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核心技术专利:CN118964589B侵权必究
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Exploring the potential of antifungal-loaded proniosomes to consolidate corneal permeation in fungal keratitis: A comprehensive investigation from laboratory characterization to microbiological 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 Feb 24;9:100322. doi: 10.1016/j.ijpx.2025.100322. eCollection 2025 Jun.


DOI:10.1016/j.ijpx.2025.100322
PMID:40094144
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11909449/
Abstract

This work aimed to prepare Terconazole loaded proniosomes (TCZ-PNS) utilizing modified coacervation technique for the management of fungal keratitis. Terconazole (TCZ) is a potent antifungal with poor aqueous solubility posing intricacies in its incorporation in ocular formulations. A 2 factorial design was adopted to probe independent formulation variables including A: Lecithin: cholesterol ratio, B: Surfactant: cholesterol ratio and C: Span® 80 contribution (% of total SAA). The formulae, generated by the design, were prepared and scrutinized regarding entrapment efficiency (%EE), particle size (PS), polydispersity index (PDI) and zeta potential (ZP). Numerical desirability algorithms selected an optimum TCZ-PNS which boasted plausible %EE (89.51 % ± 0.94 %), nanoscale vesicles consistent with TEM measurements (247.9 ± 0.42 nm), a sufficiently high ZP (-43.42 ± 0.85 mV), and an in-vitro biphasic release profile that remained stable even after Gamma irradiation and short-term storage. The transcorneal ex-vivo permeation of TCZ-PNS was higher than that of TCZ suspension (≈ 2-fold). The formulation was further evaluated for pH, corneal hydration threshold, and histopathological safety, confirming its suitability for ocular application. Confocal laser microscopy revealed substantial corneal uptake (approximately twice as deep as of TCZ suspension). Additionally, microbiological assessments of the optimal TCZ-PNS compared to TCZ suspension demonstrated an inhibition zone nearly 50 % larger, a significantly lower MIC and MFC (64-fold reduction), and enhanced biofilm inhibition activity across most tested concentrations. These findings suggest that TCZ-PNS could be a propitious treatment choice to deeply deliver antifungal therapy for the eradication of deeply rooted and inaccessible fungal keratitis.

摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/626dd340f7fa/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/2531b61844bb/ga1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/9af9a3b06c20/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/4d6ab22e07f4/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/9820f816ffd8/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/313401102959/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/9cf700157765/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/626dd340f7fa/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/2531b61844bb/ga1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/9af9a3b06c20/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/4d6ab22e07f4/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/9820f816ffd8/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/313401102959/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/9cf700157765/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6c7/11909449/626dd340f7fa/gr6.jpg

相似文献

[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]
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[8]
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引用本文的文献

[1]
Development and characterization of fenticonazole nitrate-loaded cubogel for the management of vaginal candidiasis.

Int J Pharm X. 2025-7-10

[2]
Terconazole loaded edge-activated hybrid elastosome for revamped corneal permeation in ocular mycosis: In-vitro characterization, statistical optimization, microbiological assessment, and in-vivo evaluation.

Int J Pharm X. 2025-4-8

本文引用的文献

[1]
Transdermal application of diacerin loaded-terpene enriched invasomes: an approach to augment anti-edema and nociception inhibition activity.

J Liposome Res. 2025-3

[2]
Capped flexosomes for prominent anti-inflammatory activity: development, optimization, and ex vivo and in vivo assessments.

Drug Deliv Transl Res. 2024-9

[3]
Fungal Keratitis: Diagnosis, Management, and Recent Advances.

Clin Ophthalmol. 2024-1-10

[4]
Sonophoresis-assisted transdermal delivery of antimigraine-loaded nanolipomers: Radio-tracking, histopathological assessment and in-vivo biodistribution study.

Int J Pharm. 2023-9-25

[5]
Darifenacin Self-assembled Liquid Crystal Cubic Nanoparticles: a Sustained Release Approach for an Overnight Control of Overactive Bladder.

AAPS PharmSciTech. 2023-5-12

[6]
High amount of lecithin facilitates oral delivery of a poorly soluble pyrazoloquinolinone ligand formulated in lipid nanoparticles: Physicochemical, structural and pharmacokinetic performances.

Int J Pharm. 2023-2-25

[7]
Sertaconazole-Nitrate-Loaded Leciplex for Treating Keratomycosis: Optimization Using D-Optimal Design and In Vitro, Ex Vivo, and In Vivo Studies.

Pharmaceutics. 2022-10-18

[8]
Pronounced capping effect of olaminosomes as nanostructured platforms in ocular candidiasis management.

Drug Deliv. 2022-12

[9]
Advanced Vesicular Systems for Antifungal Drug Delivery.

AAPS PharmSciTech. 2022-7-28

[10]
Hyaluronic Acid: Its Versatile Use in Ocular Drug Delivery with a Specific Focus on Hyaluronic Acid-Based Polyelectrolyte Complexes.

Pharmaceutics. 2022-7-15

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