Dissolution enhancement of active pharmaceutical ingredients by therapeutic deep eutectic systems

Ivo M Aroso, João C Silva, Francisca Mano, Ana Sofia Diogo Ferreira, Madalena Dionísio, Isabel Sá-Nogueira, Susana Barreiros, Rui L Reis, Alexandre Paiva, Ana Rita C Duarte

Research output: Contribution to journalArticle

52 Citations (Scopus)

Abstract

A therapeutic deep eutectic system (THEDES) is here defined as a deep eutectic solvent (DES) having an active pharmaceutical ingredient (API) as one of the components. In this work, THEDESs are proposed as enhanced transporters and delivery vehicles for bioactive molecules. THEDESs based on choline chloride (ChCl) or menthol conjugated with three different APIs, namely acetylsalicylic acid (AA), benzoic acid (BA) and phenylacetic acid (PA), were synthesized and characterized for thermal behaviour, structural features, dissolution rate and antibacterial activity. Differential scanning calorimetry and polarized optical microscopy showed that ChCl:PA (1:1), ChCl:AA (1:1), menthol:AA (3:1), menthol:BA (3:1), menthol:PA (2:1) and menthol:PA (3:1) were liquid at room temperature. Dissolution studies in PBS led to increased dissolution rates for the APIs when in the form of THEDES, compared to the API alone. The increase in dissolution rate was particularly noticeable for menthol-based THEDES. Antibacterial activity was assessed using both Gram-positive and Gram-negative model organisms. The results show that all the THEDESs retain the antibacterial activity of the API. Overall, our results highlight the great potential of THEDES as dissolution enhancers in the development of novel and more effective drug delivery systems.

Original languageEnglish
Pages (from-to)57-66
Number of pages10
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume98
DOIs
Publication statusPublished - Jan 2016

Keywords

  • Pharmacology & Pharmacy
  • Research Support, Non-U.S. Gov't
  • Therapeutic deep eutectic systems
  • Drug solubility
  • Green technologies
  • Pharmaceutical and biomedical applications

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