Comparative permeability studies with radioactive and nonradioactive risedronate sodium from self-microemulsifying drug delivery system and solution

Drug Dev Ind Pharm. 2015;41(9):1493-8. doi: 10.3109/03639045.2014.959022. Epub 2015 Jul 21.

Abstract

The purpose of this work is to prepare a self-microemulsifying drug delivery system (SMEDDS) for risedronate sodium (RSD) and to compare the permeability with RSD solution. The solubility of RSD was determined in different vehicles. Phase diagrams were constructed to determine the optimum concentration of oil, surfactant, and cosurfactant. RSD SMEDDS was prepared by using a mixture of soybean oil, cremophor EL, span 80, and transcutol (2.02:7.72:23.27:61.74, w/w, respectively). The prepared RSD SMEDDS was characterized by droplet size value. In vitro Caco-2 cell permeability studies were performed for SMEDDS and solution of radioactive ((99 m)Tc-labeled RSD) and nonradioactive RSD. The experimental results indicated that RSD SMEDDS has good stability and its droplet size is between 216.68 ± 3.79 and 225.26 ± 7.65 during stability time. In addition, RSD SMEDDS has higher permeability value than the RSD solution for both radioactive and nonradioactive experiments. The results illustrated the potential use of SMEDDS for delivery of poorly absorbed RSD.

Keywords: Cell culture; microemulsion; permeability; risedronate sodium; technetium-99 m.

Publication types

  • Comparative Study

MeSH terms

  • Bone Density Conservation Agents / administration & dosage*
  • Bone Density Conservation Agents / pharmacokinetics
  • Caco-2 Cells
  • Chemistry, Pharmaceutical / methods
  • Drug Delivery Systems*
  • Drug Stability
  • Emulsions
  • Excipients / chemistry*
  • Humans
  • Permeability
  • Pharmaceutical Solutions
  • Radiopharmaceuticals / chemistry
  • Risedronic Acid / administration & dosage*
  • Risedronic Acid / pharmacokinetics
  • Solubility
  • Soybean Oil / chemistry
  • Surface-Active Agents / chemistry
  • Technetium / chemistry

Substances

  • Bone Density Conservation Agents
  • Emulsions
  • Excipients
  • Pharmaceutical Solutions
  • Radiopharmaceuticals
  • Surface-Active Agents
  • Technetium
  • Soybean Oil
  • Risedronic Acid