Successfully Improving Ocular Drug Delivery Using the Cationic Nanoemulsion, Novasorb

Abstract

Topical ophthalmic delivery of active ingredients can be achieved using cationic nanoemulsions. In the last decade, Novagali Pharma has successfully developed and marketed Novasorb, an advanced pharmaceutical technology for the treatment of ophthalmic diseases. This paper describes the main steps in the development of cationic nanoemulsions from formulation to evaluation in clinical trials. A major challenge of the formulation work was the selection of a cationic agent with an acceptable safety profile that would ensure a sufficient ocular surface retention time. Then, toxicity and pharmacokinetic studies were performed showing that the cationic emulsions were safe and well tolerated. Even in the absence of an active ingredient, cationic emulsions were observed in preclinical studies to have an inherent benefit on the ocular surface. Moreover, clinical trials demonstrated the efficacy and safety of cationic emulsions loaded with cyclosporine A in patients with dry eye disease. Ongoing studies evaluating latanoprost emulsion in patients with ocular surface disease and glaucoma suggest that the beneficial effects on reducing ocular surface damage may also extend to this patient population. The culmination of these efforts has been the marketing of Cationorm, a preservative-free cationic emulsion indicated for the symptomatic treatment of dry eye.

Design of cationic lipid nanoparticles for ocular delivery: Development, characterization and cytotoxicity

“…This is a smart strategy that combines the positive surface charge of the particles and the negative surface charge of ocular mucosa by means of an electrostatic attraction. This approach could increase the drugs retention time in the eye as well as improve nanoparticles bioadhesion (Lallemand et al, 2012).…”

Preparation, characterization, and evaluation of antitumor effect of Brucea javanica oil cationic nanoemulsions

“…Some literatures have reported that cationic nanoemulsions can not only improve the permeability of poor water-soluble drugs 25 but also form complexes with macromolecular drugs (containing functional groups with a large number of negatively charge), such as nucleic acids, proteins, and other large molecules, to protect them from enzyme degradation and improve their absorption. 26 The absorption mechanism is probably that cationic particles have electrostatic interaction and mucosal adhesion with negatively charged membrane of the contacted organs, such as skin, 27,28 eyes, 26,29 and gastrointestinal mucosa, 30,31 to improve drugs' retention and permeability. 26,30 Chitosan is a kind of cationic alkaline polysaccharide extracted from crustaceans and is widely used in biomedical engineering with good biocompatibility and biodegradability.…”

Untitled

“…Many efforts in ophthalmic drug delivery have been devoted to elongate the contact time of the vehicle at ocular surface, slow down the elimination of the drug, to improved patient compliance, to increase bioavailability and increase its corneal penetration 48 .Studies have shown that NEs have the ability to provide sustained release of a drug and higher penetration to the deeper layers of the ocular structure and aqueous humor and hence as compared to conventional system of the drug delivery NE enhances the therapeutic efficacy and pharmacokinetic parameters of the drug 47,49 .…”