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Spanlastic-laden in situ gel as a promising approach for ocular delivery of Levofloxacin: In-vitro characterization, microbiological assessment, corneal permeability and in-vivo study

The objective of this study was to encapsulate the antibacterial drug levofloxacin hemihydrate (LF) into spanlastics (SLs) followed by incorporation into gelrite in situ gel to enhance its antibacterial activity and sustain ocular delivery. A combination of Span 60 as main vesicle component and Twee...

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Autores principales: Agha, Omnia Ahmed, Girgis, Germeen N.S., El-Sokkary, Mohamed M.A., Soliman, Osama Abd El-Azeem
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10407905/
https://www.ncbi.nlm.nih.gov/pubmed/37560488
http://dx.doi.org/10.1016/j.ijpx.2023.100201
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author Agha, Omnia Ahmed
Girgis, Germeen N.S.
El-Sokkary, Mohamed M.A.
Soliman, Osama Abd El-Azeem
author_facet Agha, Omnia Ahmed
Girgis, Germeen N.S.
El-Sokkary, Mohamed M.A.
Soliman, Osama Abd El-Azeem
author_sort Agha, Omnia Ahmed
collection PubMed
description The objective of this study was to encapsulate the antibacterial drug levofloxacin hemihydrate (LF) into spanlastics (SLs) followed by incorporation into gelrite in situ gel to enhance its antibacterial activity and sustain ocular delivery. A combination of Span 60 as main vesicle component and Tweens as an edge activator (EA) was used to prepare SLs using the thin film hydration method. A 3(2) factorial design was applied to study the effect of formulation variables (ratio of Span 60: EA and type of EA) on SLs characteristics (encapsulation efficiency (EE%), particle size (PS), zeta potential (ZP) and percentage of drug released). In-vitro antimicrobial study was conducted to determine the antibacterial activity of the optimized formula. Finally confocal laser scanning microscopy (CLSM) was applied to monitor SLs corneal penetration. The optimum formulation (F5), contains 240 mg Span 60 and 60 mg Tween 60 as EA. F5 exhibited EE% = 59.7 ± 4.2%, PS = 177.6 ± 1.8 nm, PDI = 0.27 ± 0.022 and ZP = -40.6 ± 0.68 mV. Furthermore, only 39.37 ± 0.72% of LF amount was released after 4 h compared to complete release from drug solution. The apparent permeation coefficient was (14.7 × 10(−3) cm/h) compared to (9.7 × 10(−3) cm/h) for LF solution. Moreover, F5 exhibited 200% and 100% increase in the antibacterial efficacy against Pseudomonas aeruginosa and Staphylococcus aureus respectively.
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spelling pubmed-104079052023-08-09 Spanlastic-laden in situ gel as a promising approach for ocular delivery of Levofloxacin: In-vitro characterization, microbiological assessment, corneal permeability and in-vivo study Agha, Omnia Ahmed Girgis, Germeen N.S. El-Sokkary, Mohamed M.A. Soliman, Osama Abd El-Azeem Int J Pharm X Research Paper The objective of this study was to encapsulate the antibacterial drug levofloxacin hemihydrate (LF) into spanlastics (SLs) followed by incorporation into gelrite in situ gel to enhance its antibacterial activity and sustain ocular delivery. A combination of Span 60 as main vesicle component and Tweens as an edge activator (EA) was used to prepare SLs using the thin film hydration method. A 3(2) factorial design was applied to study the effect of formulation variables (ratio of Span 60: EA and type of EA) on SLs characteristics (encapsulation efficiency (EE%), particle size (PS), zeta potential (ZP) and percentage of drug released). In-vitro antimicrobial study was conducted to determine the antibacterial activity of the optimized formula. Finally confocal laser scanning microscopy (CLSM) was applied to monitor SLs corneal penetration. The optimum formulation (F5), contains 240 mg Span 60 and 60 mg Tween 60 as EA. F5 exhibited EE% = 59.7 ± 4.2%, PS = 177.6 ± 1.8 nm, PDI = 0.27 ± 0.022 and ZP = -40.6 ± 0.68 mV. Furthermore, only 39.37 ± 0.72% of LF amount was released after 4 h compared to complete release from drug solution. The apparent permeation coefficient was (14.7 × 10(−3) cm/h) compared to (9.7 × 10(−3) cm/h) for LF solution. Moreover, F5 exhibited 200% and 100% increase in the antibacterial efficacy against Pseudomonas aeruginosa and Staphylococcus aureus respectively. Elsevier 2023-07-24 /pmc/articles/PMC10407905/ /pubmed/37560488 http://dx.doi.org/10.1016/j.ijpx.2023.100201 Text en © 2023 The Authors https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Research Paper
Agha, Omnia Ahmed
Girgis, Germeen N.S.
El-Sokkary, Mohamed M.A.
Soliman, Osama Abd El-Azeem
Spanlastic-laden in situ gel as a promising approach for ocular delivery of Levofloxacin: In-vitro characterization, microbiological assessment, corneal permeability and in-vivo study
title Spanlastic-laden in situ gel as a promising approach for ocular delivery of Levofloxacin: In-vitro characterization, microbiological assessment, corneal permeability and in-vivo study
title_full Spanlastic-laden in situ gel as a promising approach for ocular delivery of Levofloxacin: In-vitro characterization, microbiological assessment, corneal permeability and in-vivo study
title_fullStr Spanlastic-laden in situ gel as a promising approach for ocular delivery of Levofloxacin: In-vitro characterization, microbiological assessment, corneal permeability and in-vivo study
title_full_unstemmed Spanlastic-laden in situ gel as a promising approach for ocular delivery of Levofloxacin: In-vitro characterization, microbiological assessment, corneal permeability and in-vivo study
title_short Spanlastic-laden in situ gel as a promising approach for ocular delivery of Levofloxacin: In-vitro characterization, microbiological assessment, corneal permeability and in-vivo study
title_sort spanlastic-laden in situ gel as a promising approach for ocular delivery of levofloxacin: in-vitro characterization, microbiological assessment, corneal permeability and in-vivo study
topic Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10407905/
https://www.ncbi.nlm.nih.gov/pubmed/37560488
http://dx.doi.org/10.1016/j.ijpx.2023.100201
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