Core-shell lipid-polymer nanoparticles as a promising ocular drug delivery system to treat glaucoma |
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Authors: | Yang Zhou Aiping Fang Fazhan Wang Huili Li Quansheng Jin Lingjing Huang Chunmei Fu Jun Zeng Zhaohui Jin Xiangrong Song |
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Institution: | 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; West China School of Pharmacy, Sichuan University, Chengdu 610041, China |
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Abstract: | 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. |
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Keywords: | Core-shell lipid-polymer nanoparticles Ocular drug delivery system Sustained release Corneal permeation Intraocular pressure |
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