Controllable encapsulation of α-mangostin with quaternized β-cyclodextrin grafted chitosan using high shear mixing

Int J Pharm. 2018 Mar 1;538(1-2):21-29. doi: 10.1016/j.ijpharm.2017.12.016. Epub 2017 Dec 8.

Abstract

In this study, the inclusion complex formation between α-mangostin and water-soluble quaternized β-CD grafted-chitosan (QCD-g-CS) was investigated. Inclusion complex formation with encapsulation efficiency (%EE) of 5, 15 and 75% can be varied using high speed homogenizer. Tuning %EE plays a role on physicochemical and biological properties of α-mangostin/QCD-g-CS complex. Molecular dynamics simulations indicate that α-mangostin is included within the hydrophobic β-CD cavity and being absorbed on the QCD-g-CS surface, with these results being confirmed by Fourier transform infrared (FTIR) spectroscopy. Probing the release characteristics of the inclusion complex at various %EE (5%, 15% and 75%) in simulated saliva (pH 6.8) demonstrated that α-mangostin release rates were dependent on % EE (order 5% > 15% > 75%). Additionally, higher antimicrobial and anti-inflammation activities were observed for the inclusion complex than those of free α-mangostin due to enhance the solubility of α-mangostin through the inclusion complex with QCD-g-CS.

Keywords: Anti-inflammation; Antimicrobial; Chitosan; Effective entrapment; Inclusion complex; α-mangostin; β-CD.

Publication types

  • Comparative Study

MeSH terms

  • Anti-Infective Agents / administration & dosage
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology
  • Cell Line
  • Chemistry, Pharmaceutical / methods*
  • Chitosan / chemistry*
  • Drug Carriers / chemistry
  • Drug Liberation
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Molecular Dynamics Simulation
  • Saliva / metabolism
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • Water / chemistry
  • Xanthones / administration & dosage*
  • Xanthones / chemistry
  • Xanthones / pharmacology
  • beta-Cyclodextrins / chemistry*

Substances

  • Anti-Infective Agents
  • Anti-Inflammatory Agents
  • Drug Carriers
  • Xanthones
  • beta-Cyclodextrins
  • Water
  • Chitosan
  • betadex
  • mangostin