Purchase this article with an account.
David L Kent, Gautam Behl, Sangeeta Kumari, Niall O' Reilly, Peter McLoughlin, Orla O' Donovan, Laurence Fitzhenry; Enhanced Ocular Delivery Using Biocompatible Nanomaterials. Invest. Ophthalmol. Vis. Sci. 2019;60(9):287.
Download citation file:
© ARVO (1962-2015); The Authors (2016-present)
Dry eye disease affects an estimated 350 million people worldwide and the efficacy of conventional topical treatments can be hugely variable. The use of biocompatible nanomaterials is one approach that could enhance topical efficacy. This study focuses on the synthesis, characterisation and evaluation of lipid-based nanoformulations developed to improve therapeutic delivery using eye drops.
Two lipid-based nanoformulations were developed for the treatment of dry eye: (a) cholesterol-based nanostructed lipid carriers (NLCs) and (b) a cholesterol-based liposomal-microemulsions (LMEs) formulation. Both were used to encapsulate dexamethasone. Preparation methods at lab (probe sonication) and pilot scale (high-pressure homogenisation) were compared. Nanomaterials were initally characterised for their encapsulation efficiency, drug release, size and zeta potential. Suitable formulations were further tested for cytotoxicity, cell adhesion and ex-vivo corneal penetration. The stability of the most successful formulations was carried out over a 6-month period at 5°C and 25°C (60% Relative Humidity).
Nanomaterials prepared at a size range of 20-30 nm at the pilot scale demonstrated a reduction from 50 nm and 150 nm at lab scale preparation for LMEs and NLCs respectively. Drug encapsulation ranged from 95-99% with release rates for the LMEs of 60% in 12 hours and 0.3% in 12 hours for NLCs. All materials demonstrated excellent cytotoxicity profiles. The prepared nanomaterials also displayed mucoadhesive as well as barrier penetrating properties (Figure 1 (a)). In the ex vivo porcine eye model the optimal formulations demonstrated an increase in aqueous humour concentration 50% greater than a commercial dexamethasone formulation (Figure 1(b)).
Lipid-based nonomaterial formulations prepared from biocompatible materials displayed properties that have the potential to enhance conventional eye drop formulations for the treatment of dry eye disease. The synthesized nanomaterials demonstrated high drug loading capability, controlled drug release and excellent cytotoxicity profiles with suitable stability over a 6-month period. Formulation of a pilot scale batch suggested the potential to produce these formulations on an industrial scale.
This abstract was presented at the 2019 ARVO Annual Meeting, held in Vancouver, Canada, April 28 - May 2, 2019.
This PDF is available to Subscribers Only