Design of controlled-release formulation for ivermectin using silicone

Int J Pharm. 2003 Aug 11;261(1-2):9-19. doi: 10.1016/s0378-5173(03)00293-x.

Abstract

The purpose of this study was to design a formulation using silicone as carrier, so that release of ivermectin (IVM) can be controlled for a long period of time. The lateral side of a cylindrical matrix-type formulation composed of IVM and silicone was covered with silicone to obtain a covered-rod (CR) formulation. With this formulation, linear release of IVM was obtained. With addition of polyethylene glycol 4000 (PEG), release of IVM was accelerated. In a trial with subcutaneous administration to mice, blood concentration of IVM was maintained within one-order over a period of 3 months. The velocity of release of IVM from CR preparation depended on the change in solubility of IVM by additives, and in the case of a formulation with addition of desoxycholate sodium, linear in vitro release of IVM was observed over a period of 1 year.

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Anthelmintics / administration & dosage
  • Anthelmintics / chemistry*
  • Anthelmintics / pharmacokinetics
  • Chemistry, Pharmaceutical / methods
  • Delayed-Action Preparations
  • Deoxycholic Acid
  • Drug Carriers
  • Excipients
  • Ivermectin / administration & dosage
  • Ivermectin / chemistry*
  • Ivermectin / pharmacokinetics
  • Mice
  • Silicone Elastomers*
  • Solubility

Substances

  • Anthelmintics
  • Delayed-Action Preparations
  • Drug Carriers
  • Excipients
  • Silicone Elastomers
  • Deoxycholic Acid
  • Ivermectin