Eudragit-coated dextran microspheres of 5-fluorouracil for site-specific delivery to colon

Objective of the present investigation was to prepare and evaluate the potential of enteric coated dextran microspheres for colon targeting of 5-fluorouracil (5-FU). Dextran microspheres were prepared by emulsification-crosslinking method and the formulation variables studied included different molecular weights of dextran, drug:polymer ratio, volume of crosslinking agent, stirring speed and time. Enteric coating (Eudragit S-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method using different coat:core ratios (4:1 or 8:1). Uncoated and coated dextran microspheres were characterized by particle size, surface morphology, entrapment efficiency, DSC, in vitro drug release in the presence of dextranase and 2% rat cecal contents. The release study of 5-FU from coated dextran microspheres was pH dependent. No release was observed at acidic pH; however, the drug was released quickly where Eudragit starts solublizing there was continuous release of drug from the microspheres. Organ distribution study was suggested that coated dextran microspheres retard the release of drug in gastric and intestinal pH environment and released of drug from microspheres in colon due to the degradation of dextran by colonic enzymes.

Medienart:

E-Artikel

Erscheinungsjahr:

2016

Erschienen:

2016

Enthalten in:

Zur Gesamtaufnahme - volume:23

Enthalten in:

Drug delivery - 23(2016), 1 vom: 17., Seite 328-37

Sprache:

Englisch

Beteiligte Personen:

Rai, Gopal [VerfasserIn]
Yadav, Awesh K [VerfasserIn]
Jain, Narendra K [VerfasserIn]
Agrawal, Govind P [VerfasserIn]

Links:

Volltext

Themen:

25086-15-1
Antimetabolites, Antineoplastic
Colon cancer
Cross-Linking Reagents
Delayed-Action Preparations
Dextran microspheres
Dextranase
Dextrans
EC 3.2.1.11
Excipients
Fluorouracil
Journal Article
Methylmethacrylate-methacrylic acid copolymer
Organ distribution
PH-sensitive polymers
Polymethacrylic Acids
Solvents
U3P01618RT

Anmerkungen:

Date Completed 24.10.2016

Date Revised 03.01.2017

published: Print-Electronic

Citation Status MEDLINE

doi:

10.3109/10717544.2014.913733

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM23841437X