4.4 Review

Challenges of peptide and protein drug delivery by oral route: Current strategies to improve the bioavailability

期刊

DRUG DEVELOPMENT RESEARCH
卷 82, 期 7, 页码 927-944

出版社

WILEY
DOI: 10.1002/ddr.21832

关键词

absorption; barriers; bioavailability; peptide and protein drug delivery; permeability

资金

  1. CSIR
  2. ICMR
  3. DBT (Govt. of India)
  4. CSIR (Govt. of India)
  5. CSIR-CDRI

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Advancements in biotechnology have greatly expanded the application of peptide and protein therapeutics for treating diseases, but their limited bioavailability and stability restricts their usage to parenteral administration. Research is currently focused on overcoming the barriers of oral delivery to improve stability and bioavailability.
Advancement in biotechnology provided a notable expansion of peptide and protein therapeutics, used as antigens, vaccines, hormones. It has a prodigious potential to treat a broad spectrum of diseases such as cancer, metabolic disorders, bone disorders, and so forth. Protein and peptide therapeutics are administered parenterally due to their poor bioavailability and stability, restricting their use. Hence, research focuses on the oral delivery of peptides and proteins for the ease of self-administration. In the present review, we first address the main obstacles in the oral delivery system in addition to approaches used to enhance the stability and bioavailability of peptide/protein. We describe the physiochemical parameters of the peptides and proteins influencing bioavailability in the systemic circulation. It encounters, many barriers affecting its stability, such as poor cellular membrane permeability at the GIT site, enzymatic degradation (various proteases), and first-pass hepatic metabolism. Then describe the current approaches to overcome the challenges mentioned above by the use of absorption enhancers or carriers, structural modification, formulation and advance technology.

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