Enhanced oral bioavailability of resveratrol using lipid formulations

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ENHANC§D

ORAL

BIOAVAILABILITY

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N§§YENATROL

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LIPM

FORMULATION§

M"

Argenziana,

R.

§pagnolo,

§,

Mantoni, G,

Zwq

M. Trottt, R' Cqv*tli

Dipartimento

di

scienza e Tecnologia del Farmaco, I"lniversità degli §tudi di Torino,

Via

P' Giuria

9,

lSI25,

Torino

Resycratml, a polyphenolic phytoalexin pre§eilt

in

different plant sources, ha§ attracted increasing

attsntion

in

receni-years

pliying

an impomant

role

in

the prevention

of

rnany human diseases'

especially

for

irs

antioxiO*t

_irortrti"r.

1f1r*

in

vivo effect of resveratrcl aftor oral administration is

negligible

when

compare$

io

its

efficacy

ix

vitro.

Indced,

the

moleculc has

a pocr

aqueous

so:uU-ility and

a

hydràphobic nature

which

determines

a low

dirsolution rate and

a*

extensive presystemic metaUlnsm. Moreover resveratrol

is

an extremely photosensitive compound' Several

iormutation strategios have bcen proposed to overcome these limitations and to irnprove

solubility-chemical srabiliry-and ornt bioavailàUiUty

of

ttre molccule. The eim

*f

the present

work

was to

devetop a formuiation

in

order to increasi the bioavailability after arnl administraticn;

ir

particular

tipnsoÀes and

lipid

cornplexos based

on

phosphatidylcholine

w*rs

preparsd and characterizsd' Commercial fitasomes were used

for

comparison

purpoo*.

The interaction

nf

resveratrol

with

the

differcnt vehicles, demonstrated by Diffcrential §cànning Calorimetry

GSC)

and Fourier transfurm

infrared

spectrsscspy

{FTg1),

pioduced

a

marked increase

of

the solubility and

stabilit-v

of

resveratrol. The

amouniof

rciveiatrot pre§§$t in the complex was about 45

%

wlw' The liposomes

showed

a

loading

ef:ciency

of

?8%

and sizes abaut §00 nm. The

in

vitro

rslease kinetics

of

resveratroì

from

the formulations was

in

vitro evaluated, showing a prolongad release profile over

time. In

vivo

cxperiments were carried out administeringcrally thc

lipid

formulations.to rats' The

plasma concentràticn,

oi

r"ru**trol

were higher with ttre tipiO fcrrmulations than with the free drug'

Thc bioavaitrability

of

resveratrol was enhanced three

timei

after the

lipid

complex administration'

Lipid

f*rmulations can

be

a

§tratcgy

to

improve

the

absorption

and oral bioavailability of

lesveratrol.