Open AccessEnhanced brain targeting of curcumin by intranasal administration of a thermosensitive poloxamer hydrogel
Author(s) -
Chen Xi,
Zhi Feng,
Jia Xuefeng,
Zhang Xiang,
Ambardekar Rohan,
Meng Zhengjie,
Paradkar Anant R.,
Hu Yiqiao,
Yang Yilin
Publication year - 2013
Publication title -
journal of pharmacy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.745
H-Index - 118
eISSN - 2042-7158
pISSN - 0022-3573
DOI - 10.1111/jphp.12043
Subject(s) - curcumin , nasal administration , pharmacology , poloxamer , chemistry , drug delivery , controlled release , poloxamer 407 , nasal cavity , medicine , surgery , organic chemistry , copolymer , polymer
Objectives The aim of this study was to develop a curcumin intranasal thermosensitive hydrogel and to improve its brain targeting efficiency. Methods The hydrogel gelation temperature, gelation time, drug release and mucociliary toxicity characteristics as well as the nose‐to‐brain transport in the rat model were evaluated. Key findings The developed nasal hydrogel, composed of P luronic F 127 and P oloxamer 188, had shorter gelation time, longer mucociliary transport time and produced prolonged curcumin retention in the rat nasal cavity at body temperature. The hydrogel release mechanism was diffusion‐controlled drug release, evaluated by the dialysis membrane method, but dissolution‐controlled release when evaluated by the membraneless method. A mucociliary toxicity study revealed that the hydrogel maintained nasal mucosal integrity until 14 days after application. The drug‐targeting efficiencies for the drug in the cerebrum, cerebellum, hippocampus and olfactory bulb after intranasal administration of the curcumin hydrogel were 1.82, 2.05, 2.07 and 1.51 times that after intravenous administration of the curcumin solution injection, respectively, indicating that the hydrogel significantly increased the distribution of curcumin into the rat brain tissue, especially into the cerebellum and hippocampus. Conclusions A thermosensitive curcumin nasal gel was developed with favourable gelation, release properties, biological safety and enhanced brain‐uptake efficiency.