Benefits of cetalkonium chloride cationic oil-in-water nanoemulsions for topical ophthalmic drug delivery

Abstract

ObjectivesTopical ocular administration is the most convenient route of administration of drugs for the treatment of eye diseases. However, the bioavailability of drugs following eye instillations of eye drops is very low. Over the past 20 years, extensive efforts have been put into research to improve drug bioavailability without compromising treatment compliance and patients' quality of life.Key findingsOne of the most efficient ways to improve drug bioavailability is to increase the precorneal residence time of the eye drop formulations. As a result, new eye drops, with bioadhesive properties, have been developed based on the cationic oil-in-water (o/w) nanoemulsion technology. These low viscosity eye drop nanoemulsions have improved precorneal residence time through the electrostatic interactions between the positively charged oil nanodroplets and the negatively charged ocular surface epithelium.SummaryThis review is the first to present the benefits of this new strategy used to improve ocular drug bioavailability. The roles of the cationic agent in the stabilization of a safe cationic o/w nanoemulsion have been discussed, as well as the unexpected benefits of the cationic o/w nanoemulsion for the protection and restoration of a healthy tear film and corneal epithelium.

Development of loteprednol etabonate-loaded cationic nanoemulsified in-situ ophthalmic gel for sustained delivery and enhanced ocular bioavailability

“…All the formulations represent the zeta potential in the range of À6.22 to À20.27 mV. One of our goals was also to make cationic nanoemulsion because of its positive charge; it should form electrostatic interactions with negatively charged ocular surface and increase the precorneal residence time of formulations which may enhance permeation and ocular bioavaibility (Lallemand et al, 2012;Daull et al, 2013). The higher positive charge of the cationic agents leads to the higher stability of nanoemulsion due to the creation of an electrostatic repulsion amongst the oil droplets of the nanoemulsion.…”

Advances in ophthalmic drug delivery

“…In the present issue, Moosa et al .,[1] Souza et al [2]. and Daull et al [3]. reviewed advances in topical drug delivery.…”

“…On the other hand, the combination of these delivery systems with physical methods would appear to be a promising tool to decrease the dose and frequency of administration; thereby, patient compliance and treatment efficacy will be improved. Likewise, Daull et al [3] exclusively reviewed cationic o/w nanoemulsions that represent a new development strategy to improve ocular drug delivery of lipophilic drug molecules. Cationic oil-in-water (o/w) nanoemulsions extend one step further the benefits of the o/w nanoemulsions for drug delivery by improving their residence time over that observed with the anionic o/w nanoemulsions.…”

Secondary dry eye syndrome after keratorefractive surgeries and approaches to its treatment and prevention

“…Кроме того, возмещает водный слой, обеспечивая подлежащим структурам достаточное увлажнение, а также оказывая осмокорригирующее и осмопротекторное действие, тем самым защищая клетки поверхности глаза. За счет биоадгезии к поверхности глаза препарат способствует восстановлению муцинового слоя и уменьшает трение век о поверхность глаза во время моргания [57,58].…”