Acta Pharmaceutica Sinica B (Sep 2019)

Multifunctional oral delivery systems for enhanced bioavailability of therapeutic peptides/proteins

  • Ying Han,
  • Zhonggao Gao,
  • Liqing Chen,
  • Lin Kang,
  • Wei Huang,
  • Mingji Jin,
  • Qiming Wang,
  • You Han Bae

Journal volume & issue
Vol. 9, no. 5
pp. 902 – 922

Abstract

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In last few years, therapeutic peptides/proteins are rapidly growing in drug market considering their higher efficiency and lower toxicity than chemical drugs. However, the administration of therapeutic peptides/proteins is mainly limited in parenteral approach. Oral therapy which was hampered by harsh gastrointestinal environment and poorly penetrating epithelial barriers often results in low bioavailability (less than 1%–2%). Therefore, delivery systems that are rationally designed to overcome these challenges in gastrointestinal tract and ameliorate the oral bioavailability of therapeutic peptides/proteins are seriously promising. In this review, we summarized various multifunctional delivery systems, including lipid-based particles, polysaccharide-based particles, inorganic particles, and synthetic multifunctional particles that achieved effective oral delivery of therapeutic peptides/proteins. KEY WORDS: Multifunctional delivery systems, Oral, Bioavailability, Macromolecules, Peptides and proteins, Gastrointestinal environment, Epithelial barriers, Nanoparticles