Glaucoma is an accumulative optic neuropathy resulted from increasing intraocular pressure. Brinzolamide (BRZ) is a kind of carbonic anhydrase inhibitors for glaucoma treatment. In this study, brinzolamide-hydroxypropyl-beta-cyclodextrin (BRZ-HP-beta-CD) inclusion complex was prepared by solvent evaporation method to improve the solubility of BRZ and enhance the therapeutic effect of BRZ. The formation of the inclusion complex was confirmed by Fourier transform infrared spectroscopy, differential scanning calorimeter and nuclear magnetic resonance spectroscopy. The solubility of BRZ increased about 10-fold after the formation of the BRZ-HP-beta-CD inclusion complex. The in vitro corneal accumulative permeability of the inclusion complex increased 2.91-fold compared to the Commercial available formulation (AZOP (R)). In addition, BRZ-HP-beta-CD inclusion complex (0.5% BRZ) had an equivalent efficiency of lowering intraocular pressure with AZOPT (R) (1% BRZ) in vivo. These results identified the BRZ-HP-beta-CD inclusion complex might have a promising future as a novel formulation of BRZ for glaucoma treatment. (C) 2013 Elsevier Ltd. All rights reserved.
[1]Sichuan Univ, West China Hosp, State Key Lab Biotherapy, Chengdu 610041, Sichuan, Peoples R China.
[2]Univ Nebraska, Med Ctr, Dept Pharmaceut Sci, Omaha, NE 68198 USA.
[3]Kunming Med Univ, Sch Pharmaceut Sci, Kunming 650500, Yunnan, Peoples R China.
[4]Kunming Med Univ, Yunnan Key Lab Pharmacol Nat Prod, Kunming 650500, Yunnan, Peoples R China.
[5]Chengdu Normal Univ, Sci Educ Dept, Cent Lab, Chengdu 610041, Sichuan, Peoples R China.
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