Ocular penetration enhancers limitations

The conventional concentration of benzalkonium chloride in eyedrops is 0.01%, with a range of 0.004-0.02% [111]. While uptake of benzalkonium chloride itself into ocular tissues is limited [113], even lower concentrations of benzalkonium chloride have been reported to enhance corneal penetration of other compounds including therapeutic agents [93,112,114]. The differential effect of this preservative on the cornea compared to the conjunctiva can be exploited to target a drug for corneal absorption and delivery to the posterior segment of the eye [115]. Its use has been proposed as a means of delivering systemic doses by an ocular route of administration [116]. 

Niosomes In order to circumvent some of the limitations encountered with liposomes, such as their chemical instability, the cost and purity of the natural phospholipids, and oxidative degradation of the phospholipids, niosomes have been developed. Niosomes are nonionic surfactant vesicles which exhibit the same bilay-ered structures as liposomes. Their advantages over liposomes include improved chemical stability and low production costs. Moreover, niosomes are biocompatible, biodegradable, and nonimmunogenic [215], They were also shown to increase the ocular bioavailability of hydrophilic drugs significantly more than liposomes. This is due to the fact that the surfactants in the niosomes act as penetrations enhancers and remove the mucous layer from the ocular surface [209]. 

Penetration Enhancers The transport process across the corneal tissue is the rate-limiting step in ocular drug absorption. Increasing the permeability of the corneal epithelium by penetration enhancers is likely to enhance the drug transport across the corneal tissues and therefore improve ocular bioavailability of the drug. 

Gels The use of high-viscosity, water-soluble gel as a drug vehicle will prolong the therapeutic effect and enhance ocular penetration, reducing the frequency of application. However, only a limited number of dmgs are available as gel preparations (e.g. fusidic acid) and their use in equine practice is limited. 

---