Hydrophobic ion pairing-based self-emulsifying drug delivery systems: a new strategy for improving the therapeutic efficacy of water-soluble drugs

Expert Opin Drug Deliv. 2023 Jan;20(1):1-11. doi: 10.1080/17425247.2023.2150758. Epub 2022 Nov 29.

Abstract

Introduction: Self-emulsifying drug delivery systems (SEDDS) are formulations consisting of oil phase, emulsifiers, and co-emulsifiers, which can be spontaneously emulsified in the body to form O/W microemulsion. Traditionally, SEDDS are used commercially for the improvement of oral absorption and in vivo performances for poorly water-soluble drugs. However, SEDDS formulations were rarely reported for the delivery of water-soluble drugs. Recent studies have found that SEDDS have the potential for water-soluble macromolecular drugs by the application of the hydrophobic ion pairing (HIP) technology.

Areas covered: This review summarized the characteristics of HIP complexes in SEDDS and introduced their advantages and discussed the future prospects of HIP-based SEDDS in drug delivery.

Expert opinion: Hydrophobic ion pairing (HIP) is a technology that combines lipophilic structures on polar counterions to increase the lipophilicity through electrostatic interaction. Recent studies showed that HIP-based SEDDS offer an effective way to increase the mucosal permeability and improve the chemical stability for antibiotics, proteases, DNA-based drugs, and other water-soluble macromolecular drugs. It is believed that HIP-based SEDDS offer a potential and attractive method capable of delivering hydrophilic macromolecules with ionizable groups for oral administration.

Keywords: Self-emulsifying drug delivery systems; hydrophilic macromolecules; hydrophobic ion pairing; oral administration.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Anti-Bacterial Agents*
  • Drug Delivery Systems* / methods
  • Emulsions
  • Hydrophobic and Hydrophilic Interactions
  • Macromolecular Substances
  • Solubility

Substances

  • Emulsions
  • Anti-Bacterial Agents
  • Macromolecular Substances