polymeric particulates to improve oral bioavailability of peptide drugs聚合物颗粒改善多肽药物的口服生物利用度.pdf

Molecules 2005, 10, 65-80 molecules ISSN 1420-3049 Review Polymeric Particulates to Improve Oral Bioavailability of Peptide Drugs Florence Delie 1 and María José Blanco-Príeto 2,* 1 School of Pharmacy, 30, Quai E. Ansermet, CH-1211 Geneva 4, Switzerland, Phone: (+41) 22 379 6573, Fax: (+41) 22 379 6567, E-mail: Florence.Delie@pharm.unige.ch 2 Centro Galénico, Farmacia y Tecnología Farmacéutica, Universidad de Navarra; Ap. 177, 31080 – Pamplona, Spain, Phone: (+34) 948 42 56 00, Fax: (+34) 948 42 56 49. * Author to whom correspondence should be addressed; e-mail: mjblanco@unav.es Received: 28 May 2004 / Accepted: 7 July 2004 / Published: 31 January 2005 Abstract : 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 f