Development of in situ thermosensitive drug vehicles for glaucoma therapy.
The goal of this research was to design thermosensitive drug vehicles for glaucoma therapy. Thermosensitive ophthalmic drop was prepared by mixing linear poly(N-isopropylacrylamide-g-2-hydroxyethyl methacrylate) (PNIPAAm-g-PHEMA), PNIPAAm-g-PHEMA gel particles and antiglaucoma drug. This produced polymeric eyedrop containing the drug epinephrine was a clear solution at room temperature which became a soft film after contacting the surface of cornea. The drug entrapped within the tangled polymer chains was therefore released progressively after topical application. Evaluation of the drug release responded as a function of crosslinking density and PHEMA macromer contents. The in vivo studies indicated that the intraocular pressure (IOP)-lowering effect for a polymeric eyedrop lasted for 26 h, which is significantly better than the effect of traditional eyedrop (8 h). Hence our investigations successfully prove that the thermosensitive polymeric eyedrop with ability of controlled drug release exhibits a greater potential for glaucoma therapy.
Hsiue
Ging-Ho
GH
Department of Chemical Engineering, National Tsing Hua University, Hsinchu 300, Taiwan. ghhsiue@che.nthu.edu.tw
Chang
Ru-Wen
RW
Wang
Chau-Hui
CH
Lee
Shih-Huang
SH
D000180:Acrylic Resins / Q000737:chemistry; D000818:Animals; D002478:Cells, Cultured; D003315:Cornea / Q000187:drug effects*; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry; D004058:Diffusion; D004837:Epinephrine / Q000008:administration & dosage*; D005260:Female; D005901:Glaucoma / Q000188:drug therapy*; D006358:Hot Temperature; D007429:Intraocular Pressure / Q000187:drug effects; D008863:Microspheres; D009883:Ophthalmic Solutions / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry / Q000528:radiation effects; D014677:Pharmaceutical Vehicles / Q000138:chemical synthesis* / Q000737:chemistry / Q000528:radiation effects*; D011102:Polyhydroxyethyl Methacrylate / Q000737:chemistry; D011817:Rabbits
D000180:Acrylic Resins; D003692:Delayed-Action Preparations; D009883:Ophthalmic Solutions; D014677:Pharmaceutical Vehicles; C052970:poly-N-isopropylacrylamide; D011102:Polyhydroxyethyl Methacrylate; D004837:Epinephrine