Liposomes dispersed within a thermosensitive gel: a new dosage form for ocular delivery of oligonucleotides

Pharm Res. 1998 Sep;15(9):1364-9. doi: 10.1023/a:1011989202488.

Abstract

Purpose: The main goal of this study was to develop an ocular controlled release formulation of a model oligonucleotide (pdT16), contained within liposomes dispersed within a thermosensitive gel composed by poloxamer 407.

Methods: The influence of the poloxamer concentration 2% or 27% on the stability of the liposomes (PC: CHOL and PC: CHOL: PEG-DSPE) was investigated. The in vitro release profiles of pdT16 from various poloxamer formulations (free pdT16 dispersed within 20% and 27% poloxamer gels, pdT16 encapsulated within liposomes dispersed within 20% and 27% poloxamer gels) were realized using a membrane-free release model.

Results: The dispersion of liposomes within a dilute 2% poloxamer solution resulted in a great leakage of pdT16 from liposomes. However, the destabilization effect of poloxamer was reduced when higher concentration (27%) was used. Poloxamer dissolution was found to control the release process of pdT16, whereas the dispersion of liposomes within 27% poloxamer gel was shown to slow down the diffusion of pdT16 out from the gel.

Conclusions: The dispersion of liposomes within a 27% poloxamer gel presented an interesting system to control the release of a model oligonucleotide compare to a simple gel.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Drug Carriers
  • Drug Delivery Systems
  • Excipients*
  • HEPES
  • Humans
  • In Vitro Techniques
  • Liposomes
  • Models, Biological
  • Ocular Physiological Phenomena
  • Oligonucleotides, Antisense / administration & dosage*
  • Oligonucleotides, Antisense / chemistry
  • Ophthalmic Solutions*
  • Poloxamer*
  • Solubility

Substances

  • Drug Carriers
  • Excipients
  • Liposomes
  • Oligonucleotides, Antisense
  • Ophthalmic Solutions
  • Poloxamer
  • HEPES