Corneal targeted Amorolfine HCl-mixed micelles for the management of ocular candidiasis: Preparation, in vitro characterization, ex vivo and in vivo assessments

Abd-Elmonem, Eman M.; Makky, Amna M.A.; Antar, Assem; Abd-Elsalam, Wessam H.; Khalil, Islam A.

doi:10.1016/j.jddst.2023.104614

Cited by 3 publications

(5 citation statements)

References 72 publications

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“…Over a span of 14 days, the morphological conditions of the eyes of rabbits were observed. Symptoms such as chemosis, palpebral fissures, and conjunctival congestions indicated whether a rabbit has FK. , After the morphological observation was completed, the rabbits were euthanized with CO 2 asphyxiation and the eyeballs were enucleated and then stored at −20 °C until ready for further use. Furthermore, a portion of the corneal tissue from the rabbit’s eyeball was homogenized, diluted, and then spread over a PDA medium.…”

Section: Methodsmentioning

confidence: 99%

Solid Dispersion Incorporated into Dissolving Microneedles for Improved Antifungal Activity of Amphotericin B: In Vivo Study in a Fungal Keratitis Model

Mahfud,

Syahirah,

Akram

et al. 2023

Mol. Pharmaceutics

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Section: Methodsmentioning

confidence: 99%

Solid Dispersion Incorporated into Dissolving Microneedles for Improved Antifungal Activity of Amphotericin B: In Vivo Study in a Fungal Keratitis Model

Mahfud,

Syahirah,

Akram

et al. 2023

Mol. Pharmaceutics

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“…albicans suspension which is equivalent to 10 7 cfu/mL were injected intrastromally using a needle. After that, the eye of the rabbits was observed visually every day for signs of FK development, and the rabbits were divided into several divided into different treatment groups …”

Section: Methodsmentioning

confidence: 99%

“…After that, the samples were homogenized, diluted, and spread on PDA media and then incubated at 37 °C. Finally, after 48 h of incubation, cfus were counted according to n u m b e r .25em o f .25em c o l o n i e s .25em ( normalc normalf normalu / normalm normalL ) = n u m b e r .25em o f .25em c o l o n i e s × d i l u t i o n .25em f a c t o r v o l u m e .25em o f .25em c u l t u r e ‐ p l a t e d …”

Section: Methodsmentioning

confidence: 99%

“…After that, the samples were homogenized, diluted, and spread on PDA media and then incubated at 37 °C. Finally, after 48 h of incubation, cfus were counted according to …”

Section: Methodsmentioning

confidence: 99%

“…After that, the eye of the rabbits was observed visually every day for signs of FK development, and the rabbits were divided into several divided into different treatment groups. 48 The distribution of treatment groups in rabbits is as follows; group I (the best formula of DMN-FNL-IC), group II (eye drops), group III (eye ointment), and group IV without drug treatment (control). Each of these treatments was carried out once a day for 14 days after the induction of fungal keratitis.…”

Section: Drug Calculation Content In the Tip And Determination Drug C...mentioning

confidence: 99%

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Incorporation of Inclusion Complexes in the Dissolvable Microneedle Ocular Patch System for the Efficiency of Fluconazole in the Therapy of Fungal Keratitis

Mahfufah,

Sya’ban Mahfud,

Saputra

et al. 2024

ACS Appl. Mater. Interfaces

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Fluconazole (FNL) is one of the first-line treatments for fungal keratitis as it is an effective broad-spectrum antimicrobial commonly administered orally or topically. However, FNL has a very low water solubility, limiting its drug formulation, therapeutic application, and bioavailability through tissues. To overcome these limitations, this study aimed to develop FNL inclusion complexes (FNL-IC) with cyclodextrin (α-cyclodextrin, sulfobutylether-β-cyclodextrin, and hydroxypropyl-γ cyclodextrin) and incorporate it into a dissolvable microneedle (DMN) system to improve solubility and drug penetration. FNL-IC was evaluated for saturation solubility, Fourier transform infrared spectroscopy, differential scanning calorimetry, in vitro release, minimum inhibitory concentration, minimum fungicidal concentration, and time-killing assay. DMN-FNL-IC was evaluated for mechanical and insertion properties, surface pH, moisture absorption ability, water vapor transmission, and drug content recovery. Moreover, ocular kinetic, ex vivo antimicrobial, in vivo antifungal, and chorioallantoic membrane (HET-CAM) assays were conducted to assess the overall performance of the formulation. Mechanical strength and insertion properties revealed that DMN-FNL-IC has great mechanical and insertion properties. The in vitro release of FNL-IC was significantly improved, exhibiting a 9-fold increase compared to pure FNL. The ex vivo antifungal activity showed significant inhibition of Candida albicans from 6.54 to 0.73 log cfu/mL or 100–0.94%. In vivo numbers of colonies of 0.87 ± 0.13 log cfu/mL (F2), 4.76 ± 0.26 log cfu/mL (FNL eye drops), 3.89 ± 0.24 log cfu/mL (FNL ointments), and 8.04 ± 0.58 log cfu/mL (control) showed the effectiveness of DMN preparations against other standard commercial preparations. The HET-CAM assay showed that DMN-FNL-IC (F2) did not show any vascular damage. Finally, a combination of FNL-IC and DMN was developed appropriately for ocular delivery of FNL, which was safe and increased the effectiveness of treatments for fungal keratitis.

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Electrospun patches to deliver combination drug therapy for fungal infections

Dziemidowicz,

Meszarik,

Piovesan

et al. 2024

Front. Drug Deliv.

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Fungal infections, though affecting healthcare globally, receive insufficient attention in clinical and academic settings. Invasive fungal infections, particularly caused by combat wounds, have been identified as a critical threat by the US Department of Defense. Monotherapy with traditional antifungals is often insufficient, and so combination therapies are explored to enhance treatment efficacy. However, systemic combination treatments can result in severe adverse effects, suggesting the need for localised delivery systems, such as drug-loaded electrospun patches, to administer antifungals directly to the infection site. This proof-of-concept study hypothesised that dual amorolfine and terbinafine therapy slowly releasing from electrospun patches would be an effective way of eradicating Candida albicans when the patch was applied directly to the fungal colony. The feasibility of creating electrospun materials loaded with amorolfine and terbinafine for combination antifungal therapy was investigated. Electrospinning was used to fabricate polycaprolactone (PCL) patches with varying drug loadings (2.5%, 5%, and 10% w/w) of amorolfine and terbinafine either individually or in combination. The incorporation of both drugs in the fibres was confirmed, with the drugs predominantly in an amorphous state. Results showed that combination therapy patches had a significantly greater and prolonged antifungal effect compared to monotherapy patches, with larger zones of inhibition and sustained efficacy over at least 7 days. This study therefore demonstrates that PCL-based electrospun patches containing amorolfine and terbinafine provide superior antifungal activity against C. albicans compared to monotherapy patches. This approach could lower required drug doses, reducing adverse effects, and enhance patient compliance due to prolonged drug release, leading to more effective antifungal therapy.

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Corneal targeted Amorolfine HCl-mixed micelles for the management of ocular candidiasis: Preparation, in vitro characterization, ex vivo and in vivo assessments

Cited by 3 publications

References 72 publications

Solid Dispersion Incorporated into Dissolving Microneedles for Improved Antifungal Activity of Amphotericin B: In Vivo Study in a Fungal Keratitis Model

Solid Dispersion Incorporated into Dissolving Microneedles for Improved Antifungal Activity of Amphotericin B: In Vivo Study in a Fungal Keratitis Model

Incorporation of Inclusion Complexes in the Dissolvable Microneedle Ocular Patch System for the Efficiency of Fluconazole in the Therapy of Fungal Keratitis

Electrospun patches to deliver combination drug therapy for fungal infections

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