Development and evaluation of an in vitro vaginal model for assessment of drug's biopharmaceutical properties: curcumin
Berginc, Katja (Author), Škalko-Basnet, Nataša (Author), Basnet, Purusotam (Author), Kristl, Albin (Author)

URLURL - Presentation file, Visit http://link.springer.com/article/10.1208%2Fs12249-012-9837-9 This link opens in a new window

Vaginal administration is a promising alternative to the per-oral route in achieving systemic or local therapeutic effects, when intestinal drug absorption is hindered by problematic biopharmaceutical drug properties. The aim of this study was to establish an in vitro vaginal model and use it to characterize biopharmaceutical properties of liposomally associated curcumin destined for vaginal delivery. The in vitro permeability, metabolism, and tissue retention of high/low permeable compounds were assessed on cow vaginal mucosa and compared to the permeabilities determined through Caco-2 cells and rat jejunum in vitro. The results showed that the intestinal mucosa was superior to the vaginal one in categorizing drugs based on their permeabilities in high/low permeable classes. Passive diffusion was found to be the main mechanism of drug penetration through vaginal mucosa and it was not affected by transporter- enzyme alliance, as their expression/activity was significantly reduced compared to the intestinal tract. Curcumin permeability from the solution form was the lowest of all tested substances due to its significant tissue retention and curcumin-mucus interactions. The permeability of liposomally associated curcumin was even lower but the binding of liposomally associated curcumin to the vaginal tissue was significantly higher. The permeability and tissue retention of liposomal curcumin were vesicle size dependent. Vaginal application of liposomally associated curcumin provides relatively high levels of curcumin in vaginal tissue, with limited systemic absorption.

Keywords:curcumin, intestinal models, liposomes, permeability, vaginal mucosa
Work type:Not categorized (r6)
Tipology:1.01 - Original Scientific Article
Organization:FFA - Faculty of Pharmacy
Number of pages:str. 1045-1053
Numbering:Vol. 13, issue 4
ISSN on article:1530-9932
DOI:10.1208/s12249-012-9837-9 Link is opened in a new window
COBISS.SI-ID:3287665 Link is opened in a new window
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Record is a part of a journal

Title:AAPS PharmSciTech
Shortened title:AAPS PharmSciTech
Publisher:American Association of Pharmaceutical Scientists
COBISS.SI-ID:1247345 This link opens in a new window

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