title: Targeting of gastrointestinal tract for amended delivery of protein/peptide therapeutics: strategies and industrial perspectives.
abstract: Delivery of proteins/peptides to the gastrointestinal (GI) tract via peroral/oral route involves tremendous challenges due to unfavorable environmental conditions like harsh pH, presence of proteolytic enzymes and absorption barriers. Detailed research is being conducted at the academic and industrial levels to diminish these troubles and various products are under clinical trials. Several approaches have been established to optimize oral delivery of proteins and peptides and can be broadly categorized into chemical and physical strategies. Chemical strategies include site specific mutagenesis, proteinylation, glycosylation, PEGylation and prodrug approaches, whereas physical strategies comprise formulation based approaches including application of absorption enhancers and metabolism modifiers along with delivering them via colloidal carrier systems such as nanoparticles, liposomes, microparticles, and micro- and nano-emulsions. This review stands to accomplish the diverse aspects of oral delivery of proteins/peptides and summarizes the key concepts involved in targeting the biodrugs to specific sites of the GI tract such as the intestine and colon. Furthermore some light has also been shed on the current industrial practices followed in developing oral formulations of such bioactives.
authors.affiliation: Pharmaceutics Division, CSIR-Central Drug Research Institute, Lucknow, UP 226031, India.
authors.forename: Vivek K
authors.initials: VK
authors.lastname: Pawar
authors.affiliation: Pharmaceutics Division, CSIR-Central Drug Research Institute, Lucknow, UP 226031, India.
authors.forename: Jaya Gopal
authors.initials: JG
authors.lastname: Meher
authors.affiliation: Pharmaceutics Division, CSIR-Central Drug Research Institute, Lucknow, UP 226031, India.
authors.forename: Yuvraj
authors.initials: Y
authors.lastname: Singh
authors.affiliation: Amity Institute of Pharmacy, Amity University, Lucknow, UP 226028, India.
authors.forename: Mohini
authors.initials: M
authors.lastname: Chaurasia
authors.affiliation: Division of Natural Products Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad, AP 500007, India.
authors.forename: B
authors.initials: B
authors.lastname: Surendar Reddy
authors.affiliation: Pharmaceutics Division, CSIR-Central Drug Research Institute, Lucknow, UP 226031, India. Electronic address: manish_chourasia@cdri.res.in.
authors.forename: Manish K
authors.initials: MK
authors.lastname: Chourasia
mesh_terms: D000818:Animals; D001693:Biological Transport, Active; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D005767:Gastrointestinal Diseases / Q000188:drug therapy*; D041981:Gastrointestinal Tract / Q000378:metabolism*; D006801:Humans; D010455:Peptides / Q000008:administration & dosage* / Q000627:therapeutic use*; D011506:Proteins / Q000008:administration & dosage* / Q000627:therapeutic use*
chemical_list: D010455:Peptides; D011506:Proteins
keywords: Gastrointestinal barriers; Oral delivery; Peptide; Proteins; Targeted delivery; Transport pathways