Ocular permeability of pirenzepine hydrochloride enhanced by methoxy poly(ethylene glycol)-poly(D, L-lactide) block copolymer.
Drug Dev Ind Pharm
; 33(10): 1142-50, 2007 Oct.
Article
en En
| MEDLINE
| ID: mdl-17852364
ABSTRACT
Methoxy poly(ethylene glycol)-poly(D, L-lactide) block copolymer was tested as an ocular permeation enhancer for pirenzepine hydrochloride. The block copolymers with the methoxy poly(ethylene glycol) to poly(D, L-lactide) weight ratio of 80/20, 50/50, 40/60 were synthesized by a ring-opening polymerization procedure. In vitro transcorneal experiments demonstrated that the block copolymer 80/20 significantly enhanced the transcorneal permeation of pirenzepine at the mass ratio of 1/1.4 (pirenzepine hydrochloride/copolymer). Interaction between pirenzepine and copolymer was identified by infrared spectroscopy analysis and dialysis experiments. Ocular pharmacokinetics of pirenzepine/copolymer preparation by in vivo instillation experiments confirmed that block copolymer could enhance the ocular penetration of pirenzepine. Ocular chronic toxicity experiments of block copolymer and pirenzepine/copolymer preparation were studied on rabbits, and no significant toxicity in both groups was observed within 9 months. It could conclude that pirenzepine/copolymer preparation is effective and safe in ocular delivery of pirenzepine.
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Banco de datos:
MEDLINE
Asunto principal:
Poliésteres
/
Polietilenglicoles
/
Pirenzepina
/
Córnea
Límite:
Animals
Idioma:
En
Revista:
Drug Dev Ind Pharm
Año:
2007
Tipo del documento:
Article