Abstract
Novel ocular drug delivery systems (NODDSs) remain to be explored to overcome the anatomical and physiological barriers of the eyes. This study was to encapsulate brinzolamide (BRZ)-hydropropyl-β-cyclodextrin (HP-β-CD) inclusion complex (HP-β-CD/BRZ) into nanoliposomes and investigate its potential as one of NODDS to improve BRZ local glaucomatous therapeutic effect. HP-β-CD/BRZ was firstly prepared to enhance the solubility of poorly water-soluble BRZ. The HP-β-CD/BRZ loaded nanoliposomes (BCL) were subsequently constructed by thin-film dispersion method. After the optimization of the ratio of BRZ to HP-β-CD, the optimal BCL showed an average size of 82.29 ± 6.20 nm, ζ potential of -3.57 ± 0.46 mV and entrapment efficiency (EE) of 92.50 ± 2.10% with nearly spherical in shape. The X-ray diffraction (XRD) confirmed the formation of HP-β-CD/BRZ and BCL. The in vitro release study of BCL was evaluated using the dialysis technique, and BCL showed moderate sustained release. BCL (1 mg/mL BRZ) showed a 9.36-fold increase in the apparent permeability coefficient and had a sustained and enhanced intraocular pressure reduction efficacy when compared with the commercially available formulation (BRZ-Sus) (10 mg/mL BRZ). In conclusion, BCL might have a promising future as a NODDS for glaucoma treatment.
Highlights
Despite easy accessibility for topical drug administration, overcoming the anatomical and physiological barriers of the eye remains one of the greatest challenges for ocular drug delivery (Bucolo et al, 2012; Zhang et al, 2015)
LP/BRZ and BRZ. The HP-β-CD/BRZ loaded nanoliposomes (BCL) colloidal solution were observed as a slightly blue opalescence with obvious Tyndall effect compared with water (Figures 3E,F)
The spectrum of BCL exhibited a characteristics absorption peak at 252 nm, which was similar to the peak of BRZ. These results suggested that the HPLC method developed for BRZ measurement with a detection wavelength of 252 nm could be applied to determine the BRZ concentration in BCL
Summary
Despite easy accessibility for topical drug administration, overcoming the anatomical and physiological barriers of the eye remains one of the greatest challenges for ocular drug delivery (Bucolo et al, 2012; Zhang et al, 2015). Drug retention is impeded by tear reflex, blinking, and nasolacrimal drainage (Morrison et al, 2013). Cornea barrier protects the eye from the passage of any foreign molecules including drugs into the eye, and only a small fraction of the topically applied drug penetrates the cornea and reaches intraocular tissues (Mun et al, 2014). A system which behaves like a solution and at the same time can lead to retention of drug in the eye and increase corneal permeability is of great urgency.
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