Dexibuprofen Biodegradable Nanoparticles: One Step Closer towards a Better Ocular Interaction Study

Abstract

Ocular inflammation is one of the most prevalent diseases in ophthalmology, which can affect various parts of the eye or the surrounding tissues. Non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen, are commonly used to treat ocular inflammation in the form of eye-drops. However, their bioavailability in ocular tissues is very low (less than 5%). Therefore, drug delivery systems such as biodegradable polymeric PLGA nanoparticles constitute a suitable alternative to topical eye administration, as they can improve ocular bioavailability and simultaneously reduce drug induced side effects. Moreover, their prolonged drug release can enhance patient treatment adherence as they require fewer administrations. Therefore, several formulations of PLGA based nanoparticles encapsulating dexibuprofen (active enantiomer of Ibuprofen) were prepared using the solvent displacement method employing different surfactants. The formulations have been characterized and their interactions with a customized lipid corneal membrane model were studied. Ex vivo permeation through ocular tissues and in vivo anti-inflammatory efficacy have also been studied.

Natural Ergot Alkaloids in Ocular Pharmacotherapy: Known Molecules for Novel Nanoparticle-Based Delivery Systems

“…Nanosized particles were explored for the entrapment of drugs as a novel strategy to increase their targetability, bioavailability, and therapeutic effect, as well as the range of molecules to be clinically used [ 52 ]. Since their introduction as drug delivery systems, solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were explored for use in the most diverse administration routes ( Figure 4 ).…”

“…Since their introduction as drug delivery systems, solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were explored for use in the most diverse administration routes ( Figure 4 ). Among them, these lipid systems represent an interesting approach for the ocular route, due to their ability to improve the corneal penetration of drugs [ 48 , 52 , 53 , 54 , 55 , 56 ]. SLNs and NLCs are delivery systems that combine the advantages of liposomes and emulsions (biocompatibility and possibility to scale-up) with the advantages of polymeric nanoparticles (protection of the drug and modulation of the release profile) [ 57 ].…”

“…Such in situ formulations generally allow gelation at corneal temperature [ 51 ], thus avoiding the burst release of the loaded drug in the initial hours of administration. As a result, higher drug concentration in deeper regions of eye (aqueous humor) may take place [ 52 , 131 ]. This system was sequentially employed to increase the bioavailability of hydrophobic drugs, particularly corticosteroids for ocular disorders [ 115 ].…”

Dexibuprofen Therapeutic Advances: Prodrugs and Nanotechnological Formulations

“…Moreover, they also assessed several PLGA NPs with different PEGylation degrees and several surfactants adapted for ocular drug delivery using DXI as a model drug. In this sense, DXI potential to be used for drug delivery was demonstrated and its ability to decrease ocular inflammation more effectively using PEGylated PLGA nanoparticles was confirmed [ 63 ]. Other authors have also used PLGA nanoparticles for ocular drug delivery of NSAIDs, thus confirming the therapeutic potential of these biodegradable nanoparticles [ 64 , 65 ].…”

Liposome encapsulated surfactant abetted copper nanoparticles alleviates biofilm mediated virulence in pathogenic Pseudomonas aeruginosa and MRSA

“…One promising approach in the ground of antibacterial treatment is the application of nanotechnology-assisted components for averting and treating infections caused by resistant bacteria. Nanoparticles exhibit greater antimicrobial potential through the striking mechanisms such as (1) attachment towards bacterial superficial area, (2) deterioration of bacterial cell wall and outer membrane with alteration in its penetrability, (3) initiation of toxicity and oxidative stress by ROS release, and (4) intonation of signal transduction pathways 11 . Nanoparticles sustained on numerous suitable materials, such as carbon, polyurethane foam, polymers, and sepiolite have also been efficiently applied for bactericidal applications.…”