Vesicular phospholipid gels as topical ocular delivery system for treatment of anterior uveitis.

In this paper, we developed a vesicular phospholipid gels (VPGs) for topical ocular delivery of flurbiprofen (FLB) to treat anterior uveitis. FLB loaded VPGs (FLB VPGs), composed of FLB and egg yolk lecithin, were prepared by high-pressure homogenization technique. The effects of egg yolk lecithin content and homogenization pressure on properties of FLB VPGs, including size, encapsulation efficiency, yield and in vitro release profile were investigated. The resultant FLB VPGs were characterized by the transmission electron microscopy, differential scanning calorimetry, X-ray diffraction, fourier transform infrared spectroscopy, rheological behavior, and storage stability. Corneal permeation experiments revealed that VPGs could improve the transcorneal delivery of FLB under ex vivo conditions. VPGs were nonirritant toward to the rabbit eye, as indicated by slit lamp observation and histological observation. The results of tear pharmacokinetics and in vivo fluorescence imaging showed that VPGs could significantly prolong the precorneal retention time. In vivo biodistribution study indicated that VPGs could significantly improve drug bioavailability in ocular tissues. Moreover, FLB VPGs exhibited excellent anti-inflammatory effect in endotoxin induced uveitis in rabbits. Overall, VPGs are a promising ophthalmic drug delivery system for the treatment of anterior uveitis. The vesicular phospholipid gels showed prolonged precorneal retention time, and increased ocular bioavailability, as well as enhanced anti-inflammatory effect in rabbit model of anterior uveitis. [Display omitted] • FLB VPGs were prepared by high-pressure homogenization technique. • FLB VPGs significantly prolonged precorneal retention time. • FLB VPGs significantly increased drug bioavailability in the ocular tissues. • FLB VPGs exhibited excellent anti-inflammatory effect in rabbit model of anterior uveitis. [ABSTRACT FROM AUTHOR]