Liposomes as a Novel Ocular Delivery System for Brinzolamide: In Vitro and In Vivo Studies |
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Authors: | Huili Li Yongmei Liu Ying Zhang Dailong Fang Bei Xu Lijing Zhang Tong Chen Ke Ren Yu Nie Shaohua Yao Xiangrong Song |
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Affiliation: | 1.State Key Laboratory of Biotherapy and Cancer Center,West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy,Chengdu,China;2.School of Pharmaceutical Science & Yunnan Key Laboratory of Pharmacology for Natural Products,Kunming Medical University,Kunming,China;3.Department of Pharmaceutical Sciences,University of Nebraska Medical Center,Omaha,USA |
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Abstract: | The objective of this study was to investigate the potential of liposomes as an ophthalmic delivery system for brinzolamide (Brz) to enhance the local glaucomatous therapeutic effect. The liposomes of Brz (Brz-LPs) were produced by the thin-film dispersion method with a particle size of 84.33?±?2.02 nm and an entrapment efficiency of 98.32?±?1.61%. Differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD) analysis proved that Brz was successfully entrapped into Brz-LPs. Brz-LPs displayed a biphasic release pattern in vitro with burst release initially and sustained release afterwards. The corneal permeability was measured using modified Franz-type diffusion cells, and Brz-LPs showed 6.2-fold increase in the apparent permeability coefficient when compared with the commercial available formulation (B rz-Sus). Moreover, Brz-LPs (1 mg/mL Brz) showed a more sustained and effective intraocular pressure reduction (5–10 mmHg) than Brz-Sus (10 mg/mL Brz) in white New Zealand rabbits. Therefore, Brz-LPs were a hopeful formulation of Brz for glaucoma treatment and worthy of further investigation. |
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