaginal Application

et al. 2022

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Hydrogels have been extensively investigated to identify innovative formulations that can fulfill all the necessary purposes to improve local vaginal therapy through the mucosa. Herein, we propose in situ-forming lyotropic liquid crystals (LLCs) derived from a cheap and GRAS (generally recognized as safe) ingredient as an intravaginal delivery system. The system consists of a precursor solution loaded with sertaconazole nitrate as a model drug, which is able to easily swell in a stable three-dimensional structure by absorbing simulated vaginal fluid. Under polarized light microscopy the precursor solution and the formed phase of LLCs showed the typical textures belonging to anisotropic and an isotropic mesophases, respectively. A deep rheological investigation by Kinexus® Pro proved the stability and strength of the cubic phase, as well as its potential in mucoadhesion. In vitro degradation studies showed a slow matrix erosion, consistent with data obtained from lipophilic drug release studies in simulated vaginal fluid. Therefore, the suggested cubic phase based on lyotropic liquid crystals could represent a valid proposal as a vaginal drug delivery system due to its characteristics of resistance, adhesion and the possibility of providing a slow and controlled release of drugs directly at the administration site.

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Section: Resultsmentioning

confidence: 99%

In Situ Swelling Formulation of Glycerol-Monooleate-Derived Lyotropic Liquid Crystals Proposed for Local Vaginal Application

et al. 2022

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“…In situ gels or self‐assembling gels, on the contrary, are prepared in liquid form. They transition into a semi‐solid state after their application onto the nail plate due to changes in concentration (by evaporation of water or solvent), pH or temperature 53,54 …”

Section: Strategies To Enhance Nail Plate Penetrationmentioning

confidence: 99%

Strategies for the enhancement of nail plate permeation of drugs to treat onychomycosis

Gupta

Ravi

Choi

et al. 2022

Acad Dermatol Venereol

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Onychomycosis is caused by dermatophytes, non‐dermatophytes and yeasts. It has a global prevalence of 5.5%, requires long treatment periods, and has high relapse rates following therapy. Oral antifungals are generally the most common treatment. While effective, they have limitations such as drug–drug interactions, hepatotoxicity and adverse side effects; thus, they cannot be used in several populations. Topical antifungals do not have the safety limitations but are typically not as effective. The primary challenge of topical treatment is the permeation of drug molecules across the nail plate barrier, which is a highly cross‐linked keratin network. The use of drugs and formulations with favourable characteristics such as small size, absence of lipophilicity, hydrophilic nature, hydrating properties and appropriate pH can greatly improve permeation. Here, we review physical, nanoparticle‐based, formulation‐based, mechanical and chemical drug delivery strategies to improve the permeation of drugs across the nail plate.

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“…Although azoles have high antimycotic activity, their application is limited due to the insufficient water solubility [ 146 , 147 ]. Emulsion-based antifungal azoles formulations displayed high drug loading capacity, as well as increased drug bioavailability after both oral and topical administration as compared to commercial formulations and neat substances [ 148 , 149 , 150 , 151 , 152 , 153 , 154 , 155 , 156 , 157 ].…”

Section: Emulsion-based Vaginal Dosage Forms With Drugs From Different Therapeutic Groups—biological Evaluation and Examples Of In Vivo Amentioning

confidence: 99%

Emulsion-Based Multicompartment Vaginal Drug Carriers: From Nanoemulsions to Nanoemulgels

Smoleński

Karolewicz

Gołkowska

et al. 2021

IJMS

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In order to overcome the limitations associated with vaginal administration of drugs, e.g., the short contact time of the drug form with the mucosa or continuous carrier wash-out, the development of new carriers for gynecological use is necessary. Furthermore, high individual anatomical and physiological variability resulting in unsatisfactory therapeutic efficacy of lipophilic active substances requires application of multicompartment drug delivery systems. This manuscript provides an up-to-date comprehensive review of the literature on emulsion-based vaginal dosage forms (EVDF) including macroemulsions, microemulsions, nanoemulsions, multiple emulsions and self-emulsifying drug delivery systems. The first part of the paper discusses (i) the influence of anatomical-physiological conditions on therapeutic efficacy of drug forms after local and systemic administration, (ii) characterization of EVDF components and the manufacturing techniques of these dosage forms and (iii) methods used to evaluate the physicochemical and pharmaceutical properties of emulsion-based vaginal dosage forms. The second part of the paper presents (iv) the results of biological and in vivo studies as well as (v) clinical evaluation of EVDF safety and therapeutic efficacy across different indications.

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Antifungal efficacy of liquid poloxamer 407-based emulsions loaded with sertaconazole nitrate

Cited by 13 publications

References 25 publications

In Situ Swelling Formulation of Glycerol-Monooleate-Derived Lyotropic Liquid Crystals Proposed for Local Vaginal Application

In Situ Swelling Formulation of Glycerol-Monooleate-Derived Lyotropic Liquid Crystals Proposed for Local Vaginal Application

Strategies for the enhancement of nail plate permeation of drugs to treat onychomycosis

Emulsion-Based Multicompartment Vaginal Drug Carriers: From Nanoemulsions to Nanoemulgels

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