Self-Nanoemulsifying Drug Delivery System of Lutein: Physicochemical Properties and Effect on Bioavailability of Warfarin
Biomolecules & Therapeutics
; : 173-179, 2013.
Article
in English
| WPRIM (Western Pacific)
| ID: wpr-201014
Responsible library:
WPRO
ABSTRACT
Objective of present study was to prepare and characterize self-nanoemulsifying drug delivery system (SNEDDS) of lutein and to evaluate its effect on bioavailability of warfarin. The SNEDDS was prepared using an oil, a surfactant, and co-surfactants with optimal composition based on pseudo-ternary phase diagram. Effect of the SNEDDS on the bioavailability of warfarin was performed using Sprague Dawley rats. Lutein was successfully formulated as SNEDDS for immediate self-emulsification and dissolution by using combination of Peceol as oil, Labrasol as surfactant, and Transcutol-HP or Lutrol-E400 as co-surfactant. Almost complete dissolution was achieved after 15 min while lutein was not detectable from the lutein powder or intra-capsule content of a commercial formulation. SNEDDS formulation of lutein affected bioavailability of warfarin, showing about 10% increase in Cmax and AUC of the drug in rats while lutein as non-SNEDDS did not alter these parameters. Although exact mechanism is not yet elucidated, it appears that surfactant and co-surfactant used for SNEDDS formulation caused disturbance in the anatomy of small intestinal microvilli, leading to permeability change of the mucosal membrane. Based on this finding, it is suggested that drugs with narrow therapeutic range such as warfarin be administered with caution to avoid undesirable drug interaction due to large amount of surfactants contained in SNEDDS.
Full text:
Available
Health context:
Sustainable Health Agenda for the Americas
Health problem:
Goal 5: Medicines, vaccines and health technologies
Database:
WPRIM (Western Pacific)
Main subject:
Permeability
/
Surface-Active Agents
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Warfarin
/
Lutein
/
Biological Availability
/
Drug Delivery Systems
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Rats, Sprague-Dawley
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Area Under Curve
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Drug Interactions
/
Membranes
Type of study:
Prognostic study
Limits:
Animals
Language:
English
Journal:
Biomolecules & Therapeutics
Year:
2013
Document type:
Article