Enhanced aqueous dissolution of hydrophobic apixaban via direct incorporation of hydrophilic nanographene oxide

Mohammad Saiful Islam, Faradae Renner, Kimberly Foster, Martins S. Oderinde, Kevin Stefanski, Somenath Mitra

Research output: Contribution to journalArticlepeer-review

4 Scopus citations

Abstract

In this study, we have directly incorporated nanographene oxide (nGO) into a hydrophobic drug for enhanced dissolution performance through an antisolvent technique. Apixaban (APX) drug composites were synthesized with nGO incorporation ranging from 0.8% to 2.0% concentration. It was observed that the nGO was successfully embedded without any changes to the original drug crystal structure or physical properties. Dissolution of the drug composites was evaluated using US Pharmacopeia Paddle Method (USP 42). The time needed to reach a 50% release (T50) reduced from 106 min to 24 min with the integration of 1.96% nGO in APX and the T80 also dropped accordingly. Alternatively, dissolution rate showed promising performance with increase in nGO concentration. Initial dissolution rate increased dramatically from 74 µg/min to 540 µg/min. Further, work done in intestinal media revealed T50 went from not dissolving to 79.0 min. Decreased lipophilicity or logP value and increased aqueous solubility are both accredited to hydrophilic nGO water dispersion, producing a hydrophilic channel into the drug crystal surfaces through intermolecular interaction. Additionally, physical, and chemical characterizations confirm that hydrophobic apixaban was successfully transformed into a hydrophilic composite, showing potential for this technology to improve dissolution rate of a model hydrophobic compound.

Original languageEnglish (US)
Article number112512
JournalColloids and Surfaces B: Biointerfaces
Volume216
DOIs
StatePublished - Aug 2022

All Science Journal Classification (ASJC) codes

  • Biotechnology
  • Surfaces and Interfaces
  • Physical and Theoretical Chemistry
  • Colloid and Surface Chemistry

Keywords

  • Bioavailability
  • Direct incorporation
  • Enhanced dissolution
  • Graphene oxide
  • Hydrophobic apixaban
  • Paddle method

Fingerprint

Dive into the research topics of 'Enhanced aqueous dissolution of hydrophobic apixaban via direct incorporation of hydrophilic nanographene oxide'. Together they form a unique fingerprint.

Cite this