Design and evaluation of a liposomal delivery system targeting the posterior segment of the eye.
The purpose of this study was to evaluate the potential of submicron-sized liposomes (ssLips) as a novel system for delivering ocular drugs to the eye's posterior segment. Fluorescence emission of coumarin-6 formulated into ssLip was obvious in that segment in mice after eyedrop administration of the liposomal suspension. Such fluorescence was not observed after administration of either multilamellar vesicles or dimethyl sulfoxide (DMSO) solution containing the same amount of coumarin-6. The highest fluorescence of ssLip occurred 30 min after eyedrop administration, and all fluorescence disappeared after 180 min. The ssLip based on l-alpha-distearoyl phosphatidylcholine (DSPC ssLip) showed higher fluorescence emission in the retina than that based on egg phosphatidylcholine (EPC ssLip). These results confirmed that the magnitude of fluorescence in the retina was closely related to both liposome rigidity and particle size. Images of the entire eye showed that ssLip was delivered via the non-corneal pathway after administration. The liposomes tested in ocular cells showed little cytotoxicity. These results suggest that ssLip can be used to deliver drugs to the posterior segment of the eye.
Hironaka
Kohei
K
Laboratory of Pharmaceutical Engineering, Gifu Pharmaceutical University, Japan.
Inokuchi
Yuta
Y
Tozuka
Yuichi
Y
Shimazawa
Masamitsu
M
Hara
Hideaki
H
Takeuchi
Hirofumi
H
D000818:Animals; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002645:Chickens; D003228:Conjunctiva / Q000166:cytology; D003315:Cornea / Q000166:cytology; D003374:Coumarins; D005123:Eye / Q000378:metabolism; D005456:Fluorescent Dyes; D006801:Humans; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics* / Q000633:toxicity*; D008297:Male; D051379:Mice; D018625:Microscopy, Atomic Force; D008856:Microscopy, Fluorescence; D009883:Ophthalmic Solutions / Q000008:administration & dosage; D010063:Ovum / Q000737:chemistry; D010316:Particle Size; D010713:Phosphatidylcholines / Q000737:chemistry*; D012160:Retina / Q000378:metabolism*; D013844:Thiazoles
D003374:Coumarins; D005456:Fluorescent Dyes; D008081:Liposomes; D009883:Ophthalmic Solutions; D010713:Phosphatidylcholines; D013844:Thiazoles; C517282:coumarin 6; C010942:1,2-distearoyllecithin