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Titolo:
Controlled release and ocular absorption of tilisolol utilizing ophthalmicinsert-incorporated lipophilic prodrugs
Autore:
Kawakami, S; Nishida, K; Mukai, T; Yamamura, K; Nakamura, J; Sakaeda, T; Nakashima, M; Sasaki, H;
Indirizzi:
Nagasaki Univ, Sch Pharmaceut Sci, Nagasaki 8528521, Japan Nagasaki Univ Nagasaki Japan 8528521 maceut Sci, Nagasaki 8528521, Japan Kobe Univ, Sch Med, Dept Hosp Pharm, Chuo Ku, Kobe, Hyogo 6500017, Japan Kobe Univ Kobe Hyogo Japan 6500017 m, Chuo Ku, Kobe, Hyogo 6500017, Japan Nagasaki Univ, Sch Med, Dept Hosp Pharm, Nagasaki 8528505, Japan Nagasaki Univ Nagasaki Japan 8528505 Hosp Pharm, Nagasaki 8528505, Japan
Titolo Testata:
JOURNAL OF CONTROLLED RELEASE
fascicolo: 3, volume: 76, anno: 2001,
pagine: 255 - 263
SICI:
0168-3659(20011019)76:3<255:CRAOAO>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
DRUG-DELIVERY SYSTEM; ALBINO RABBITS; BETA-BLOCKERS; TIMOLOL; PENETRATION; MEMBRANES; VEHICLE;
Keywords:
prodrugs; ophthalmic inserts; controlled released; tilisolol;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
29
Recensione:
Indirizzi per estratti:
Indirizzo: Kawakami, S Nagasaki Univ, Sch Pharmaceut Sci, 1-14 Bunkyo-machi, Nagasaki8528521, Japan Nagasaki Univ 1-14 Bunkyo-machi Nagasaki Japan 8528521 Japan
Citazione:
S. Kawakami et al., "Controlled release and ocular absorption of tilisolol utilizing ophthalmicinsert-incorporated lipophilic prodrugs", J CONTR REL, 76(3), 2001, pp. 255-263

Abstract

To control ocular drug delivery, the O-butyryl ester prodrug of tilisolol (BUTL) and the O-palmitoyl ester prodrug of tilisolol (PalTL) were incorporated into an ophthalmic insert. The released TL from BUTL inserts and PalTLinserts in pH 7.4 phosphate-buffered saline until 5 h were similar to 25% and 3% of that from TL inserts, respectively. In addition, BUTL was also released front BUTL inserts. However, PalTL was not released from the PalTL insert. The release of drugs from TL inserts and BUTL inserts was little affected by the addition of bovine serum albumin (BSA) in pH 7.4 phosphate-buffered saline. In contrast, the release of drugs from PalTL inserts were enhanced by the addition of BSA. After application of TL, BUTL, and PalTL inserts to the rabbit eye, the aqueous humor concentration of TL was prolonged compared with TL instillation, and the plasma concentration of TL was much lower than that of TL instillation. The ratios of the area under the TL concentration-time curve (AUC) in the aqueous humor to AUC in the plasma (AUC(aqueous)/AUC(plasma)) after application of BUTL until 8 h were 3.1-fold and3.8-fold higher than those of the TL insert and PalTL insert, respectively. (C) 2001 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 15/08/20 alle ore 19:20:31