Abstract

This review highlights the application of lipid nanoparticles (Solid Lipid Nanoparticles, Nanostructured Lipid Carriers, or Lipid Drug Conjugates) as effective drug carriers for pathologies affecting the posterior ocular segment. Eye anatomy and the most relevant diseases affecting the posterior segment will be summarized. Moreover, preparation methods and different types and subtypes of lipid nanoparticles will also be reviewed. Lipid nanoparticles used as carriers to deliver drugs to the posterior eye segment as well as their administration routes, pharmaceutical forms and ocular distribution will be discussed emphasizing the different targeting strategies most recently employed for ocular drug delivery.

Highlights

  • Ocular diseases associated with the posterior segment of the eye may lead to visual impairment, which might result in blindness

  • The retinal pigment epithelium (RPE) is a single-layered structure with tight juncand cones, which are adjacent to the RPE, and their distribution varies in different regions tions which is outside the neurosensory retina

  • Posterior juxtascleral, sub-Tenon and retrobulbar routes are usually used for administration of anesthesics [26,32], subconjunctival, suprachoroidal, subretinal and trans-scleral routes are used for delivering active compounds to inner tissues; (i) the subconjunctival route involves the insertion of the drug or implant underneath the conjunctiva, which allows the access to the sclera [26,32,45]; (ii) the suprachoroidal route is used for implants, microneedles and other formulations

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Summary

Introduction

Ocular diseases associated with the posterior segment of the eye may lead to visual impairment, which might result in blindness. Less than 5% of the administered traditional ocular eye drops are effectively absorbed into the eye, reaching the inner ocular tissues. Ocular drug delivery systems were investigated to improve ocular retention and drug absorption. They can act as controlled release systems that reduce administration frequency. These drug delivery systems include hydrogels, nanomicelles, dendrimers, polymeric nanoparticles, nanosuspensions, liposomes and lipid nanoparticles [4,5]. Pharmaceutics 2022, 14, 90 constitute one of the most relevant systems due to their unique characteristics and their multiple advantages compared to other drug delivery approaches such as liposomes or polymeric nanoparticles [6,7]

Ocular Anatomy
The Anterior Segment
Tear Film
Corneal Barrier
90 REVIEW
Conjunctival Barrier
Post-Corneal
Efflux Transporters
The Posterior Segment
Anatomy of the Posterior Segment
Drug Delivery Routes
Topical Administration
Permeation
Pugliaet
Intravitreal Administration
Periocular Administration
Lipid Nanoparticles
Types of Lipid Nanoparticles
Solid Lipid Nanoparticles
Nanostructured Lipid Carriers
Solvent Emulsification-Evaporation
Solvent Emulsification-Diffusion
Ultrasonication or High Shear Homogenization
Supercritical Fluid Extraction of Emulsions
Microemulsion Based Method
Double Emulsion Method
Precipitation Method
Film-Ultrasound Dispersion
3.2.10. Solvent Injection Method
3.2.11. Membrane Contractor Method
3.2.12. Phase Inversion Temperature Method
3.2.13. Coacervation Method
Physicochemical Characteristics of Nanoparticles to Achieve Posterior Segment
Excipients for Ocular Drug Delivery
Lipids
Penetration Enhancers
Viscosity-Enhancing Agents
Other Excipients
Lipid Nanoparticles for the Posterior Segment
Diabetic Retinopathy
Uveitis
Glaucoma
Retinitis Pigmentosa
Challenges in Ocular Drug Delivery to the Posterior Segment of the Eye
Conclusions
Findings
Methods
Full Text
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