Affiliation:
1. Department of Chemistry, Aligarh Muslim University, Aligarh-202002, India
Abstract
Abstract
The aim of this investigation is the characterization of interaction
of different bile salts – sodium cholate (NaC), sodium deoxycholate
(NaDC) and sodium taurocholate (NaTC) with amphiphilic drug imipramine
hydrochloride (IMP) because the bioavailability of lipophilic drugs
following oral administration strongly depends on the presence of food
components. These bile salts improve the bioavailability of poorly
absorbable drugs by lowering the surface tension of the
gastrointestinal fluid or by solubilization. The interactions in the
binary systems (drug and bile salts) were studied by determining
various physicochemical parameters like critical micelle concentration
(cmc), ideal cmc (cmcid
),
counterion dissociation (g), standard Gibbs free energy (ΔG
m
0), enthalpy (ΔH
m
0), and
entropy of micellization (ΔS
m
0), micellar
mole fractions of bile salt (X
1
Rub, X
1
M,
X
1
Rod), micellar mole fraction of bile salt in ideal
state (X
1
id), interaction parameter (β),
activity coefficients (f
1, f
2), and excess free energy of
mixing (ΔG
ex) of the mixed micelles using
Clint's, Rubingh's, Motomura's and Rodenas's theories for mixed
micellar systems. All the results point out synergism and attractive
interactions in the mixed systems of drug and bile salts. NaDC is more
effective in reducing the cmc of drug IMP as compared to NaC
and NaTC because it binds strongly to the positively charged drug ions
and reduces the head group area more in comparison to other. This
study will give insight into the selection of drugs in different
applications as their properties get modified by interaction with bile
salts, thus influencing their solution behavior which, in turn,
modifying the phase-forming behavior, microemulsion, clouding
phenomenon, besides solubilization. The modification of solubilization
ability in a medium can be exploited for the purpose of selective
encapsulation and release.
Subject
Physical and Theoretical Chemistry
Cited by
45 articles.
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