Atorvastatin calcium inclusion complexation with polysaccharide arabinogalactan and saponin disodium glycyrrhizate for increasing of solubility and bioavailability

Ruiping Kong, Xingyi Zhu, Elizaveta S. Meteleva, Nikolay E. Polyakov, Mikhail V. Khvostov, Dmitry S. Baev, Tatjana G. Tolstikova, Alexander V. Dushkin, Weike Su

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)

Abstract

The aim of the present investigation was to enhance the solubility and dissolution of atorvastatin calcium (ATV), a poorly water-soluble drug with larch polysaccharide arabinogalactan (AG) and disodium glycyrrhizate (Na2GA) as carriers of drug delivery systems for improving its bioavailability. The interactions of ATV with AG or Na2GA were investigated by DSC, XRD, SEM, and NMR techniques. The molecular weights of supramolecular systems—inclusion complexes and micelles—which are the hosts for ATV molecules were measured. On the other hand, the rapid storage assay (+ 40 °C for 3 months) showed that the chemical stability of ATV/AG and ATV/Na2GA complexes had been enhanced compared with pure ATV. In vitro drug release showed a significant increase in ATV’s dissolution rate after formation of a complex with Na2GA or AG. Pharmacokinetic tests in vivo on laboratory animals showed a significant increase in ATV’s bioavailability after its introduction as a complex with Na2GA or AG. Moreover, ATV/AG and ATV/Na2GA complexes showed a more prominent decrease of total cholesterol (TC) level compared to net ATV. Therefore, the novel mechanochemically synthesized complexes of ATV with AG or Na2GA as drug delivery systems might be potential and promising candidates for hypercholesterolemia treatment and deserved further researches.

Original languageEnglish
Pages (from-to)1200-1213
Number of pages14
JournalDrug Delivery and Translational Research
Volume8
Issue number5
DOIs
Publication statusPublished - 1 Oct 2018

Keywords

  • Arabinogalactan
  • Atorvastatin calcium
  • Disodium glycyrrhizin
  • Mechanochemistry
  • Solubility
  • Supramolecular complexes
  • ACID MICELLES
  • ENHANCED BIOAVAILABILITY
  • MECHANOCHEMICAL PREPARATION
  • SOLUBLE INTERMOLECULAR COMPLEXES
  • PHYSICOCHEMICAL PROPERTIES
  • SOLID DISPERSIONS
  • ORAL BIOAVAILABILITY
  • BETA-CYCLODEXTRIN
  • IN-VIVO EVALUATION
  • DISSOLUTION RATE

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