Abstract
Dry eye disease (DED) or keratoconjunctivitis sicca is a chronic multifactorial disorder of the ocular surface caused by tear film dysfunction. Symptoms include dryness, irritation, discomfort and visual disturbance, and standard treatment includes the use of lubricants and topical steroids. Secondary inflammation plays a prominent role in the development and propagation of this debilitating condition. To address this we have investigated the pilot scale development of an innovative drug delivery system using a dexamethasone-encapsulated cholesterol-Labrafac™ lipophile nanostructured lipid carrier (NLC)-based ophthalmic formulation, which could be developed as an eye drop to treat DED and any associated acute exacerbations. After rapid screening of a range of laboratory scale pre-formulations, the chosen formulation was prepared at pilot scale with a particle size of 19.51 ± 0.5 nm, an encapsulation efficiency of 99.6 ± 0.5%, a PDI of 0.08, and an extended stability of 6 months at 4 °C. This potential ophthalmic formulation was observed to have high tolerability and internalization capacity for human corneal epithelial cells, with similar behavior demonstrated on ex vivo porcine cornea studies, suggesting suitable distribution on the ocular surface. Further, ELISA was used to study the impact of the pilot scale formulation on a range of inflammatory biomarkers. The most successful dexamethasone-loaded NLC showed a 5-fold reduction of TNF-α production over dexamethasone solution alone, with comparable results for MMP-9 and IL-6. The ease of formulation, scalability, performance and biomarker assays suggest that this NLC formulation could be a viable option for the topical treatment of DED.
Highlights
Dry eye disease (DED) is one of the most prevalent eye conditions seen throughout the world
It can be broadly divided into two predominant, but often overlapping categories, of evaporative dry eye (EDE) and aqueous deficient dry eye (ADDE), with EDE being the more prevalent [1]
Garrigue et al recently outlined the importance of lipid-based technologies in an extensive review and nanostructured lipid carrier (NLC) are suitably well placed in terms of biocompatibility and potential drug encapsulation for such purposes [28]
Summary
Dry eye disease (DED) is one of the most prevalent eye conditions seen throughout the world. It can be broadly divided into two predominant, but often overlapping categories, of evaporative dry eye (EDE) and aqueous deficient dry eye (ADDE), with EDE being the more prevalent [1]. ADDE refers to conditions effecting lacrimal gland function while. EDE is related to disorders of the lid margin such as meibomian gland disease (MGD) and ocular surface abnormalities such as mucin deficiency and contact lens-related problems. Redness, irritation, blurred vision, light sensitivity, itching and foreign body sensation and in addition to these ocular surface-related problems, there are Pharmaceutics 2021, 13, 905.
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