Title:Circumventing the Gastrointestinal Barrier for Oral Delivery of
Therapeutic Proteins and Peptides (PPTS): Current Trends and Future
Trajectories
Volume: 21
Issue: 2
Author(s): Lily Ellysa Hashim, Akmal Hidayat Sabri, Malihah Athirah Mohamad, Qonita Kurnia Anjani, Mohd Faiz Mustaffa and Khuriah Abdul Hamid*
Affiliation:
- Department of Pharmaceutics, Department of Pharmacology and Pharmaceutical Chemistry, Faculty of Pharmacy,
Universiti Teknologi MARA (UiTM) Cawangan Selangor, 42300, Bandar Puncak Alam, Selangor, Malaysia
- Department of Pharmaceutics, Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), UiTM Cawangan
Selangor, 42300, Bandar Puncak Alam, Selangor, Malaysia
Keywords:
Proteins drugs, peptides, permeation enhancers, gastrointestinal tract, insulin, erythropoietin.
Abstract: Therapeutic proteins and peptides (PPTs) have become one of the most important biological
molecules for the management of many common and complex diseases due to their high specificity and
high bioactivity. However, these biomolecules are mainly given by the hypodermic injection, which
often leads to poor patient compliance due to the invasive nature of this route of administration. The
oral route has been considered the most convenient and patient-friendly route for drug delivery relative
to hypodermic injections. Despite the ease and simplicity conferred by oral administration, this drug
delivery route suffers rapid peptide degradation in gastric fluid and low intestinal uptake. In order to
circumvent these issues, several strategies, such as enzyme inhibitors, permeation enhancers, chemical
modification, mucoadhesive and stimuli-responsive polymers, and specialised particulate formulation
have been developed. Such strategies are designed with the aim of protecting PPTs from the harsh gastrointestinal
environment as well as providing a strategy to enhance the uptake of the therapeutic across
the gastrointestinal tract. This review aims to provide an overview of the current development in enteral
drug delivery strategies for PPTs. The design of these drug delivery systems in overcoming physical
and chemical barriers along the gastrointestinal tract while improving oral bioavailability will be highlighted
and discussed.