One-side-coated insert as a unique ophthalmic drug delivery system.
We newly prepared a unique one-side-coated insert that releases drug from only uncoated side. The purpose of this study is to determine whether ocular and systemic absorption of ophthalmic drug could be altered by an inserting direction of the insert in rabbit eyes. One-side-coated insert was prepared by attaching a polypropylene tape on the one side of the polymer disc of poly(2-hydroxypropyl methacrylate) (HPM) containing tilisolol as a model ophthalmic drug. The insert was applied in the lower conjunctival cul-de-sac of albino rabbits with the uncoated side facing bulbar conjunctiva/sclera (SC insert) or palpebral conjunctiva (CJ insert). At the adequate intervals, the tear fluid, plasma, aqueous humor, conjunctiva, and sclera were collected and the drug concentrations were determined by an HPLC. A release of tilisolol from the one-side-coated insert was twice slower than from the uncoated insert. Ocular application of the one-side-coated insert produced the constant concentrations of tilisolol in the tear fluid over 180 min. SC insert showed higher drug concentrations in the aqueous humor and sclera, and lower drug concentrations in the plasma and conjunctiva than CJ insert.The one-side-coated insert can alter the ocular and systemic absorption of drug by an inserting direction.
Sasaki
Hitoshi
H
Department of Hospital Pharmacy, Nagasaki University School of Medicine, 1-7-1 Sakamoto, Nagasaki 852-8501, Japan. sasaki@net.nagasaki-u.ac.jp
Nagano
Toshiaki
T
Sakanaka
Koji
K
Kawakami
Shigeru
S
Nishida
Koyo
K
Nakamura
Junzo
J
Ichikawa
Nobuhiro
N
Iwashita
Junji
J
Nakamura
Tadahiro
T
Nakashima
Mikiro
M
D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D000818:Animals; D001082:Aqueous Humor / Q000378:metabolism; D019540:Area Under Curve; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D003228:Conjunctiva / Q000378:metabolism; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D016503:Drug Delivery Systems / Q000295:instrumentation / Q000379:methods*; D005123:Eye / Q000378:metabolism*; D007546:Isoquinolines / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D008297:Male; D011109:Polymethacrylic Acids / Q000737:chemistry; D011817:Rabbits; D012590:Sclera / Q000378:metabolism; D013666:Tears / Q000378:metabolism
D000319:Adrenergic beta-Antagonists; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D007546:Isoquinolines; D011109:Polymethacrylic Acids; C011533:Duxon; C036593:tilisolol