Ocular Drug Delivery Systems and Formulations

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: 20 December 2025 | Viewed by 918

Special Issue Editor


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Guest Editor
1. Department of Pharmacology, Pharmacy and Pharmaceutical Technology, University of Santiago de Compostela (USC), 15705 Santiago de Compostela, Spain
2. Instituto de Investigação e Inovação em Saúde (i3S), Universidade do Porto, Porto, Portugal
Interests: drug delivery systems; pharmaceutics; nanoparticles; cyclodextrins; ophtalmic formulations
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Special Issue Information

Dear Colleagues,

Efficient drug delivery to ocular tissues remains a challenge due to the eye’s unique anatomical and physiological barriers. These barriers limit drug absorption, bioavailability, and therapeutic efficacy. In response, recent advances in the development of nanoscale drug delivery systems and novel biomaterials have opened new possibilities for targeted and sustained ocular therapies.

Innovative formulations—such as nanoparticles, liposomes, dendrimers, hydrogels, in situ gelling systems, and biodegradable implants, among others—offer enhanced drug stability, controlled release, prolonged residence time, and the ability to overcome conventional delivery limitations. These strategies enhance the penetration of therapeutic agents through ocular tissues, improving the treatment of different ocular structures, minimizing systemic absorption, and reducing potential side effects.

This Special Issue provides a comprehensive overview of recent advances in ocular drug delivery, focusing on cutting-edge formulations and delivery systems that are designed to overcome various ocular barriers.

By emphasizing the synergy between material science, pharmaceutical technology, and ocular biology, this Special Issue aims to inform and inspire future research toward more effective and patient-friendly ocular therapeutics.

Dr. Victoria Díaz-Tomé
Guest Editor

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Keywords

  • ocular drug delivery
  • ophthalmic formulations
  • ophthalmic drug bioavailability
  • ophthalmic hydrogels
  • ophthalmic pharmaceutical nanotechnology
  • ocular therapies

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Published Papers (1 paper)

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Research

27 pages, 16394 KB  
Article
Sustained Intraocular Pressure Reduction Using Bisoprolol-Loaded PLGA Nanoparticles: A Promising Strategy for Enhanced Ocular Delivery with Reduced GFAP Expression Indicative of Lower Glial Activation
by Sammar Fathy Elhabal, Omnia Mohamed Mahfouz, Mohamed Fathi Mohamed Elrefai, Mahmoud H. Teaima, Ahmed Abdalla and Mohamed El-Nabarawi
Pharmaceutics 2025, 17(11), 1418; https://doi.org/10.3390/pharmaceutics17111418 - 31 Oct 2025
Viewed by 638
Abstract
Background/Objectives: Glaucoma is a neurodegenerative optic disorder which occurs due to persistent elevation of the intraocular pressure. It leads to permanent blindness and currently affects over 75 million individuals worldwide. Nowadays, topical ocular medications are the leading therapy despite their poor ocular [...] Read more.
Background/Objectives: Glaucoma is a neurodegenerative optic disorder which occurs due to persistent elevation of the intraocular pressure. It leads to permanent blindness and currently affects over 75 million individuals worldwide. Nowadays, topical ocular medications are the leading therapy despite their poor ocular penetration and short residence time. Methods: The purpose of this research is to formulate bisoprolol hemifumarate-loaded polylactic-co-glycolic acid (PLGA) nanoparticles and improve their ocular penetration and bioavailability for the treatment of glaucoma by enhancing the delivery of the drug to the posterior part of eye. By using the solvent displacement method, formulations were prepared and optimum formula was elected using Design-Expert® software. Results: In vitro characterization demonstrated that the optimum formula contained 25 mg BSP, 22.5 mg PLGA, and 60 mg Tween80, yielding high values of drug encapsulation (75%) and zeta potential (−18.7 ± 0.41 mV), with a low particle size (105 ± 0.35 nm) and polydispersity index (0.411 ± 0.71). Transmission electron microscopy and atomic force microscopy showed smooth and spherical nanosized particles. X-ray diffraction, differential scanning calorimetry, and Fourier-transform infrared spectroscopy revealed successful encapsulation of the drug inside the polymeric matrix. Ex vivo confocal laser scanning microscopy proved that there was better uptake of the drug upon using PLGA-NPs. In vitro release profiles indicated biphasic drug release from the PLGA-NPs, confirming a sustained drug release over 12 h. In vivo studies showed that BSP-PLGA-NPs significantly reduced the IOP compared to bisoprolol solution. Quantitative immunohistochemistry showed lower retinal GFAP expression with BSP-PLGA-NPs compared with induced controls and drug solution, which is indicative of attenuated glial activation. Conclusions: These data support improved ocular delivery and an improved pharmacodynamic effect; however, they demonstrate association rather than a direct mechanistic suppression of glial pathways. Full article
(This article belongs to the Special Issue Ocular Drug Delivery Systems and Formulations)
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