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核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2025

Terconazole loaded edge-activated hybrid elastosome for revamped corneal permeation in ocular mycosis: In-vitro characterization, statistical optimization, microbiological assessment, and in-vivo evaluation.

作者信息

Ahmed Sadek, Farag Michael M, Attia Heba, Balkhi Bander, Adel Islam M, Nemr Asmaa Ashraf

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.

Department of Microbiology and Immunology, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.

出版信息

Int J Pharm X. 2025 Apr 8;9:100333. doi: 10.1016/j.ijpx.2025.100333. eCollection 2025 Jun.


DOI:10.1016/j.ijpx.2025.100333
PMID:40292341
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12023791/
Abstract

Herein, we investigated the preparation and characterization of Terconazole loaded edge-activated hybrid elastosome (TCN-EHE) adopting thin film hydration technique for the treatment of ocular mycosis. Terconazole (TCN) is a broad spectrum antimycotic agent suffering from sparse aqueous solubility impeding its use in ophthalmic preparations. The scrutinized formulation variables namely X: Surfactant: Edge activator ratio (SAA: EA), X: Pluronic® L121 contribution (% of total SAA) and X: EA concentration (%/) were optimized adopting D-optimal design. Ten runs were prepared and characterized regarding their entrapment efficiency, particle size, polydispersity index and zeta potential. An optimized formula was generated, with high desirability, exhibited satisfactory entrapment efficiency, nanoscaled particle size aligning with TEM, plausible zeta potential and bi-phasic release pattern which were not altered after short-term storage. The optimized TCN-EHE displayed 1.94-fold enhanced ex-vivo corneal permeation flux. Safety was ratified through measured corneal hydration level, pH and histopathological evaluation. In-vivo corneal uptake visualized by confocal laser microscopy demonstrated 2.7-fold deeper penetration. Moreover, Superior antifungal activity has been demonstrated displaying 37 % bigger zone of inhibition, 8-fold lower minimum inhibitory and minimum fungal concentration alongside significantly higher biofilm inhibition activity at all tested concentrations for the optimized TCN-EHE compared to TCN suspension. Conclusively, we could prospect that TCN-EHE might be a revamped therapeutic alternative for the delivery of poorly soluble antimycotic agents for the combat of ocular mycosis.

摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/9d99b21b25c5/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/af1e05f9ec2b/ga1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/702e6b397386/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/d632c61be6ef/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/543831737592/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/513a01452d9a/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/6421e30830a9/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/9522fa33365b/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/9d99b21b25c5/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/af1e05f9ec2b/ga1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/702e6b397386/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/d632c61be6ef/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/543831737592/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/513a01452d9a/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/6421e30830a9/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/9522fa33365b/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c7b/12023791/9d99b21b25c5/gr7.jpg

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本文引用的文献

[1]
Exploring the potential of antifungal-loaded proniosomes to consolidate corneal permeation in fungal keratitis: A comprehensive investigation from laboratory characterization to microbiological evaluation.

Int J Pharm X. 2025-2-24

[2]
Augmented glycerosomes as a promising approach against fungal ear infection: Optimization and microbiological, and assessments.

Int J Pharm X. 2024-10-22

[3]
Self-Nanoemulsifying/ Self-Assembled Cubic Nanoparticles Lyophilized Tablet: A Novel Biphasic Release Approach to Enhance the Bioavailability of a Lipophilic Drug.

AAPS PharmSciTech. 2024-10-21

[4]
Development of transferosomes for topical ocular drug delivery of curcumin.

Eur J Pharm Biopharm. 2024-12

[5]
Transdermal application of diacerin loaded-terpene enriched invasomes: an approach to augment anti-edema and nociception inhibition activity.

J Liposome Res. 2025-3

[6]
Capped flexosomes for prominent anti-inflammatory activity: development, optimization, and ex vivo and in vivo assessments.

Drug Deliv Transl Res. 2024-9

[7]
Flexosomes as a promising nanoplatform for enhancing tolnaftate ocular delivery: Formulation, in vitro characterization, statistical optimization, ex vivo and microbial in vivo studies.

Int J Pharm. 2023-11-5

[8]
Sonophoresis-assisted transdermal delivery of antimigraine-loaded nanolipomers: Radio-tracking, histopathological assessment and in-vivo biodistribution study.

Int J Pharm. 2023-9-25

[9]
The effect of charges on the corneal penetration of solid lipid nanoparticles loaded Econazole after topical administration in rabbits.

Eur J Pharm Sci. 2023-8-1

[10]
Recent trends and updates on ultradeformable and elastic vesicles in ocular drug delivery.

Drug Discov Today. 2023-8

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