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Scientific article
English

A poly(ortho ester) designed for combined ocular delivery of dexamethasone sodium phosphate and 5-fluorouracil: subconjunctival tolerance and in vitro release

Published inEuropean journal of pharmaceutics and biopharmaceutics, vol. 50, no. 2, p. 251-255
Publication date2000
Abstract

A viscous hydrophobic poly(ortho ester) (POE) has been developed as a biocompatible, biodegradable sustained release system for selected cases of glaucoma filtering surgery. Dexamethasone and 5-fluorouracil (5-FU) are frequently administered together post-operatively, for their anti-fibroblastic and anti-inflammatory properties, respectively. A combined sustained release of both drugs could be advantageously used. Drug release kinetics were studied using specially designed thermostated cells. Subconjunctival tolerance was evaluated on New Zealand albino rabbits by clinical evaluation. Due to its basicity, the addition of dexamethasone sodium phosphate (DEX-P) stabilized the polymer and prolonged 5-FU in vitro release from 2 to 4 days. Both therapeutic agents were released concomitantly, according to a linear profile. The presence of 5-FU only slightly affected the overall subconjunctival tolerance of POE in rabbits, whereas the addition of DEX-P markedly improved POE tolerance by reducing the hyperemia of the conjunctiva to a minimal grade.

Keywords
  • Animals
  • Biocompatible Materials/administration & dosage
  • Conjunctiva/metabolism
  • Delayed-Action Preparations
  • Dexamethasone/administration & dosage/analogs & derivatives/chemistry/pharmacokinetics
  • Drug Carriers
  • Eye/metabolism
  • Fluorouracil/administration & dosage/chemistry/pharmacokinetics
  • Hydrogen-Ion Concentration
  • Polymers/administration & dosage/pharmacokinetics
  • Rabbits
  • Solubility
Citation (ISO format)
ZIGNANI, Monia et al. A poly(ortho ester) designed for combined ocular delivery of dexamethasone sodium phosphate and 5-fluorouracil: subconjunctival tolerance and in vitro release. In: European journal of pharmaceutics and biopharmaceutics, 2000, vol. 50, n° 2, p. 251–255. doi: 10.1016/S0939-6411(00)00107-7
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ISSN of the journal0939-6411
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