Liposomes as a Novel Ocular Delivery System for Brinzolamide: In Vitro and In Vivo Studies.
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.
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu, Sichuan, 610041, China.
Huili
H
Li
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu, Sichuan, 610041, China.
Yongmei
Y
Liu
School of Pharmaceutical Science & Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming, Yunnan, 650500, China.
Ying
Y
Zhang
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu, Sichuan, 610041, China.
Dailong
D
Fang
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu, Sichuan, 610041, China.
Bei
B
Xu
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu, Sichuan, 610041, China.
Lijing
L
Zhang
School of Pharmaceutical Science & Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming, Yunnan, 650500, China.
Tong
T
Chen
Department of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, Nebraska, 68198, USA.
Ke
K
Ren
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu, Sichuan, 610041, China.
Yu
Y
Nie
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu, Sichuan, 610041, China. shaohuayao@scu.edu.cn.
Shaohua
S
Yao
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu, Sichuan, 610041, China. songxr@scu.edu.cn.
Xiangrong
X
Song
D060433:Administration, Ophthalmic; D000818:Animals; D002152:Calorimetry, Differential Scanning / Q000379:methods; D002257:Carbonic Anhydrase Inhibitors / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D003315:Cornea / Q000187:drug effects / Q000378:metabolism*; D016503:Drug Delivery Systems / Q000379:methods*; D008081:Liposomes; D008297:Male; D009924:Organ Culture Techniques; D011817:Rabbits; D013449:Sulfonamides / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D013843:Thiazines / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D014961:X-Ray Diffraction / Q000379:methods
D002257:Carbonic Anhydrase Inhibitors; D008081:Liposomes; D013449:Sulfonamides; D013843:Thiazines; C111827:brinzolamide
brinzolamide; glaucoma; intraocular pressure; liposomes; permeability