Abstract
Due to complicated anatomical and physical properties, targeted drug delivery to ocular tissues continues to be a key challenge for formulation scientists. Various attempts are currently being made to improve the in vivo performance of therapeutic molecules by encapsulating them in various nanocarrier systems or devices and administering them via invasive/non-invasive or minimally invasive drug administration methods. Biocompatible and biodegradable lipid nanoparticles have emerged as a potential alternative to conventional ocular drug delivery systems to overcome various ocular barriers. Lipid-based nanocarrier systems led to major technological advancements and therapeutic advantages during the last few decades of ocular therapy, such as high precorneal residence time, sustained drug release profile, minimum dosing frequency, decreased drug toxicity, targeted site delivery, and, therefore, an improvement in ocular bioavailability. In addition, such formulations can be given as fine dispersion in patient-friendly droppable preparation without causing blurred vision and ocular sensitivity reactions. The unique advantages of lipid nanoparticles, namely, solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions, and liposomes in intraocular targeted administration of various therapeutic drugs are extensively discussed. Ongoing and completed clinical trials of various liposome-based formulations and various characterization techniques designed for nanoemulsion in ocular delivery are tabulated. This review also describes diverse solid lipid nanoparticle preparation methods, procedures, advantages, and limitations. Functionalization approaches to overcome the drawbacks of lipid nanoparticles, as well as the exploration of new functional additives with the potential to improve the penetration of macromolecular pharmaceuticals, would quickly progress the challenging field of ocular drug delivery systems.
Highlights
Pharmaceutics 2022, 14, x FOR PEER REVIEWThe complex anatomy, physiology, and biochemistry of the human eye make it nearly inaccessible to foreign particulates, including drugs
The complex anatomy, physiology, and biochemistry of the human eye make it drug delivery system is to offset the protective barriers of the eye to provide high theranearly inaccessible to foreign particulates, including drugs
The low retention many ophthalmic preparations is oftenuptake restricted by short retention time, restricted per- volume meability epithelium, high pre-corneal clearance rate due to corneal rapid blinking rates transport
Summary
Pharmaceutics 2022, 14, x FOR PEER REVIEWThe complex anatomy, physiology, and biochemistry of the human eye make it nearly inaccessible to foreign particulates, including drugs. As a result, developing an ocular drug delivery system remains a fascinating and difficult issue facing formulation and. The performance ular drug deliverywithout system remains a fascinating andtissue difficult issue facing formulation and of many ophthalmic preparations is often restricted by short retention development experts. The key objective behind the design and development of an time, ocularrestricted permeability of corneal epithelium, high barriers pre-corneal rate high due therato rapid blinkdrug delivery system is to offset the protective of theclearance eye to provide ing rates (6–15 times/min), tear turn over The low retention many ophthalmic preparations is oftenuptake restricted by short retention time, restricted per- volume meability epithelium, high pre-corneal clearance rate due to corneal rapid blinking rates transport (~30 μL)ofofcorneal the conjunctival sac typically results in decreased or scleral (6–15 times/min), high tear turn over The low retention volume drug delivery strategies involving lipid nanocarriers
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