Tropical Journal of Pharmaceutical Research
Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria
Vol. 15, No. 7, 2016, pp. 1369-1374
Bioline Code: pr16181
Full paper language: English
Document type: Research Article
Document available free of charge
Tropical Journal of Pharmaceutical Research, Vol. 15, No. 7, 2016, pp. 1369-1374
© Copyright 2016 - Tropical Journal of Pharmaceutical Research
In situ epicatechin-loaded hydrogel implants for local drug delivery to spinal column for effective management of post-traumatic spinal injuries|
Lu, Jun; Ju, You-ting; Chen, Shou-lin; Cai, Jun-ying; Xu, Guo-hai & Hu, Yan-hui
Purpose: To prepare hydrogels loaded with epicatechin, a strong antioxidant, anti-inflammatory, and
neuroprotective tea flavonoid, and characterise them in situ as a vehicle for prolonged and safer drug
delivery in patients with post-traumatic spinal cord injury.
Methods: Five in situ gel formulations were prepared using chitosan and evaluated in terms of their
visual appearance, clarity, pH, viscosity, and in vitro drug release. In vivo anti-inflammatory activity was
determined and compared with 2 % piroxicam gel as standard. Motor function activity in a rat model of
spinal injury was examined comparatively with i.v. methylprednisolone as standard.
Results: The N-methyl pyrrolidone solution (containing 1 % w/w epicatechin with 2 to 10 % w/w
chitosan) of the in situ gel formulation had a uniform pH in the range of 4.01 ± 0.12 to 4.27 ± 0.02. High
and uniform drug loading, ranging from 94.48 ± 1.28 to 98.08 ± 1.24 %, and good in vitro drug release
(79.48 ± 2.84 to 96.48 ± 1.02 % after 7 days) were achieved. The in situ gel prepared from 1 %
epicatechin and 2 % chitosan (E5) showed the greatest in vivo anti-inflammatory activity (60.58 %
inhibition of paw oedema in standard carrageenan-induced hind rat paw oedema model, compared with
48.08 % for the standard). The gels showed significant therapeutic effectiveness against post-traumainduced
spinal injury in rats. E5 elicited maximum motor activity (horizontal bar test) in the spinal injury
rat model; the rats that received E5 treatment produced an activity score of 3.62 ± 0.02 at the end of 7
days, compared with 5.0 ± 0.20 following treatment with the standard.
Conclusion: In situ epicatechin-loaded gel exhibits significant neuroprotective and anti-inflammatory
effects, and therefore can potentially be used for prolonged and safe drug delivery in patients with
traumatic spinal cord injury.
Epicatechin; In situ gel; Chitosan; Spinal injury; Post-traumatic; Motor activity; Antiinflammatory
Alternative site location: http://www.tjpr.org