Efficiency of cell-penetrating peptides on the nasal and intestinal absorption of therapeutic peptides and proteins
| Autor: | Mariko Morishita, Yohei Ikeno, El-Sayed Khafagy, Yoshimi Eda, Noriyasu Kamei, Kozo Takayama |
|---|---|
| Rok vydání: | 2009 |
| Předmět: |
Male
Biological Availability Pharmaceutical Science Mucous membrane of nose Cell-Penetrating Peptides Absorption (skin) Pharmacology Intestinal absorption Catheterization Rats Sprague-Dawley Route of administration Isomerism Pharmacokinetics Intestinal mucosa Glucagon-Like Peptide 1 Ileum Animals Hypoglycemic Agents Medicine Intestinal Mucosa Administration Intranasal Analysis of Variance Drug Carriers Venoms business.industry Interferon-beta Rats Nasal Mucosa Intestinal Absorption Area Under Curve Cell-penetrating peptide Exenatide Nasal administration Carrier Proteins Peptides business Algorithms |
| Zdroj: | International Journal of Pharmaceutics. 381:49-55 |
| ISSN: | 0378-5173 |
| DOI: | 10.1016/j.ijpharm.2009.07.022 |
| Popis: | The purpose of our study was to investigate the potential of cell-penetrating peptides; penetratin as novel delivery vector, on the systemic absorption of therapeutic peptides and proteins across different mucosal administration sites. The absorption-enhancing feasibility of l- and d-penetratin (0.5mM) was used for glucagon-like peptide-1 (GLP-1), and exendin-4 as novel antidiabetic therapy, in addition to interferon-beta (IFN-beta) as protein biotherapeutic model from nasal and intestinal route of administration was evaluated as first time in rats. Nasal route is the most feasible for the delivery of therapeutic peptides coadministered with penetratin whereas the intestinal route appears to be more restricted. The absolute bioavailability (BA (%)) values depend on the physichochemical characters of drugs, stereoisomer character of penetratin, and site of administration. Penetratin significantly increased the nasal more than intestinal absorption of GLP-1 and exendin-4, as the BA for nasal and intestinal administration of GLP-1 was 15.9% and 5%, and for exendin-4 were 7.7% and 1.8%, respectively. Moreover, the BA of IFN-beta coadministered with penetratin was 11.1% and 0.17% for nasal and intestinal administration, respectively. From these findings, penetratin is a promising carrier for transmucosal delivery of therapeutic peptides and macromolecules as an alternative to conventional parenteral routes. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect