Cationic lipid emulsions as potential bioadhesive carriers for ophthalmic delivery of palmatine

Abstract

Palmatine (PM) is a potent anti-infective agent used to treat eye diseases. However, PM is less effective for ocular application due to short residence time within the eyes. This study aimed to develop a cationic lipid emulsions (CLEs) for ophthalmic delivery of PM and evaluate its suitability in infection treatment. PM-loaded CLEs (PM-CLEs) were prepared through emulsifying/high-pressure homogenisation and characterised by particle size, ζ potential and morphology. The resulting PM-CLEs possessed a particle size of 192 nm and ζ potential of 45 mV around. In vitro release illustrated that PM was released less from CLEs. Corneal bioadhesion test showed that PM-CLEs exhibited an enhanced ocular residence time. Improved anti-infective activity was achieved in the model of fungus-induced keratitis. Furthermore, PM-CLEs demonstrated predominant cellular uptake and internalisation in the corneal epithelial cells. These results provide proof of concept that CLEs are promising bioadhesive carriers for ophthalmic delivery of PM.

Novel Eye Drop Delivery Systems: Advance on Formulation Design Strategies Targeting Anterior and Posterior Segments of the Eye

“…As a drug reservoir, MEs can deliver both hydrophilic and hydrophobic drugs to the cornea [193]. In addition to this, they have a wide range of properties: natural biodegradability, nanoscale droplet size, sterility, good solubility in either the innermost oil phase or the oil-water interface, and good ocular absorption [194]. Nanoemulsions (NEs) are also nanostructured emulsion consisting of an aqueous phase, an oil phase, a surfactant, and a cosurfactant and differ most from MEs in that they have a smaller particle size.…”

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

“…As a result, a considerable elongation in residence time and uptake of drug moieties is observed [ 72 ]. Therefore, cationic lipid nanoparticles may prove highly promising vehicles for ophthalmic delivery of drug, particularly for poorly water-soluble moieties [ 88 ]. Table 2 lists recent studies reporting the development of cationic lipid nanoparticle for ocular delivery.…”

Ophthalmic Drug Delivery Systems for Antibiotherapy—A Review

“…The researchers obtained a particle size of 190 nm, a zeta potential of +45 mV. They demonstrated an improvement of the ocular residence time and concluded on a predominant cellular uptake and an internalization in the corneal epithelial cells [ 58 ].…”