Development of a stick-type transdermal eyelid delivery system of ketotifen fumarate for ophthalmic diseases.
A transdermal eyelid delivery system for treating ocular diseases (eye-stick) has been developed. Ketotifen fumarate (KT) was used as a model drug. An in vivo study using rabbits showed that the eye-stick device maintained a constant conjunctival concentration of the drug for an extended period of time, which was equivalent or higher than the therapeutic level following eye drop administration. Moreover, the conjunctival concentration after eye-stick application was well predicted using the physicochemical parameters, diffusion coefficient and partition coefficient, obtained from in vitro hairless mouse skin permeation experiments.
Kimura
Chiharu
C
College of Computer Science and Systems Engineering, Kyushu Institute of Technology, Kawazu, Lizuka, Fukuoka, Japan.
Tojo
Kakuji
K
D000279:Administration, Cutaneous; D000818:Animals; D003228:Conjunctiva / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D016503:Drug Delivery Systems / Q000295:instrumentation / Q000379:methods*; D005123:Eye / Q000187:drug effects; D005143:Eyelids / Q000187:drug effects*; D005260:Female; D007665:Ketotifen / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D008297:Male; D051379:Mice; D008812:Mice, Hairless; D023421:Models, Animal; D008954:Models, Biological; D009226:Myristates / Q000737:chemistry; D009924:Organ Culture Techniques; D011817:Rabbits; D012867:Skin / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D014885:Waxes / Q000737:chemistry
D009226:Myristates; D014885:Waxes; C008205:isopropyl myristate; C038228:beeswax; D007665:Ketotifen