Investigation of the Drug Carrier Properties of Insoluble Cyclodextrin Polymer Microspheres

Biomolecules. 2022 Jul 2;12(7):931. doi: 10.3390/biom12070931.

Abstract

The investigation of the usability of solid insoluble β-cyclodextrin polymers (βCDP) in micro-sized, controlled drug delivery systems has only recently attracted interest. Our aim was to form complexes with poorly soluble active pharmaceutical ingredients (APIs) with two types of βCDP for drug delivery applications. Solid insoluble cyclodextrin polymer of irregular shape (βCDPIS) and cyclodextrin microbeads (βCDPB) were used in the experiments. Morphology, surface area, size distribution and swelling capacity of carriers were investigated. We created complexes with two APIs, curcumin and estradiol, and applied powder X-ray diffraction, FTIR and thermal analysis (TGA/DSC) to prove the complexation. Finally, the dissolution, biocompatibility and permeation of APIs on Caco-2 cells were investigated. The size of the beads was larger than 100 µm, their shape was spherical and surfaces were smooth; while the βCDPIS particles were around 4 µm with irregular shape and surface. None of the polymers showed any cytotoxic effect on Caco-2 cells. Both carriers were able to extract curcumin and estradiol from aqueous solutions, and the dissolution test showed prolonged estradiol release. Caco-2 permeability tests were in accordance with the complexation abilities and dissolution of the complexes. This study offers useful data for further pharmaceutical applications of insoluble cyclodextrin polymers.

Keywords: complexation; curcumin; cyclodextrin beads; drug delivery; estradiol-glow; insoluble cyclodextrin polymer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Caco-2 Cells
  • Cellulose
  • Curcumin* / pharmacology
  • Cyclodextrins*
  • Drug Carriers
  • Estradiol
  • Humans
  • Microspheres
  • Polymers
  • Solubility

Substances

  • Cyclodextrins
  • Drug Carriers
  • Polymers
  • cyclodextrin polymer
  • Estradiol
  • Cellulose
  • Curcumin

Grants and funding

Project no. TKP2021-EGA-18 has been implemented with the support provided from the National Research, Development and Innovation Fund of Hungary, financed under the TKP2021-EGA funding scheme. The project was supported by the EFOP-3.6.3-VEKOP-16-2017-00009 project, co-financed by EU and the European Social Fund. The powder X-ray diffraction was co-financed by the European Regional Development Fund under the project GINOP-2.3.3-15-2016-00004. Synthesis of insoluble CD polymers was financed by University of Turin, Turin, Italy (Fondi Ricerca Locale 2020).