Nanoemulsion as a feasible and biocompatible carrier for ocular delivery of travoprost: Improved pharmacokinetic/pharmacodynamic properties.

Travoprost is a synthetic prostaglandin F2α analogue used in treatment of glaucoma. Due to its water insolubility and oily nature, novel delivery systems need to be developed to enhance its bioavailability, and sustain its release. In the current work, travoprost nanoemulsion was explored as a novel carrier prepared using low energy technique. Results showed that travoprost nanoemulsions exhibited suitable nanodroplet size, zeta potential, pH, refractive index, controlled release, as well as sufficient stability under accelerated conditions. In vivo studies delineated the enhanced absorption of travoprost nanoemulsion compared to the marketed eye drops Travatan®, as proven by the higher Cmax and AUC of the former, and its prolonged intraocular pressure reduction time. Moreover, the nanoemulsion formulation was proven safe and non-irritant to ocular surfaces. Therefore, it can be suggested that travoprost nanoemulsion is a promising ocular delivery system for glaucoma treatment.

Pharmacokinetics and Safety of Travoprost 0.004% Ophthalmic Solution Preserved with Polyquad in Pediatric Patients with Glaucoma.

PURPOSE: To evaluate the systemic pharmacokinetics (PKs) of travoprost 0.004% preserved with Polyquad® (TRAVATAN®) in pediatric patients with glaucoma or ocular hypertension. METHODS: This was a phase 1, open-label, multicenter clinical study of patients aged ≥2 months to <18 years. Patients received daily administration of travoprost 0.004% preserved with Polyquad in both eyes for 7 days. Plasma samples were collected 30 min before the final dose and at 10, 20, 40, and 80 min postdose. The main outcome measure was maximum concentration of travoprost free acid in plasma (Cmax). RESULTS: Included in the PK analysis were 24 patients (average age 9.6 ± 4.9 years). At least 1 sample with quantifiable levels of travoprost free acid was collected for 11 patients. The mean Cmax was 0.0471 ± 0.0105 ng/mL for patients aged 2 months to <3 years; 0.0258 ± 0.0128 ng/mL for ages 3 to <12 years; and 0.0109 ± 0.0005 ng/mL for ages 12 to <18 years. Travoprost was undetectable in samples collected predose from pediatric patients. Treatment-related adverse events (AEs) included hyperemia, eye pain, and eye pruritus (n = 1 each). There were no discontinuations or drug-related serious AEs. CONCLUSIONS: Travoprost free acid concentration in plasma was low in pediatric patients, detectable in only 11 of 24 patients. There was no accumulation of travoprost over the course of treatment. No clear relationship was observed between age/body surface area and Cmax. No increased risk was identified for the use of travoprost 0.004% preserved with Polyquad in patients <18 years of age.