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Titre du document / Document title

Preparation and antitumor characteristics of PLA/(PEG-PPG-PEG) nanoparticles loaded with camptothecin

Auteur(s) / Author(s)

KUNII Ryotaro (1) ; ONISHI Hiraku (1) ; MACHIDA Yoshiharu (1) ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

(1) Department of Drug Delivery Research, Hoshi University, Tokyo, JAPON

Résumé / Abstract

Camptothecin (CPT)-loaded nanoparticles were prepared using poly(DL-lactic acid) (PLA) and poly(ethylene glycol)-block-poly(propylene glycol)-block-poly(ethylene glycol) copolymer (PEG-PPG-PEG), and examined for particle characteristics, in vitro release, pharmacokinetics and efficacy. The preparative condition, in which the ratio of PLA/PEG-PPG-PEG/CPT was 35/35/4 (w/w/w) and organic solvent (dichloromethane) was evaporated from the emulsion at 18 °C, gave the nanoparticles with the diameter of approximately 230 nm, fairly high drug content (ca. 1.6% (w/w)) and stable entrapment of the drug, which were used for in vivo studies. After i.v. administration to normal rats, the nanoparticles showed slightly smaller AUC but much larger MRT as compared with CPT solution, and delivered the drug greatly to the surrounding tissues, in particular to the liver. When antitumor effect was examined by i.v. administration to mice bearing sarcoma 180 (S-180) solid tumor, the nanoparticles showed a significant suppression of tumor growth without body weight loss, and their effect was better than that of CPT solution. The PLA/PEG-PPG-PEG nanoparticles were considered potentially useful to enhance the efficacy of CPT, to which the high drug retention in the body and gradual drug release appeared to be importantly related.

Revue / Journal Title

European journal of pharmaceutics and biopharmaceutics    ISSN  0939-6411 

Source / Source

2007, vol. 67, no1, pp. 9-17 [9 page(s) (article)] (31 ref.)

Langue / Language

Anglais
Revue : Anglais

Editeur / Publisher

Elsevier, Amsterdam, PAYS-BAS  (1991) (Revue)

Mots-clés anglais / English Keywords

Enzyme inhibitor

;

Enzyme

;

Isomerases

;

DNA topoisomerase

;

Alkaloid

;

Microparticle

;

Pharmaceutical technology

;

Pharmacokinetics

;

Release

;

In vitro

;

Nanoparticle

;

Ethylene oxide polymer

;

Lactic acid polymer

;

Antineoplastic agent

;

Preparation

;

Mots-clés français / French Keywords

Inhibiteur de la topoisomérase I

;

Inhibiteur enzyme

;

Enzyme

;

Isomerases

;

DNA topoisomerase

;

Alcaloïde

;

Microparticule

;

Technologie pharmaceutique

;

Pharmacocinétique

;

Libération

;

In vitro

;

Camptothécine

;

Nanoparticule

;

Ethylène oxyde polymère

;

Lactique acide polymère

;

Anticancéreux

;

Préparation

;

Mots-clés espagnols / Spanish Keywords

Inhibidor enzima

;

Enzima

;

Isomerases

;

DNA topoisomerase

;

Alcaloide

;

Micropartícula

;

Tecnología farmacéutica

;

Farmacocinética

;

Liberación

;

In vitro

;

Nanopartícula

;

Etileno óxido polímero

;

Láctico ácido polímero

;

Anticanceroso

;

Preparación

;

Mots-clés d'auteur / Author Keywords

PLA/(PEG-PPG-PEG) nanoparticles

;

Camptothecin

;

In vitro release

;

Pharmacokinetics

;

Antitumor effect

;

Localisation / Location

INIST-CNRS, Cote INIST : 17483, 35400016162696.0020

Nº notice refdoc (ud4) : 18913728



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