Lipid-Based Nanoparticulate Systems for the Ocular Delivery of Bioactives with Anti-Inflammatory Properties

• Published in: International journal of molecular sciences 2022-10, Vol.23 (20), p.12102
• Main Authors: Ana, Raquel da, Fonseca, Joel, Karczewski, Jacek, Silva, Amélia M., Zielińska, Aleksandra, Souto, Eliana B.
• Format: Article
• Language: English
• Subjects: Anti-inflammatory agents; Bioavailability; Biocompatibility; Biological activity; Compliance; Cornea; Drug delivery; Drug delivery systems; Drug development; Drugs; Inflammation; Lipids; Lipophilic; Nanoparticles; Nanotechnology; Ophthalmology; Particle size; Physiology; Retina; Review; Therapeutic applications; Topical medication; Tumor necrosis factor-TNF
• ISSN: 1422-0067; 1661-6596; 1422-0067
• DOI: 10.3390/ijms232012102

The complexity of the eye structure and its physiology turned ocular drug administration into one of the most challenging topics in the pharmaceutical field. Ocular inflammation is one of the most common ophthalmic disorders. Topical administration of anti-inflammatory drugs is also commonly used as a side treatment in tissue repair and regeneration. The difficulty in overcoming the eye barriers, which are both physical and chemical, reduces drug bioavailability, and the frequency of administration must be increased to reach the therapeutic effect. However, this can cause serious side effects. Lipid nanoparticles seem to be a great alternative to ocular drug delivery as they are composed from natural excipients and can encapsulate both hydrophilic and lipophilic drugs of different sources, and their unique properties, as their excellent biocompatibility, safety and adhesion allow to increase the bioavailability, compliance and achieve a sustained drug release. They are also very stable, easy to produce and scale up, and can be lyophilized or sterilized with no significant alterations to the release profile and stability. Because of this, lipid nanoparticles show a great potential to be an essential part of the new therapeutic technologies in ophthalmology to deliver synthetic and natural anti-inflammatory drugs. In fact, there is an increasing interest in natural bioactives with anti-inflammatory activities, and the use of nanoparticles for their site-specific delivery. It is therefore expected that, in the near future, many more studies will promote the development of new nanomedicines resulting in clinical studies of new drugs formulations.