Sunflower Oil-Based Polyol-Urethane Nanoparticles for Sustained Delivery of Olanzapine

Nova Southeastern University, Davie, Florida, USA

Objective. A facile route based on cyclic carbonate ring-opening reaction has been utilized to synthesize a bio-based polyol-containing urethane bond [polyol-urethane (POU)] as a nanoparticulate drug delivery system of olanzapine in order to enhance its bioavailability. Background. The forefront horizon of biomedical investigations in recent decades is parceling-up and delivery of drugs to achieve controlled/targeted release. In this regard, developing green-based delivery systems for a spatiotemporal controlling therapeutic agent have drawn a lot of attention. Methods. The biodegradable and biocompatible hyper-branched POU containing several hydroxyl and urethane bonds, was synthesized via an easy method of cyclic carbonate ring opening reaction followed by ethanol amine addition. After characterization, the nanoparticles were also estimated for in vitro release, toxicity, and pharmacokinetic studies. Results. As olanzapine has shown poor bioavailability and permeability in the brain, the sustained release of olanzapine from the designed carriers could enhance pharmacokinetic effectiveness. POU in the aqueous solution formed micelles with a hydrophobic core and embedded olanzapine under the influence of its hydrophobic nature. Drug release from the nanoparticles (90 ± 0.43 nm in diameter) indicated a specific pattern with initial burst release, and then a sustained release behavior (82 ± 3% after 168 h), by the Higuchi-based release mechanism. Pharmacokinetics assessments of POU-olanzapine nanoparticles were carried in male Wistar rats through intravenous administration. Conclusion. The obtained results paved a way to introduce the POU as an efficient platform to enhance the bioavailability of olanzapine in therapeutic methods. The POU is a safe drug carrier due to bio-based materials used in its preparation.