Abstract
Dry eye syndrome (DES) is one of the most common disorders of the eye for which combined treatment includes modification of the ocular environment and pathogenic therapies. Cyclosporine A (CsA), a immunosuppressive agent, has been demonstrated to be effective for the treatment of DES but is limited clinically by its low ocular bioavailability due to poor water solubility. In this paper, methoxy poly (ethylene glycol)-poly (lactide) polymer (mPEG-PLA) micelles were investigated as alternative vehicles for the solubilization and delivery of CsA to the eye. The in vitro stability indicated that CsA-loaded micellar lyophilized powder was stable for at least 3 months and the release profile showed a sustained release manner of CsA from micelles physically. In vivo ocular distribution studies demonstrated that the micellar formulations exhibited a 4.5-fold increase in retention effect at eyes compared with 0.05% CsA emulsion. In addition, the in vivo pharmacokinetics profile showed that the CsA-loaded micelles could enhance the retention time, achieving longer effect toward the DES. These studies proposed an effective micelle formulation as a novel ocular drug delivery system to improve solubility and bioavailability of ophthalmic CsA-controlled delivery.
Highlights
Dry eye syndrome (DES) is a multifactorial disease of the ocular surface with tear film abnormalities, resulting in tear film stability decrease, eye discomfort, inflammation and lesion of ocular surface (Lemp, 2007)
The in vitro release showed that Cyclosporine A (CsA) micelles had sustained and delayed release
The in vitro cytotoxicity study showed that mPEG-PLA blank micelles were nontoxic
Summary
Dry eye syndrome (DES) is a multifactorial disease of the ocular surface with tear film abnormalities, resulting in tear film stability decrease, eye discomfort, inflammation and lesion of ocular surface (Lemp, 2007). DES is one of the corneal diseases that cause blindness. Traditional treatments for DES are focused on increasing lubrication of the ocular surface with artificial tears (Wan et al, 2015). These therapies do not address the underlying ocular surface inflammation. A combination of symptomatic therapy, which includes modification of the ocular environment (by increasing humidity, occlusion of lacrimal canaliculi, or simulation of tears), and pathogenic treatments, including the use of antibacterial and anti-inflammatory agents (corticosteroids, antihistamines, tetracyclines and CsA), is currently recommended for DES therapy (Shoji et al, 2005; Kymionis et al, 2008; Moscovici et al, 2012)
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