Evaluation of topical econazole nitrate formulations with potential for treating Raynaud’s phenomenon

Bahl, Dherya; Daftardar, Saloni; Bachu, Rinda Devi; Boddu, Sai H. S.; Altorok, Nezam; Kahaleh, Bashar

doi:10.1080/10837450.2019.1578371

Cited by 9 publications

(8 citation statements)

References 33 publications

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“…Wasan et al [62 ▪ ] reported a preclinical study investigating the formulation of a novel nifedipine cream stable to ultraviolet light. Topical PDE5 inhibitors are also being researched [63,64] and topical econazole nitrate, an antagonist of Transient Receptor Potential Melastatin 8 has been studied in vitro [61,66 ▪ ]. These are all important steps forward towards long-awaited clinical trials of topical treatments.…”

Section: Treatmentmentioning

confidence: 99%

“…Although the use of topical glyceryl trinitrate for Raynaud's phenomenon was suggested as far back as 1951 [56], progress with topical therapies has been very slow. It is hoped that recent systematic reviews on topical nitrates [57,58] herald a wave of new interest, with several publications on topical therapies over the last 3 years [59–61,62 ▪ ,63–65,66 ▪ ]. Wasan et al [62 ▪ ] reported a preclinical study investigating the formulation of a novel nifedipine cream stable to ultraviolet light.…”

Section: Treatmentmentioning

confidence: 99%

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Raynaud's phenomenon and digital ulcers: advances in evaluation and management

Herrick¹

2021

Current Opinion in Rheumatology

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Purpose of reviewThe aim of this review is to give an update on advances in evaluation and management of systemic sclerosis (SSc)-related Raynaud's phenomenon and digital ulceration, focusing on reports from the last 18 months. The increasing recognition of the huge impact of Raynaud's phenomenon and of digital ulceration on the everyday lives of patients with SSc has sparked enthusiasm internationally to develop better outcome measures and better treatments, and so a review is timely.Recent findingsThere have been recent advances in the development of patient reported outcome instruments [e.g. the Hand Disability in Systemic Sclerosis-Digital Ulcers (HDISS-DU) instrument] and also in noninvasive imaging techniques, including thermography and laser Doppler methods. Improved outcome measures will facilitate future clinical trials, both early phase proof-of-concept and later phase trials. New insights have been gained into mechanisms of action and methods of administration of ‘conventional’ therapies, for example phosphodiesterase inhibitors and intravenous prostanoids. New treatment approaches are being investigated, including topical and procedural therapies.SummaryClinicians can look forward to seeing these advances translating into clinical benefit over the next 5 years. To help ensure this, they should strive whenever possible to recruit patients with SSc-related digital vasculopathy into observational studies and clinical trials.

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Section: Treatmentmentioning

confidence: 99%

Section: Treatmentmentioning

confidence: 99%

Raynaud's phenomenon and digital ulcers: advances in evaluation and management

Herrick¹

2021

Current Opinion in Rheumatology

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“…A formulation is more stable when all particles are positively or negatively charged, instead of some particles having negative potential and some particles having positive potential, because the opposite charges attract each other and are considered less stable. In addition, there are repulsive forces between the same charges, which keeps the formulation stable for a long time ( Tummala et al, 2015 ; Bahl, 2017 ).…”

Section: Resultsmentioning

confidence: 99%

Enhanced Antifungal and Wound Healing Efficacy of Statistically Optimized, Physicochemically Evaluated Econazole-Triamcinolone Loaded Silica Nanoparticles

et al. 2022

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Co-encapsulated econazole nitrate-triamcinolone acetonide loaded biocompatible, physically stable, and non-irritating mesoporous silica nanoparticles (EN-TA–loaded MSNs) were prepared and optimized by using a central composite rotatable design (CCRD) for providing better therapeutic efficacy against commonly prevailed resistant fungal infections. These drugs loaded MSNs can significantly overcome the deficiencies and problems like short duration of action, requirement of frequent administration, erythema, and burning sensation and irritation associated with conventional drug delivery systems. The stability of optimized drugs loaded MSNs prepared with 100 gm of oil at pH 5.6 with a stirring time of 2 h was confirmed from a zeta potential value of −25 mV. The remarkable compatibility of formulation ingredients was depicted by X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR) spectra while scanning electron microscopy (SEM) and size analysis represented a very fine size distribution of nanoparticles ranging from 450–600 nm. The CCRD clearly predicted that the optimized parameters of drugs loaded MSNs have better values of percentage yield (85%), EN release (68%), and TA release (70%). Compared to pure drugs, the decreased cytotoxicity of EN-TA–loaded MSNs was quite evident because they showed a cell survival rate of 90%, while in the case of pure drugs, the survival rate was 85%. During in vivo antifungal testing against Candida albicans performed on three different groups, each consisting of six rabbits, the EN-TA–loaded MSNs were relatively superior in eradicating the fungal infection as a single animal exhibited a positive culture test. Rapid recovery of fungal infection and a better therapeutic effect of EN-TA–loaded MSN were quite evident in wound healing and histopathology studies. Likewise, on the 14th day, a larger inhibitory zone was measured for optimized nanoparticles (15.90 mm) compared to the suspension of pure drugs (13.90 mm). In skin irritation studies, MSNs did not show a grade of erythema compared to pure drugs, which showed a four-fold grade of erythema. As a result, MSNs loaded with combination therapy seem to have the potential of improving patient compliance and tolerability by providing enhanced synergistic antifungal effectiveness at a reduced dose with accelerated wound healing and reduced toxicity of therapeutics.

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“…Permeability (P app ) = Flux/C d Flux (J) was calculated by dividing the slope obtained by plotting the cumulative amount of drug permeated (M) through the skin vs. time (t) with the cross-sectional area of the membrane (A) exposed to the drug. C d was the initial drug concentration in the donor chamber [49].…”

Section: Experimental Parameters Affecting the Permeation Studymentioning

confidence: 99%

Alternatives to Biological Skin in Permeation Studies: Current Trends and Possibilities

et al. 2020

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The transdermal route of drugs has received increased attention in recent years due to numerous advantages over the oral and injectable routes, such as avoidance of the hepatic metabolism, protection of drugs from the gastrointestinal tract, sustained drug delivery, and good patient compliance. The assessment of ex vivo permeation during the pharmaceutical development process helps in understanding the product quality and performance of a transdermal delivery system. Generally, excised human skin relevant to the application site or animal skin is recommended for ex vivo permeation studies. However, the limited availability of the human skin and ethical issues surrounding the use of animal skin rendered these models less attractive in the permeation study. In the last three decades, enormous efforts have been put into developing artificial membranes and 3D cultured human skin models as surrogates to the human skin. This manuscript provides an insight on the European Medicines Agency (EMA) guidelines for permeation studies and the parameters affected when using Franz diffusion cells in the permeation study. The need and possibilities for skin alternatives, such as artificially cultured human skin models, parallel artificial membrane permeability assays (PAMPA), and artificial membranes for penetration and permeation studies, are comprehensively discussed.

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Evaluation of topical econazole nitrate formulations with potential for treating Raynaud’s phenomenon

Cited by 9 publications

References 33 publications

Raynaud's phenomenon and digital ulcers: advances in evaluation and management

Raynaud's phenomenon and digital ulcers: advances in evaluation and management

Enhanced Antifungal and Wound Healing Efficacy of Statistically Optimized, Physicochemically Evaluated Econazole-Triamcinolone Loaded Silica Nanoparticles

Alternatives to Biological Skin in Permeation Studies: Current Trends and Possibilities

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