Targeted oral peptide delivery using multi-unit particulates: Drug and permeation enhancer layering approach

Oral delivery of peptides is a challenge due to their instability and their limited transport and absorption characteristics within the gastrointestinal tract. In this work, we used layering techniques in a fluidized bed dryer to create a configuration in which the active peptide, permeation enhancers, and polymers are coated to control the release of the peptide.

Formulations were developed to disintegrate at pH values of 5.5 and 7.0. In addition, sustained-release or mucoadhesive polymers were coated to trigger release at a desired site in the gastrointestinal tract. Dissolution studies with a USP Type I (basket) apparatus confirmed the duration of release. Pharmacokinetic studies were performed in beagle dogs to evaluate bioavailability.

A high-disintegration pH was found to be advantageous in enhancing bioavailability. Continue onTargeted oral peptide delivery using multi-unit particulates

Article information: Puneet Tyagi, Ruchit Trivedi, Sergei Pechenov, Chandresh Patel, Jefferson Revell, Sarah Wills, Yue Huang, Anton I. Rosenbaum, J. Anand Subramony, Targeted oral peptide delivery using multi-unit particulates: Drug and permeation enhancer layering approach, Journal of Controlled Release, Volume 338, 2021. https://doi.org/10.1016/j.jconrel.2021.09.002.

Interested in a full webinar series on Multiparticulates? Then have a view here