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Updated: Jul 12, 2025
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Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
Published on: September 20, 2017
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Systems Biology and Peptide Engineering to Overcome Absorption Barriers for Oral Peptide Delivery: Dosage Form
Puneet Tyagi1, Chandresh Patel1, Kimberly Gibson2
1Dosage Form Design and Development, BioPharmaceuticals R&D, AstraZeneca, Gaithersburg, MD 20878, USA.
Pharmaceutics
|October 28, 2023
Summary
Developing oral peptide formulations like MEDI7219 with permeation enhancers (sodium chenodeoxycholate and propyl gallate) achieved significant oral bioavailability in dogs, offering a potential alternative to injections.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Biotechnology
Background:
- Oral delivery of peptides faces challenges like low bioavailability and high variability.
- MEDI7219 is a stabilized, lipidated glucagon-like peptide 1 agonist peptide.
- Sodium chenodeoxycholate (Na CDC) and propyl gallate (PG) were identified as effective permeation enhancers.
Purpose of the Study:
- To develop and optimize oral tablet formulations for MEDI7219.
- To evaluate the in vivo performance of different tablet designs in dogs.
- To improve oral bioavailability and reduce pharmacokinetic variability of MEDI7219.
Main Methods:
- Formulation of immediate-release tablets incorporating Na CDC and PG.
- Application of enteric coatings dissolving at pH ≥ 5.5 for upper duodenal targeting.
- Development of sustained-release formulations with Carbopol and enteric coatings dissolving at pH ≥ 7.0.
- Testing of a proprietary delayed-release erodible barrier layer tablet (OralogiK™).
- In vivo pharmacokinetic studies in dogs.
Main Results:
- Optimized tablet formulations achieved up to 10.1% absolute oral bioavailability of MEDI7219 in dogs.
- Pharmacokinetic variability was reduced to as low as 26% for MEDI7219.
- Different formulation strategies demonstrated varying release profiles and absorption characteristics.
Conclusions:
- Successful development of oral tablet formulations for MEDI7219 with enhanced bioavailability and reduced variability.
- The optimized formulations show promise for clinical development as an alternative to peptide injections.
- Targeted delivery to the gastrointestinal tract using advanced coating technologies is crucial for peptide oral delivery.
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