Physostigmine emulsion: a new injectable controlled release delivery system

Simon Benita*, Doron Friedman, Marta Weinstock

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

40 Scopus citations

Abstract

Physostigmine salicylate was incorporated in a soybean injectable emulsion in an attempt to control the drug release from the emulsion. In vitro examination of the physicochemical properties of the emulsions revealed that a mixture of an anionic (phospholipid) and non-ionic surfactant (Pluronic) was required to prepare stable physostigmine emulsions. Variation in concentration of either the anionic or non-ionic emulsifier decreased the mean droplet size while the zeta potential did not show any clear correlation with increasing phospholipid concentration but decreased, reached a plateau and fell again with increasing Pluronic concentration. In the presence of physostigmine salicylate. instability was introduced which changed the profile of zeta potential dependency on phospholipids and Pluronic concentrations. Zeta potential increased with physostigmine concentration as a result of increasing ionization of various polar groups at the oil-water droplet interface. Moreover, physostigmine incorporated in the emulsion was protected from its aqueous decomposition and remained intact. Stable physostigmine emulsions preserved over long periods of time were obtained using appropriate experimental conditions probably as a result of optimization of effects due to surface potential increase, droplet size reduction and formation of a resistant close-packed interfacial mixed film. which confers steric stabilization to the dispersed droplets.

Original languageEnglish
Pages (from-to)47-55
Number of pages9
JournalInternational Journal of Pharmaceutics
Volume30
Issue number1
DOIs
StatePublished - May 1986

Keywords

  • physostigmine salicylate-injectable emulsion-controlled-release delivery system

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