Application of lipid nanoparticles to ocular drug delivery

Abstract

Although eye drops are widely used as drug delivery systems for the anterior segment of the eye, they are also associated with poor drug bioavailability due to transient contact time and rapid washout by tearing. Moreover, effective drug delivery to the posterior segment of the eye is challenging, and alternative routes of administration (periocular and intravitreal) are generally needed, the blood-retinal barrier being the major obstacle to systemic drug delivery. Areas covered: Nanotechnology, and especially lipid nanoparticles, can improve the therapeutic efficiency, compliance and safety of ocular drugs, administered via different routes, to both the anterior and posterior segment of the eye. This review highlights the main ocular barriers to drug delivery, as well as the most common eye diseases suitable for pharmacological treatment in which lipid nanoparticles have proved efficacious as alternative delivery systems. Expert opinion: Lipid-based nanocarriers are among the most biocompatible and versatile means for ocular delivery. Mucoadhesion with consequent increase in pre-corneal retention time, and enhanced permeation due to cellular uptake by corneal epithelial cells, are the essential goals for topical lipid nanoparticle delivery. Gene delivery to the retina has shown very promising results after intravitreal administration of lipid nanoparticles as non-viral vectors.

Nanocarrier mediated retinal drug delivery: overcoming ocular barriers to treat posterior eye diseases

“…As controlled release systems, they can reduce the need for frequent intravitreal injections while their small size (<500 nm) may enhance penetration across any rate‐limiting barriers thus providing the potential to deliver therapeutic concentrations to the retinal tissues . Additionally, nanocarriers can remain in the eye for several months after administration maintaining therapeutic concentrations at the target site over longer periods . In this review, we discuss the effectiveness of different nanocarriers reported to date, including polymeric nanosphere, nanocapsules, liposomes, nanomicelles, nanocrystals, and dendrimers, in delivering therapeutic agents to the retinal tissues in a safe and effective manner with reference to recent preclinical studies.…”

Mildly Cross-Linked Dendrimer Hydrogel Prepared via Aza-Michael Addition Reaction for Topical Brimonidine Delivery

“…9, 10 Lipids, Hyaluronic acid, PEG, PLGA and chitosan are commonly used polymers as topical drug delivery carriers and have been fabricated into particles and hydrogels. 11–19 In particular, particle-based colloidal drug delivery systems help overcome the cornea barrier and realize prolonged drug release. 20–22 In addition, they do not cause blurriness.…”

Functional intercalated nanocomposites with chitosan-glutathione-glycylsarcosine and layered double hydroxides for topical ocular drug delivery

“…7 Effective topical drug delivery poses a major challenge due to the presence of various elimination mechanisms and physiological barriers that result in low ocular bioavailability. [8][9][10] Increasing the retention time in the precorneal area and improving the permeability across ocular tissues of drugs are two major key aspects to enhance ocular bioavailability. 1 Ban et al developed positively charged chitosan (CTS)-coated solid lipid nanoparticles with high ocular bioavailability, which was ascribed to the electrostatic interaction between the positively charged nanoparticles and the negatively charged ocular surface.…”