Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 410, Issue 1-2, Pages 31-40Publisher
ELSEVIER
DOI: 10.1016/j.ijpharm.2011.03.007
Keywords
Sustained ophthalmic delivery; In situ gelling system; Baicalin; Carbopol; Hydroxypropylmethylcellulose
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Funding
- International Science Cooperation Project of China [2007DFC31670]
- National Key Technology Research and Development Program of China [2009ZX09311-002]
- Chinapostdoctor Special Funded Project [2010003304]
- Program for Changjiang Scholars and Innovative Research Team in University
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Baicalin has been reported to have anti-inflammatory and anti-cataract effects on eye tissues, but it has a low bioavailability partly due to its poor stability of baicalin, the special anatomic structure and efficient protective mechanism of eyes. The aim of this study was to investigate the correlation between the stability of baicalin and in situ pH-triggered gelling system. Carbopol (R) 974P (0.3%, w/v) was used as the gelling agent combined with hydroxypropylmethylcellulose E4M (0.6%, w/v) which acted as a viscosity enhancing agent. In vitro and in vivo evaluations were performed using several techniques, namely confocal scanning light microscopy analysis, rheometry, Gamma scintigraphic technique and microdialysis method. The rheological behavior showed a significant enhancement in gel strength under physiological conditions, and the formulation provided sustained release of the drug over an 8-h period. In elimination studies, the radioactivity of formulation was always higher than that of the control solution. Additionally, the AUC and C-max values were 6.1-fold and 3.6-fold higher than those of the control solution, respectively. The results demonstrated that an in situ pH-triggered gelling system have better ability to keep baicalin stable and retain drug release than marketed baicalin eye drops to enhance the ocular bioavailability. Crown Copyright (C) 2011 Published by Elsevier B.V. All rights reserved.
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