ArticleDaru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences2015
Improved intraocular bioavailability of ganciclovir by mucoadhesive polymer based ocular microspheres: development and simulation process in Wistar rats.
Article in Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 33 citations in OpenAlex.
- Trial
- Chitosan Nanoparticles: Approaches to Preparation, Key Properties, Drug Delivery Systems, and Developments in Therapeutic Efficacy.AAPS PharmSciTech · 2025Review
- Biodegradable microspheres come into sight: A promising biomaterial for delivering drug to the posterior segment of the eyeball.Materials today. Bio · 2024Review
- Biodegradable Polymer-Based Drug-Delivery Systems for Ocular Diseases.International journal of molecular sciences · 2023Review
- Updates on Biodegradable Formulations for Ocular Drug Delivery.Pharmaceutics · 2023Review
- Management and control of intraocular pressure applying macitentan hydrogel film formulation: improved effect of surfactant and cosurfactant system.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2022Article
- Nanotechnology for Topical Drug Delivery to the Anterior Segment of the Eye.International journal of molecular sciences · 2021Review
- Self-Assembled chitosan/phospholipid nanoparticles: from fundamentals to preparation for advanced drug delivery.Drug delivery · 2020Review
- Chitosan and its Derivatives for Ocular Delivery Formulations: Recent Advances and Developments.Polymers · 2020Review
- Advances and limitations of drug delivery systems formulated as eye drops.Journal of controlled release : official journal of the Controlled Release Society · 2020Review
- Strategies for Improving Ocular Drug Bioavailability and Corneal Wound Healing with Chitosan-Based Delivery Systems.Polymers · 2018Review
- A comprehensive insight on ocular pharmacokinetics.Drug delivery and translational research · 2016Review
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundThe poor ocular bioavailability of the conventional eye drops is due to lack of corneal permeability, nasolacrimal drainage and metabolic degradation. To overcome this issue, drug encapsulated in mucoadhesive polymer based ocular microspheres have the advantages of improved drug stability, easy administration in liquid form, diffuse rapidly and better ocular tissue internalization.
methodsThe ganciclovir chitosan microspheres (GCM) were prepared by modified water-in-oil emulsification method. The formulation was optimized and characterized by investigating in vitro release study, release kinetics, XRD and microspheres stability. Ocular irritancy, in vivo ocular pharmacokinetic parameters and histopathology study was evaluated in Wistar rats. The use of pharmacokinetic/pharmacodynamic indices and simulation process was carried out to further ensure clinical applicability of the formulation.
resultsThe in vitro release study showed initial burst (nearly 50 %) in first few minutes and followed Fickian (R(2) = 0.9234, n-value = 0.2329) type of diffusion release mechanism. The XRD and stability studies showed favorable results. The Wistar rat eyes treated with GCM showed significant increase in ganciclovir AUC (~4.99-fold) and Cmax (2.69-fold) in aqueous humor compared to ganciclovir solution and delay in Tmax. The Cmax/MIC90, AUC0-24/MIC90, AUC above MIC90 and T above MIC90 were significantly higher in GCM group. The aqueous humor concentration-time profile of ganciclovir in GCM and ganciclovir solution was simulated with every 28.1 and 12.8 h, respectively. The simulated concentration-time profile shows that in duration of 75 h, the ganciclovir solution require six ocular instillations compared to three ocular instillations of the GCM formulation. The photomicrograph of GCM and ganciclovir solution treated rat retina showed normal organization and cytoarchitecture.
conclusionsCorrelating with in vitro data, the formulation showed sustained drug release along with improved intraocular bioavailability of ganciclovir in Wistar rats.
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