ArticleAAPS PharmSciTech2026
DoE-Optimized Chitosan-Coated pH-Sensitive Liposomes for Targeted Nose-to-Brain Delivery of Temozolomide.
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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Authors and funding
3 authors.
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Abstract
Glioblastoma is an aggressive brain tumor with limited treatment efficacy due to poor blood-brain barrier (BBB) penetration and intrinsic resistance. Temozolomide (TMZ), the frontline chemotherapeutic, undergoes rapid hydrolysis at physiological pH, with low systemic bioavailability and efflux-mediated clearance. To address this, we developed chitosan-coated pH-sensitive liposomes (SpH-TMZ-CS-LIPO) that were optimized via Box-Behnken design, achieving 223.48 ± 1.93 particle size, 35.72 ± 0.51 zeta potential, and 78.85 ± 2.62% entrapment. The formulation exhibited pH-sensitive release, with cumulative TMZ release of 92-94% at pH 4.5-5.5, following diffusion-controlled kinetics. Ex vivo permeation across goat nasal mucosa at pH 5.5 showed a 1.39-fold increase in TMZ flux compared to Free TMZ, while mucin adsorption studies demonstrated superior mucoadhesion. In U87MG cells, SpH-TMZ-CS-LIPO showed 4.6-fold higher uptake than Free TMZ and markedly enhanced cytotoxicity, reducing viability to 3.92 ± 1.56% (IC
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