Antidermatophytic Activity and Skin Retention of Clotrimazole Microemulsion and Microemulsion-Based Gel in Comparison to Conventional Cream

Kaewbanjong, Jarika; Amnuaikit, Thanaporn; Souto, Eliana B.; Boonme, Prapaporn

doi:10.1159/000491756

Cited by 17 publications

(6 citation statements)

References 20 publications

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“…Sampling intervals were 1, 2, 3, 4, 5, 6, 7, 8, 12, 16, 20, and 24 h. Results showed that clotrimazole was not permeated through the skin up to 24 h following the permeation studies from all the tested formulations. Similar results were observed in reports published in literature with clotrimazole microemulsions [43], clotrimazole loaded three-dimensionally-structured hybrid vesicles [17], and roxithromycin ufosomes [18]. As most of the fungal infections are localized on the surface of the skin, systemic bioavailability of clotrimazole is not required.…”

Section: Resultssupporting

confidence: 88%

Clotrimazole Loaded Ufosomes for Topical Delivery: Formulation Development and In-Vitro Studies

et al. 2019

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Global incidence of superficial fungal infections caused by dermatophytes is high and affects around 40 million people. It is the fourth most common cause of infection. Clotrimazole, a broad spectrum imidazole antifungal agent is widely used to treat fungal infections. Conventional topical formulations of clotrimazole are intended to treat infections by effective penetration of drugs into the stratum corneum. However, drawbacks such as poor dermal bioavailability, poor penetration, and variable drug levels limit the efficiency. The present study aims to load clotrimazole into ufosomes and evaluate its topical bioavailability. Clotrimazole loaded ufosomes were prepared using cholesterol and sodium oleate by thin film hydration technique and evaluated for size, polydispersity index, and entrapment efficiency to obtain optimized formulation. Optimized formulation was characterized using scanning electron microscopy (SEM), X-ray diffraction (XRD), and differential scanning calorimetry (DSC). Skin diffusion studies and tape-stripping were performed using human skin to determine the amount of clotrimazole accumulated in different layers of the skin. Results showed that the optimized formulation had vesicle size <250 nm with ~84% entrapment efficiency. XRD and DSC confirmed the entrapment of clotrimazole into ufosomes. No permeation was observed through the skin up to 24 h following the permeation studies. Tape-stripping revealed that ufosomes led to accumulation of more clotrimazole in the skin compared to marketed formulation (Perrigo). Overall, results revealed the capability of ufosomes in improving the skin bioavailability of clotrimazole.

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Section: Resultssupporting

confidence: 88%

Clotrimazole Loaded Ufosomes for Topical Delivery: Formulation Development and In-Vitro Studies

et al. 2019

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“…For example, studies have verified that the colloidal drug delivery system, including microemulsions, nanoemulsions, and micelles; vesicle drug delivery system, including liposomes, alcohol liposomes, liposome-like structures, and transporters; and nanoparticle drug delivery system, including solid lipid nanoparticles and nanostructured liposomes, promote skin penetration and retention of drugs. [10][11][12][13] Polymer micelles are colloidal solutions with core-shell structures that are formed by the self-assembly of amphiphilic copolymers above the critical micelle concentration. They are often used as carriers of water-insoluble drugs and have good biocompatibility.…”

Section: Introductionmentioning

confidence: 99%

<p>Berberine-Loaded Thiolated Pluronic F127 Polymeric Micelles for Improving Skin Permeation and Retention</p>

Niu¹,

Yuan²,

Chen³

et al. 2020

IJN

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“…The characteristic peak of the aromatic group (C–H stretching) at 3167 cm –1 is indicated, while the peak at 1593 cm –1 showed the aromatic group (CC stretching). The peak at 1570 cm –1 corresponds to CN stretching, while the peak at 1040 cm –1 showed C–H stretching as shown in Figure S10 (Supporting Information) . The FTIR spectra of CTZ-free μE, CTZ-μE, CTZ-free μEG, and CTZ-μEG for both formulation A and formulation B are given in Figure .…”

Section: Resultsmentioning

confidence: 96%

“…The peak at 1570 cm −1 corresponds to CN stretching, while the peak at 1040 cm −1 showed C−H stretching as shown in Figure S10 (Supporting Information). 61 The FTIR spectra of CTZ-free μE, CTZ-μE, CTZ-free μEG, and CTZ-μEG for both formulation A and formulation B are given in Figure 4.…”

Section: ■ Results and Discussionmentioning

confidence: 99%

Microemulsified Gel Formulations for Topical Delivery of Clotrimazole: Structural and In Vitro Evaluation

et al. 2021

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Microemulsified gels (μEGs) with fascinating functions have become indispensable as topical drug delivery systems due to their structural flexibility, high stability, and facile manufacturing process. Topical administration is an attractive alternative to traditional methods because of advantages such as noninvasive administration, bypassing first-pass metabolism, and improving patient compliance. In this article, we report on the new formulations of microemulsion-based gels suitable for topical pharmaceutical applications using biocompatible and ecological ingredients. For this, two biocompatible μE formulations comprising clove oil/Brij-35/water/ethanol (formulation A) and clove oil/Brij-35/water/1-propanol (formulation B) were developed to encapsulate and improve the load of an antimycotic drug, Clotrimazole (CTZ), and further gelatinized to control the release of CTZ through skin barriers. By delimiting the pseudo-ternary phase diagram, optimum μE formulations with clove oil (∼15%) and Brij-35 (∼30%) were developed, keeping constant surfactant/co-surfactant ratio (1:1), to upheld 2.0 wt % CTZ. The as-developed formulations were further converted into smart gels by adding 2.0 wt % carboxymethyl cellulose (CMC) as a cross-linker to adhere to the controlled release of CTZ through complex skin barriers. Electron micrographs show a fine, monodispersed collection of CTZ-μE nanodroplets (∼60 nm), which did not coalesce even after gelation, forming spherical CTZ-μEG (∼90 nm). However, the maturity of CTZ nanodroplets observed by dynamic light scattering suggests the affinity of CTZ for the nonpolar microenvironment, which was further supported by the peak-to-peak correlation of Fourier transform infrared (FTIR) analysis and fluorescence measurement. In addition, HPLC analysis showed that the in vitro permeation release of CTZ-μEG from rabbit skin in the ethanolic phosphate buffer (pH = 7.4) was significantly increased by >98% within 6.0 h. This indicates the sustained release of CTZ in μEBG and the improvement in transdermal therapeutic efficacy of CTZ over its traditional topical formulations.

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Antidermatophytic Activity and Skin Retention of Clotrimazole Microemulsion and Microemulsion-Based Gel in Comparison to Conventional Cream

Cited by 17 publications

References 20 publications

Clotrimazole Loaded Ufosomes for Topical Delivery: Formulation Development and In-Vitro Studies

Clotrimazole Loaded Ufosomes for Topical Delivery: Formulation Development and In-Vitro Studies

<p>Berberine-Loaded Thiolated Pluronic F127 Polymeric Micelles for Improving Skin Permeation and Retention</p>

Microemulsified Gel Formulations for Topical Delivery of Clotrimazole: Structural and In Vitro Evaluation

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