Improvement on dissolution rate of inclusion complex of Rifabutin drug with β-cyclodextrin

Int J Biol Macromol. 2013 Nov:62:472-80. doi: 10.1016/j.ijbiomac.2013.09.006. Epub 2013 Sep 25.

Abstract

The effect of β-cyclodextrin (β-CD) on the improvement of solubility and antimicrobial activity of poorly water soluble drug Rifabutin (RFB) was studied. The solid inclusion complex is prepared under different methods and it is characterized by FT-IR, XRD, DSC and SEM methods. Solubility type, stability constant, stoichiometric ratio were investigated from phase solubility diagram of inclusion complex (RFB with β-CD). The dissolution profiles of the inclusion complexes were carried out and obvious increase in dissolution rate was observed when compared with pure RFB drug. Inclusion complexation process was further confirmed by molecular docking studies using PatchDock server. The in vitro antimicrobial and antibiofilm activity of RFB sensible microorganisms was significantly increased by on inclusion complexation process. This trend of inclusion complexation of poorly water soluble drugs is highly recognized as a successful and useful approach for the application in pharmaceutical field.

Keywords: Dissolution rate; Rifabutin; β-cyclodextrin.

MeSH terms

  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology
  • Calorimetry, Differential Scanning
  • Microbial Sensitivity Tests
  • Models, Molecular
  • Molecular Structure
  • Rifabutin / chemistry*
  • Rifabutin / pharmacology
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • X-Ray Diffraction
  • beta-Cyclodextrins / chemistry*

Substances

  • Anti-Bacterial Agents
  • beta-Cyclodextrins
  • Rifabutin
  • betadex