Abstract
Eye drops are ophthalmic formulations routinely used to treat dry eye. However, the low ocular bioavailability is an obvious drawback of eye drops owing to short ocular retention time and weak permeability of the cornea. Herein, to improve the ocular bioavailability of eye drops, a cationic liposome eye drop was constructed and used to treat dry eye. Tacrolimus liposomes exhibit a diameter of around 300 nm and a surface charge of +30 mV. Cationic liposomes could interact with the anionic ocular surface, extending the ocular retention time and improving tacrolimus amount into the cornea. The cationic liposomes notably prolonged the ocular retention time of eye drops, leading to an increased tacrolimus concentration in the ocular surface. The tacrolimus liposomes were also demonstrated to reduce reactive oxygen species and dry eye–related inflammation factors. The use of drug-loaded cationic liposomes is a good formulation in the treatment of ocular disease; the improved ocular retention time and biocompatibility give tremendous scope for application in the treatment of ocular disease, with further work in the area recommended.
Highlights
Eye drops are pretty restricted by low ocular bioavailability
The chemicals and solvents used for mass spectrum–highperformance liquid chromatography (MS-HPLC) and HPLC were of HPLC grade, while the others were of analytical grade
The entrapment efficiency of the FK506 liposomes was 90.11 ± 2.87%, and the FK506 loading level was around 9.07 ± 0.03%
Summary
Eye drops are pretty restricted by low ocular bioavailability. Despite this, many clinicians prefer topical ophthalmic solutions to other treatment options as eye drops are accessible and noninvasive, and this formulation accounts for nearly 90% of ophthalmic drugs (Weng et al, 2018; Jain et al, 2019). The structure of the ocular surface comprises the adnexa, tear film, lacrimal gland, meibomian glands, cornea, conjunctiva, and eyelids (Craig et al, 2017). It protects the eyes from bacteria and chemicals, becoming an obstacle to drug permeability. The blink reflex and tear turnover rate are the main contributing factors to a short ocular retention time (Chhonker et al, 2015). To remedy this problem, eye drops need to be frequently used to improve the therapeutic effect. The requirement of multiple administrations, in turn, may cause patients to become noncompliant
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