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Official PDF TranslationChinese Traditional and Herbal Drugs

Preparation and Anti-Migraine Pharmacodynamic Evaluation of Puerarin-Loaded Chitosan-Modified β-Cyclodextrin Nasal Supramolecular Gel

Authors: ZONG Shiyu; WANG Miao; MA Xinyu; LIU Shuo; REN Jia; CHENG Yunlong; WANG Chunliu

DOI: 10.7501/j.issn.0253-2670.2026.16.20261609Status: Verified Translated Edition
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Key Findings in This Report

• • Optimal formulation: CS-β-CD to sodium carboxymethylcellulose mass ratio 1:9, total polymer concentration 2.6%, puerarin loading 40 mg. This specific ratio and concentration yielded a three-dimensional porous gel with pH 6.5, a critical quality attribute for nasal tolerability and mucoadhesion. • • In vitro release: 82.75% cumulative puerarin release within 4 h, followed by sustained release. This biphasic profile addresses the clinical need for rapid onset (migraine abortive phase) combined with extended action (prophylactic phase), potentially reducing dosing frequency. • • Pharmacodynamic efficacy: In nitroglycerin-induced chronic migraine rats, the gel significantly reduced brain CGRP and IL-1β levels and increased 5-HT content. These biomarker shifts directly correlate with attenuated neurogenic inflammation and restored neurotransmitter balance, supporting a multi-target anti-migraine mechanism. • • Safety and translational gap: No nasal mucosal irritation was observed, but brain-targeting efficiency remains unquantified. The absence of LC-MS/MS or imaging data for brain puerarin concentration means that while efficacy is promising, the actual brain bioavailability and nose-to-brain transport fraction are unknown, representing a critical hurdle for clinical translation.