Advantages of introducing an effective crystalline inhibitor in curcumin amorphous solid dispersions formulated by Eudragit E100

J Pharm Pharmacol. 2021 Mar 4;73(2):185-192. doi: 10.1093/jpp/rgaa012.

Abstract

Objectives: This paper was to elucidate the advantages of using an effective crystalline inhibitor, which was hydroxypropyl methylcellulose E5 (HPMC), in inhibiting crystallisation for curcumin amorphous solid dispersion (Cur ASDs) formulated by Eudragit E100 (E100).

Methods: Physical characterisation such as differential scanning calorimetry and powder X-ray diffraction revealed the solid state during the formation of dispersion and clarified the compatibility between Cur and excipient.

Key findings: The liquidity of excipient and the change of Tg in Cur ASDs demonstrated that the addition of HPMC can reduce molecule motion of the whole system, improve Tg of Cur ASDs and inhibit crystallisation of Cur ASDs. The water uptake experiment and molecular dynamic modelling further confirmed the effective solution and matrix crystallisation inhibition role of HPMC.

Conclusions: The elucidation of HPMC as auxiliary excipient on inhibiting crystallisation for Cur ASDs will bring huge value in designing Cur ASDs in the future.

Keywords: crystallisation inhibition; curcumin amorphous solid dispersions; physical characterisation.

MeSH terms

  • Acrylates / chemistry*
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / chemistry
  • Calorimetry, Differential Scanning
  • Chemistry, Pharmaceutical
  • Crystallization
  • Curcumin / administration & dosage
  • Curcumin / chemistry*
  • Excipients / chemistry*
  • Hypromellose Derivatives / chemistry*
  • Polymers / chemistry*
  • X-Ray Diffraction

Substances

  • Acrylates
  • Antineoplastic Agents
  • Eudragit E100
  • Excipients
  • Polymers
  • Hypromellose Derivatives
  • Curcumin