Pluronics
(tri-block copolymers) have a significant role in the
pharmaceutical industry and are being used to enhance the solubility
and delivery of hydrophobic drugs in different marketed formulations.
However, instability and unsatisfactory drug-loading capacity are
the major weak spots of these pluronic micelles. The present research
work is designed to solve the existing issues by the solubilization
study of hydrophobic drugs in different pluronic micelles at variable
temperatures. The solubilization of the hydrophobic antiepileptic
drug lamotrigine (LAM) in five different pluronic micelles viz. P84,
P85, F127, F108, and F68 was studied at different temperatures, 37,
47, and 57 °C, using UV–visible spectroscopy. The solubilization
of LAM in pluronic micelles increased with the increase in temperature.
Small-angle neutron scattering (SANS) measurements were used to observe
the morphological and structural changes taking place in pluronics
by increasing the temperature. The SANS results showed the morphological
changes of spherical P84 micelles to prolate ellipsoidal micelles
at 57 °C due to remarkable increase in the aggregation number.
This morphological conversion was further confirmed by the heat transfer
method (HTM) and dynamic light scattering (DLS) measurements. DLS
measurements confirmed that LAM-loaded micelles showed a greater hydrodynamic
diameter (
D
h
) compared to unloaded micelles,
assuring LAM solubilization in the pluronic micelles. The rate of
controlled release of LAM from five different pluronic micelles was
accessed by using different kinetic models to evaluate the in vitro
release profile. This is the first report in which HTM measurements
are established for the analysis of morphological changes in the thermoresponsive
pluronic micelles in real time. The present work corroborates how
we can control the drug-loading capacity, morphological structure
of the drug carrier, as well as drug release by simply changing the
temperature of pluronic micellar media.
Catanionic surfactant-hydrotrope mixtures have proven to be a striking alternative to tune microstructures over a wide range of compositions and also to minimize precipitation that is normally observed in catanionic mixtures at an equimolar ratio. These mixtures are supposed to be of great relevance in biological systems when a hydrotrope is a "drug". Keeping this in view, here we report composition- and dilution-induced structural changes in a catanionic mixture comprising ionic liquids (ILs), such as 1-dodecyl-3-methylimidazolium bromide (C12mimBr)/1-tetradecyl-3-methylimidazolium bromide (C14mimBr), and a drug, diclofenac sodium (DFNa), in aqueous solution. The structural changes are probed by small-angle neutron scattering (SANS), dynamic light scattering (DLS), and zeta-potential measurements. SANS data and size distribution curves clearly depict the formation of low curvature structures on going from the cation-rich to anion-rich composition up to a 0.7 mole fraction of DFNa (XDFNa). The amphiphilic nature of DFNa is supposed to alter the surface charge density, which is provoked by its incorporation into resulting aggregates, as confirmed by modified zeta-potential values. The modification of the average packing parameter resulting from the IL and DFNa complexation equilibrium seems to play a vital role in bringing out structural transitions of mixed aggregates. We also focused our attention to study the effect of dilution in concentrations ranging from 100 to 25 mM. At XDFNa = 0.0 and 0.1, the size of prolate ellipsoids decreases on dilution, mimicking classic behavior, but an opposite trend is observed at other XDFNa values. Dilution-induced transformation to larger aggregates is thought to be driven by the release of DFNa molecules from the mixed micelles on account of the critical micelle concentration (cmc) (solubility) mismatch between the two components. The role of other interactions such as cation-π and π-π in stabilizing the mixed aggregates in addition to hydrophobic interactions is probed by (1)H NMR.
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