ArticleAAPS PharmSciTech2006
Effect of formulation factors on in vitro transcorneal permeation of gatifloxacin from aqueous drops.
Article in AAPS PharmSciTech, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 77 citations in OpenAlex.
- Randomized pharmacokinetic and pharmacodynamic comparison of fluoroquinolones for tuberculous meningitis.Antimicrobial agents and chemotherapy · 2011Trial
- Clinical Benefits of Preservative-Free Treatment for Glaucoma with a Focus on Preservative-Free Latanoprost.Ophthalmology and therapy · 2025Review
- Cord blood-derived biologics lead to robust axonal regeneration in benzalkonium chloride-injured mouse corneas by modulating the Il-17 pathway and neuropeptide Y.Molecular medicine (Cambridge, Mass.) · 2024Article
- Preparation and Evaluation of Cubosomes/Cubosomal Gels for Ocular Delivery of Beclomethasone Dipropionate for Management of Uveitis.Pharmaceutical research · 2020Article
- Ocular Surface Disease and Glaucoma Medications: A Clinical Approach.Eye & contact lens · 2019Review
- Current perspectives on corneal collagen crosslinking (CXL).Graefe's archive for clinical and experimental ophthalmology = Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie · 2018Review
- Topical delivery of acetazolamide by encapsulating in mucoadhesive nanoparticles.Asian journal of pharmaceutical sciences · 2017Article
- RES-loaded pegylated CS NPs: for efficient ocular delivery.IET nanobiotechnology · 2017Article
- Systematic review and Meta-analysis comparing modified cross-linking and standard cross-linking for progressive keratoconus.International journal of ophthalmology · 2017Article
- Comprehensive evaluation of formulation factors for ocular penetration of fluoroquinolones in rabbits using cassette dosing technique.Drug design, development and therapy · 2016Article
- Phytosome-hyaluronic acid systems for ocular delivery of L-carnosine.International journal of nanomedicine · 2016Article
- Evaluation of gatifloxacin pluronic micelles and development of its formulation for ocular delivery.Drug delivery and translational research · 2014Article
- BAC-EDTA transepithelial riboflavin-UVA crosslinking has greater biomechanical stiffening effect than standard epithelium-off in rabbit corneas.Experimental eye research · 2014Article
- Effect of formulation factors on in vitro transcorneal permeation of voriconazole from aqueous drops.Journal of advanced pharmaceutical technology & research · 2013Article
- Aliphatic β-nitroalcohols for therapeutic corneoscleral cross-linking: corneal permeability considerations.Cornea · 2013Article
- [Morphological alterations induced by preservatives in eye drops].Der Ophthalmologe : Zeitschrift der Deutschen Ophthalmologischen Gesellschaft · 2012Article
- Ocular insert for sustained delivery of gatifloxacin sesquihydrate: Preparation and evaluations.International journal of pharmaceutical investigation · 2012Article
- Transepithelial corneal collagen cross-linking in ultrathin keratoconic corneas.Clinical ophthalmology (Auckland, N.Z.) · 2012Article
- Corneal alternations induced by topical application of benzalkonium chloride in rabbit.PloS one · 2011Article
- Effect of pH and formulation variables on in vitro transcorneal permeability of flurbiprofen: a technical note.AAPS PharmSciTech · 2008Article
Corrections and comments
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Authors and funding
2 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The purpose of this research was to optimize the formulation factors for maximum in vitro permeation of gatifloxacin from aqueous drops through excised goat cornea and to evaluate the permeation characteristics of drug from selected marketed eyedrop formulations. Permeation studies were conducted by putting 1 mL of formulation on the cornea (0.67 cm(2)) fixed between the donor and receptor compartments of an all-glass modified Franz diffusion cell and measuring gatifloxacin concentration in the receptor (containing normal saline under stirring) by spectrophotometry at 291.5 nm, after 120 minutes. Raising the drug concentration of the drops increased the drug permeation but decreased the percent permeation and the in vitro ocular availability. Raising the pH of the formulation from pH 5 to 7.2 increased both the drug permeation and the in vitro ocular availability. Eyedrops containing benzalkonium chloride (BAK; 0.01% wt/vol) and disodium edetate (EDTA; 0.01% wt/vol) showed maximum permeation, followed by Zymar, BAK (0.01% wt/vol), Gatilox, Gatiquin, and Gate (statistically significant P < .05 compared with control). In vitro titration of the formulations with 0.1N NaOH indicated the presence of a buffer in Zymar (pH 6) and Gate (pH 5.8), which may cause irritation and induce lacrimation, resulting in reduced ocular availability in vivo. Thus, formulation with BAK and EDTA, which is unbuffered, has a better likelihood of being absorbed in vivo. The BAK-EDTA formulation significantly (P < .05) increased the permeation of gatifloxacin through paired excised corneas of goat, sheep, and buffalo, compared with the control formulation. The goat cornea showed the greatest increase in permeation, followed by the sheep and buffalo corneas.
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