Citation: Zhou Yang, Fang Aiping, Wang Fazhan, Li Huili, Jin Quansheng, Huang Lingjing, Fu Chunmei, Zeng Jun, Jin Zhaohui, Song Xiangrong. Core-shell lipid-polymer nanoparticles as a promising ocular drug delivery system to treat glaucoma[J]. Chinese Chemical Letters, ;2020, 31(2): 494-500. doi: 10.1016/j.cclet.2019.04.048 shu

Core-shell lipid-polymer nanoparticles as a promising ocular drug delivery system to treat glaucoma

Zhou Yang ^a,1 ,
Fang Aiping ^a,1 ,
Wang Fazhan ^a,1 ,
Li Huili ^a ,
Jin Quansheng ^a ,
Huang Lingjing ^b ,
Fu Chunmei ^b ,
Zeng Jun ^a ,
Jin Zhaohui ^a,*, ,
Song Xiangrong ^a,*,

a.
State Key Laboratory of Biotherapy and Cancer Center/Department of Pharmacy, West China Hospital, and Collaborative Innovation Center for Biotherapy, Sichuan University, Chengdu 610041, China
b.
West China School of Pharmacy, Sichuan University, Chengdu 610041, China

jzh-pharmacy@scu.edu.cn

songxr@scu.edu.cn

Received Date: 28 February 2019
Revised Date: 30 March 2019
Accepted Date: 1 April 2019
Available Online: 18 April 2019

Figures(5)

Nowadays, tremendous researches have been focused on the core-shell lipid-polymer nanoparticles (LPNs) due to the advantages of both liposomes and polymer nanoparticles. In this work, LPNs were applied to encapsulate brinzolamide (Brz-LPNs) for achieving sustained drug release, improving drug corneal permeation and enhancing drug topical therapeutic effect. The structure of Brz-LPNs was composed of poly(lactic-co-glycolic) acid (PLGA) nanocore which encapsulated Brz (Brz-NPs) and lipid shell around the core. Brz-LPNs were prepared by a modified thin-film dispersion method. With the parameters optimization of Brz-LPNs, optimal Brz-LPNs showed an average particle size of 151.23±1.64 nm with a high encapsulation efficiency (EE) of 86.7%±2.28%. The core-shell structure of Brz-LPNs were confirmed by transmission electronic microscopy (TEM). Fourier transformed infrared spectra (FTIR) analysis proved that Brz was successfully entrapped into Brz-LPNs. Brz-LPNs exhibited obvious sustained release of Brz, compared with AZOPT^® and Brz-LPs. Furthermore, the corneal accumulative permeability of Brz-LPNs significantly increased compared to the commercial available formulation (AZOPT^®) in vitro. Moreover, Brz-LPNs (1 mg/mL Brz) showed a more sustained and effective intraocular pressure (IOP) reduction than Brz-LPs (1 mg/mL) and AZOPT^® (10 mg/mL Brz) in vivo. In conclusion, Brz-LPNs, as promising ocular drug delivery systems, are well worth developing in the future for glaucoma treatment.
- Core-shell lipid-polymer nanoparticles,
- Ocular drug delivery system,
- Sustained release,
- Corneal permeation,
- Intraocular pressure
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