Polymeric particulates to improve oral bioavailability of peptide drugs

• Published in: Molecules (Basel, Switzerland) Vol. 10; no. 1; pp. 65 - 80
• Main Authors: Delie, Florence, Blanco-Príeto, María José
• Format: Journal Article Book Review
• Language: English
• Published: Switzerland MDPI AG 31-01-2005; MDPI
• Subjects: Administration, Oral; Animals; Biological Availability; calcitonin; Gastrointestinal Tract - drug effects; Gastrointestinal Tract - metabolism; Humans; insulin; Intestinal Absorption - drug effects; mechanisms of absorption; microparticle; Models, Biological; Nanoparticle; Nanoparticles - administration & dosage; Nanoparticles - chemistry; oral route; Particle Size; peptide; Peptides - administration & dosage; Peptides - pharmacokinetics; Pharmaceutical Preparations - administration & dosage; Polymers - chemical synthesis; Polymers - chemistry; Polymers - pharmacokinetics; protein; Review
• DOI: 10.3390/10010065
• EISSN: 1420-3049

Oral administration remains the most convenient way of delivering drugs. Recent advances in biotechnology have produced highly potent new molecules such as peptides, proteins and nucleic acids. Due to their sensitivity to chemical and enzymatic hydrolysis as well as a poor cellular uptake, their oral bioavailability remains very low. Despite sophisticated new delivery systems, the development of a satisfactory oral formulation remains a challenge. Among the possible strategies to improve the absorption of drugs, micro- and nanoparticles represent an exciting approach to enhance the uptake and transport of orally administered molecules. Increasing attention has been paid to their potential use as carriers for peptide drugs for oral administration. This article reviews the most common manufacturing methods for polymeric particles and the physiology of particle absorption from the gastrointestinal (GI) tract. In a second part, the use of polymeric particulate systems to improve the oral absorption of insulin is discussed.