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

IF 5.2 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Omnia Ahmed Agha , Germeen N.S. Girgis , Mohamed M.A. El-Sokkary , Osama Abd El-Azeem Soliman
{"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","authors":"Omnia Ahmed Agha ,&nbsp;Germeen N.S. Girgis ,&nbsp;Mohamed M.A. El-Sokkary ,&nbsp;Osama Abd El-Azeem Soliman","doi":"10.1016/j.ijpx.2023.100201","DOIUrl":null,"url":null,"abstract":"<div><p>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<sup>2</sup> 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<sup>−3</sup> cm/h) compared to (9.7 × 10<sup>−3</sup> cm/h) for LF solution. Moreover, F5 exhibited 200% and 100% increase in the antibacterial efficacy against <em>Pseudomonas aeruginosa</em> and <em>Staphylococcus aureus</em> respectively.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":null,"pages":null},"PeriodicalIF":5.2000,"publicationDate":"2023-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/1c/ad/main.PMC10407905.pdf","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Pharmaceutics: X","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S2590156723000452","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0

Abstract

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 32 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.

Abstract Image

作为左氧氟沙星眼部给药的一种有前景的方法:体外表征、微生物学评估、角膜渗透性和体内研究
本研究的目的是将抗菌药物半水合左氧氟沙星(LF)包封在塑料(SLs)中,然后加入到凝胶原位凝胶中,以增强其抗菌活性并维持眼部给药。以Span 60为主要囊泡组分,Tweens为边缘活化剂(EA),采用薄膜水化法制备了SLs。采用32因子设计研究了处方变量(Span 60: EA比和EA类型)对SLs特性(包封率(EE%)、粒径(PS)、ζ电位(ZP)和释药率)的影响。通过体外抑菌实验确定优化后的配方的抑菌活性。最后应用共聚焦激光扫描显微镜(CLSM)监测SLs角膜穿透。最佳配方(F5)以240 mg Span 60和60 mg Tween 60为EA,其EE% = 59.7±4.2%,PS = 177.6±1.8 nm, PDI = 0.27±0.022,ZP = -40.6±0.68 mV。与药物溶液完全释放相比,4 h后LF的释放量仅为39.37±0.72%。其表观渗透系数为14.7 × 10−3 cm/h,而LF溶液的表观渗透系数为9.7 × 10−3 cm/h。F5对铜绿假单胞菌和金黄色葡萄球菌的抑菌效果分别提高200%和100%。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 求助全文
来源期刊
International Journal of Pharmaceutics: X
International Journal of Pharmaceutics: X Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.60
自引率
0.00%
发文量
32
审稿时长
24 days
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信