ArticleAAPS PharmSciTech2026
Comparison of Chitosan-Poloxamer Nanoparticles and Poloxamer-based In-Situ Forming Gel for Nose-to-Brain Delivery of Cetrorelix: In Vitro and Pharmacokinetic Studies in Rats.
Article in AAPS PharmSciTech, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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5 authors.
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Abstract
Intranasal drug delivery provides rapid absorption and high bioavailability while reducing systemic exposure, making it a hopeful route for nose-to-brain (N2B) transport. However, no effective N2B system has yet been systematically studied for cetrorelix, which is a GnRH antagonist used in reproductive medicine. In this study, a cetrorelix-loaded chitosan-Pluronic F-127 (Chi-Plx) nanoparticle system with a complementary Plx in-situ gel to extend nasal residence time was developed. The formulations were characterized for physicochemical properties, release behavior, cytotoxicity, and pharmacokinetics in rats. Chi-Plx nanoparticles exhibited a mean diameter of 18.7 ± 2.1 nm, PDI of 0.35 ± 0.03, and near-neutral zeta potential. They demonstrated a biphasic release profile with an initial burst (52%) followed by sustained release, achieving 70-80% cumulative release at 1440 min, while the in-situ gel released 65-70% over the same period. Cytotoxicity assays confirmed acceptable biocompatibility, with lower toxicity than the gel formulation. Pharmacokinetic analysis revealed that Chi-Plx nanoparticles achieved markedly higher brain C
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Registered trials
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