Microemulsion topical delivery platform

摘要

Provided are pharmaceutical carriers based on oil-in-water microemulsions and methods of making same. Also provided are pharmaceutical compositions comprising a carrier of the invention and a lipophilic active pharmaceutical ingredient (API), as well as methods for making same. The pharmaceutical compositions are particularly suitable for use in formulating lipophilic APIs for topical administration to the eye. Specifically included are pharmaceutical compositions comprising fenofibrate or fenofibric acid as API. Also provided is a method of treating a disease of the posterior segment of the eye. Also provided is a pharmaceutical composition comprising a compound represented by;
formulated for topical administration to the eye.

主权项

1. A pharmaceutical carrier suitable for topical administration to the eye, comprising:
an oil-in-water microemulsion comprising (i) an oil selected from the group consisting of isopropyl myristate, isopropyl palmitate, and medium chain triglycerides; (ii) a pair of surfactants selected from the group consisting of two polysorbates, a polysorbate and propylene glycol, a polysorbate and glycerol, a polysorbate and 1,2,3-triacetoxypropane, polyethoxylated castor oil and 1,2,3-triacetoxypropane, and polyethoxylated castor oil and propylene glycol; and (iii) water, wherein: the water represents 50 to about 95 percent (w/w) of the pharmaceutical carrier; the oil and the pair of surfactants represent substantially all of the remainder of the pharmaceutical carrier; and the ratio of percent (w/w) the pair of surfactants to percent (w/w) the oil is at least about 10:1.