International Journal of Molecular Sciences,
Journal Year:
2024,
Volume and Issue:
25(23), P. 12778 - 12778
Published: Nov. 28, 2024
Cinnamic
acid
(CA)
has
many
beneficial
effects
on
human
health.
However,
its
poor
water
solubility
(0.23
g/L,
at
25
°C)
is
responsible
for
bioavailability.
This
drawback
prevents
clinical
use.
To
overcome
the
limits
of
this
extraordinary
natural
compound,
in
study,
we
developed
a
highly
water-soluble
inclusion
complex
CA
with
randomly
methylated-β-cyclodextrin
(RAMEB).
The
host-guest
interaction
was
explored
liquid
and
solid
states
by
UV-Vis
titration,
phase
analysis,
FT-IR
spectroscopy,
1H-NMR.
Additionally,
molecular
modeling
studies
were
carried
out.
Both
experimental
theoretical
revealed
1:1
CA/RAMEB
complex,
high
apparent
stability
constant
equal
to
15,169.53
M−1.
increases
about
250-fold
dissolves
within
5
min.
Molecular
demonstrated
that
inserts
phenyl
ring
into
RAMEB
cavity
propyl-2-enoic
tail
leaning
from
wide
rim.
Finally,
biological
vitro
study
compared
free
components,
performed
neuroblastoma
SH-SY5Y
cell
line.
None
them
showed
cytotoxic
assayed
concentrations.
Of
note,
pretreatment
cells
10,
30,
125
µM
doses
significantly
counteracted
effect
neurotoxin
MPP+,
whilst
alone
did
not
show
any
neuroprotection.
Overall,
our
data
complexes
problems,
supporting
their
use
applications.
International Journal of Nanomedicine,
Journal Year:
2025,
Volume and Issue:
Volume 20, P. 25 - 52
Published: Jan. 1, 2025
Abstract:
The
effective
clinical
translation
of
messenger
RNA
(mRNA),
small
interfering
(siRNA),
and
microRNA
(miRNA)
for
therapeutic
purposes
hinges
on
the
development
efficient
delivery
systems.
Key
challenges
include
their
susceptibility
to
degradation,
limited
cellular
uptake,
inefficient
intracellular
release.
Polymeric
drug
conjugates
(PDCs)
offer
a
promising
solution,
combining
benefits
polymeric
carriers
agents
targeted
treatment.
This
comprehensive
review
explores
nucleic
acid
therapeutics,
focusing
conjugates.
It
investigates
how
these
address
obstacles,
enhance
systemic
circulation,
reduce
immunogenicity,
provide
controlled
release,
improving
safety
profiles.
delves
into
conjugation
strategies,
preparation
methods,
various
classes
PDCs,
as
well
strategic
design,
highlighting
role
in
delivery.
Applications
PDCs
treating
diseases
such
cancer,
immune
disorders,
fibrosis
are
also
discussed.
Despite
significant
advancements,
adoption
persist.
concludes
with
insights
future
directions
this
transformative
technology,
underscoring
potential
advance
acid-based
therapies
combat
infectious
significantly.
Keywords:
polymer
conjugates,
International Journal of Biological Macromolecules,
Journal Year:
2025,
Volume and Issue:
unknown, P. 140064 - 140064
Published: Jan. 1, 2025
Curcumin,
a
hydrophobic
drug
derived
from
the
rhizome
of
Curcuma
longa,
exhibits
significant
bioactive
properties,
including
antioxidant
and
antimicrobial
potential.
However,
its
poor
water
solubility
rapid
degradation
limit
practical
applications.
This
study
presents
novel
design
electrospun
nanofibers
using
Curcumin/hydroxypropyl-β-cyclodextrin
inclusion
complex
(HP-β-CD-IC)
combined
with
pullulan
to
enhance
thermal
stability
controlled
release.
In
uniaxial
nanofibers,
curcumin/HP-β-CD-IC
is
uniformly
distributed,
whereas
in
coaxial
serves
as
core
material,
wall
material.
X-ray
diffraction
Fourier-transform
infrared
spectroscopy
confirmed
successful
formation,
fibers
showing
no
crystalline
peaks
curcumin.
Differential
scanning
calorimetry
indicated
enhanced
stability,
melting
points
shifting
279.19
°C
291.63
for
fibers,
respectively.
Scanning
electron
microscopy
transmission
verified
core-shell
structure
uniform
morphology.
vitro
release
studies
revealed
that
achieved
higher
cumulative
(93
±
1.41
%)
compared
(80
2.82
over
350
min.
Antibacterial
tests
demonstrated
improved
activity
against
S.
aureus
E.
coli.
Addressing
critical
need
stable
bioavailable
delivery
compounds,
this
innovative
nanofiber
holds
great
promise
revolutionizing
applications
food
technology
delivery.
Chemical Communications,
Journal Year:
2018,
Volume and Issue:
54(21), P. 2643 - 2646
Published: Jan. 1, 2018
Mixing
γ-cyclodextrin
(γ-CD),
cucurbit[6]uril
(CB[6])
and
tetraammonium-bearing
axles
together
led
to
a
spontaneous
formation
of
γ-CD-CB[6]-cowheeled
[4]pseudorotaxanes.
The
well-defined
unsymmetrical
cavities
thus
formed
enhance
the
binding
affinity
towards
chiral
amines
by
factors
several
hundreds
show
remarkably
improved
discrimination.
AAPS PharmSciTech,
Journal Year:
2024,
Volume and Issue:
25(7)
Published: Oct. 8, 2024
Abstract
This
review
investigates
the
progression
and
effectiveness
of
colon-targeted
drug
delivery
systems,
offering
a
comprehensive
understanding
colon's
anatomy
physiological
environment.
Recognizing
distinctive
features
colon
is
crucial
for
successfully
formulating
oral
dosage
forms
that
precisely
target
specific
areas
in
gastrointestinal
tract
(GIT)
while
minimizing
side
effects
through
mitigating
off-target
sites.
basis
designing
effective
targeted
systems.
The
article
extensively
examines
diverse
approaches
to
drugs
colonic
targeting,
highlighting
key
polymers
excipients
their
production.
Special
emphasis
given
innovative
such
as
hot-melt
extrusion
(HME)
three-dimensional
printing
(3D-P),
renowned
accuracy
release
kinetics
intricate
form
geometry.
However,
challenges
arise
regarding
material
standardization
complex
network
regulatory
clearances
required
confirm
safety
effectiveness.
provides
insights
into
each
application’s
advantages
potential
challenges.
Furthermore,
it
sheds
light
on
local
diseases
necessitate
targeting
available
marketed
products,
providing
an
overview
current
state
Additionally,
emphasizes
importance
testing
controlled
vitro
environment
during
development
phase.
It
also
discusses
future
directions
successful
this
field.
By
integrating
knowledge
across
anatomy,
formulation
techniques,
assessment
methodologies,
valuable
resource
researchers
navigating
dynamic
field
delivery.
Graphical
Organic Letters,
Journal Year:
2025,
Volume and Issue:
27(4), P. 973 - 977
Published: Jan. 17, 2025
Benzene-containing
cucurbituril[2,4]
and
benzene-containing
cucurbituril[3,6],
the
structures
of
cucurbit[n]urils
with
some
glycoluril
units
replaced
by
benzene
rings,
are
constructed
through
condensation
specific
motifs.
These
novel
macrocycles
inherit
cucurbit[n]urils'
concave
cavity
provide
chemical
modification
potentiality
chromophores.
shows
a
C2-symmetric
macrocycle,
while
cucurbituril[3,6]
exhibits
distinctive
two-cavity
structure
(one
big
one
small)
that
resembles
gourd
could
potentially
accommodate
two
guests
different
in
size
simultaneously.
Catalysts,
Journal Year:
2025,
Volume and Issue:
15(2), P. 120 - 120
Published: Jan. 26, 2025
The
regioselective
glycosylation
and
product
specificity
of
hydroxyflavonoid
compounds
profoundly
influences
their
biological
activity
stability,
offering
significant
therapeutic
potential.
However,
most
cyclodextrin
glucosyltransferases
(CGTases)
inherently
lack
regioselectivity
for
flavone
glycosylation.
Herein,
a
CGTase
from
Paenibacillus
macerans
was
engineered
enhanced
by
combining
molecular
docking
analysis
saturation
mutagenesis
strategies.
K232L
(favoring
4′-and
6-hydroxyflavones)
K232V
7-hydroxyflavone)
were
identified
with
distinct
preferences.
In
addition,
H233Y
(preferring
4′-hydroxyflavones),
H233T
6′-hydroxyflavones),
H233K
7′-hydroxyflavones)
also
demonstrated
regioselectivity.
These
variants
further
exhibited
hydrolytic
activity,
enabling
the
efficient
production
short
sugar-chain
glycosides.
Molecular
dynamics
(MDs)
simulations
revealed
that
adopted
optimized
catalytic
conformations
increased
loop
region
flexibility
near
binding
pocket,
enhancing
substrate
accessibility.
findings
underscore
pivotal
roles
K232
H233
in
broadening
scope
offer
valuable
guidance
enzyme
engineering
targeting
