Pharmaceutical Development and Technology,
Journal Year:
2023,
Volume and Issue:
28(9), P. 865 - 876
Published: Oct. 5, 2023
AbstractIn
situ
forming
depots
(ISFDs)
represent
attractive
alternatives
to
the
conventional
sustained
drug
delivery
systems.
Carvedilol,
a
short
half-life
used
on
daily
basis
manage
chronic
conditions,
could
benefit
from
this
technology.
The
aim
of
work
was
develop,
for
first
time,
new
injectable
long-acting
carvedilol-ISFD.
Accordingly,
4
different
grades
polyesters
with
varying
properties
as
i)
lactide-to
glycolide
ratio
(polylactide-co-glycolide
(PLGA)
vs.
polylactide
(PLA)),
and
ii)
end
functionality
(acid-
ester-capped)
were
utilized
preparation
ISFD
formulations.
In
addition,
organic
solvents
(i.e.
N-methyl-2-pyrrolidone
(NMP),
dimethyl
sulfoxide
(DMSO),
ethyl
acetate,
benzyl
benzoate)
also
investigated.
It
found
that
NMP
DMSO
more
suitable
formation
depots.
Furthermore,
all
formulations
demonstrated
excellent
encapsulation
efficiency
96–98%).
Interestingly,
both
PLGA-based
ISFDs
(acid-capped
exhibited
similar
release
behaviors
able
extend
carvedilol
over
30
days.
On
other
hand,
acid-capped
ester-capped
PLA-based
slower
days
an
average
only
36%
60%,
respectively.
conclusion,
developed
carvedilol-ISFDs
resulted
in
tunable
extended-release
behavior,
simply
by
choosing
appropriate
grade
polymer.
These
results
open
door
toward
novel
carvedilol-ISFD
formulation.Keywords:
ImplantsPLGAPLAsustained
AcknowledgmentThe
authors
thank
University
Jordan
financial
support.Disclosure
statementNo
potential
conflict
interest
reported
author(s).Additional
informationFundingThe
support.
Advanced Drug Delivery Reviews,
Journal Year:
2023,
Volume and Issue:
201, P. 115055 - 115055
Published: Aug. 17, 2023
The
minimally-invasive
and
painless
nature
of
microneedle
(MN)
application
has
enabled
the
technology
to
obviate
many
issues
with
injectable
drug
delivery.
MNs
not
only
administer
therapeutics
directly
into
dermal
ocular
space,
but
they
can
also
control
release
profile
active
compound
over
a
desired
period.
To
enable
prolonged
delivery
payloads,
various
MN
types
have
been
proposed
evaluated,
including
dissolving
MNs,
polymeric
loaded
or
coated
nanoparticles,
fast-separable
hollow
hydrogel
MNs.
These
intricate
yet
intelligent
platforms
provide
an
attractive
approach
decrease
side
effects
administration
frequency,
thus
offer
potential
increase
patient
compliance.
In
this
review,
formulations
that
are
for
long-acting
address
clinical
needs
myriad
diseases
discussed.
We
highlight
design
aspects,
such
as
polymer
selection
geometry,
in
addition
computational
mathematical
modeling
necessary
help
streamline
develop
high
translational
value
impact.
Finally,
up-scale
manufacturing
regulatory
hurdles
along
avenues
require
further
research
bring
market
carefully
considered.
It
is
hoped
review
will
insight
formulators
clinicians
judicious
materials
tandem
refined
may
elegant
achieve
sustained
payloads
through
simple
patch.
Infection and Drug Resistance,
Journal Year:
2025,
Volume and Issue:
Volume 18, P. 1471 - 1483
Published: March 1, 2025
Upper
respiratory
tract
infections
are
among
the
most
prevalent
diseases,
imposing
both
financial
and
physical
burdens
on
affected
individuals.
Roxithromycin
(ROX),
a
primary
drug
for
treating
bacterial-induced
infections,
is
typically
administered
orally
due
to
its
hydrophobic
nature.
However,
non-specific
distribution
resulting
from
oral
administration
reduces
bioavailability
can
cause
side
effects
such
as
diarrhea.
In
this
study,
we
prepared
thermo-sensitive
in-situ
gel
using
facile
highly
reproducible
method
by
simply
mixing
two
types
of
poloxamers
with
ROX.
The
ROX
be
well
dissolved
in
poloxamer
matrix
amorphous
state
give
solution.
Upon
intranasal
administration,
solution
undergoes
phase
transition
form
under
body
temperature.
This
remains
nasal
cavity
an
extended
period,
releasing
directly
site
infection
minimizing
distribution.
Pharmacokinetic
experiments
revealed
that,
compared
local
increased
1.5
times,
concentration
8
times.
contrast,
concentrations
liver
small
intestine
did
not
significantly
differ
those
following
administration.
vivo
antibacterial
also
showed
that
has
superior
efficacy
excellent
biocompatibility.
These
results
suggest
promising
formulation
bacterial
upper
infections.
International Journal of Pharmaceutics,
Journal Year:
2024,
Volume and Issue:
664, P. 124623 - 124623
Published: Aug. 25, 2024
Docetaxel
(DTX)
is
a
recommended
treatment
in
patients
with
metastasic
prostate
cancer
(PCa),
despite
its
therapeutic
efficacy
limited
by
strong
systemic
toxicity.
However,
localized
PCa,
intratumoral
(IT)
administration
of
DTX
could
be
an
alternative
to
consider
that
may
help
overcome
the
disadvantages
conventional
intravenous
(IV)
therapy.
In
this
context,
we
here
present
first
vivo
preclinical
study
PCa
therapy
nanomedicines
mesoporous
silica
nanoparticles
(MSN)
and
IT
injection
over
xenograft
mouse
model
bearing
human
adenocarcinoma
tumors.
The
tolerability,
biodistribution
histopathology
after
have
been
investigated
for
nanomedicine
free
drug,
compared
IV
DTX.
obtained
results
demonstrate
allows
precise
selective
non-metastatic
minimize
diffusion
showing
superior
activity
than
route.
This
reducing
dose
one
order
widens
substantially
window
drug.
Furthermore,
use
as
promotes
antitumor
drug
accumulation
at
tumor
site,
improving
same
Acta Biomaterialia,
Journal Year:
2024,
Volume and Issue:
187, P. 1 - 19
Published: Aug. 28, 2024
Inflammatory
skin
conditions
highly
influence
the
quality
of
life
patients
suffering
from
these
disorders.
Symptoms
include
red,
itchy
and
painful
lesions,
which
are
visible
to
rest
world,
causing
stigmatization
a
significantly
lower
mental
health
patients.
Treatment
options
often
unsatisfactory,
as
they
suffer
either
low
patient
adherence
or
risk
severe
side
effects.
Considering
this,
there
is
need
for
new
treatments,
notably
ways
delivering
drugs.
Stimuli-responsive
drug
delivery
systems
able
deliver
their
cargo
in
response
given
stimulus
are,
thus,
promising
treatment
inflammatory
conditions.
For
example,
use
external
stimuli
such
ultraviolet
light,
near
infrared
radiation,
alteration
magnetic
field
enables
release
be
precisely
controlled
space
time.
On
other
hand,
internal
induced
by
pathological
condition,
including
pH
upregulation
reactive
oxygen
species
enzymes,
can
utilized
create
that
specifically
target
diseased
achieve
better
efficacy
safety.
In
latter
context,
however,
it
key
importance
match
trigger
mechanism
system
actual
features
specific
condition.
Hence,
focus
this
article
placed
not
only
on
reviewing
stimuli-responsive
developed
treat
conditions,
but
also
critically
evaluating
context
diseases.
STATEMENT
OF
SIGNIFICANCE:
Skin
diseases
affect
one-third
world's
population,
lowering
patients,
who
deal
with
symptoms
well
due
visibility
symptoms.
Current
treatments
hampered
serious
Therefore,
more
emphasis
should
developing
innovative
formulations
provide
safety
hold
considerable
promise
regard,
where
when
needed,
reducing
adverse
effects
potentially
offering
outcomes.
Architecturally
hindered
crystallization
of
bottlebrush
graft
copolymers
offers
a
reaction-
and
solvent-free
pathway
for
creating
injectable
elastomers
with
tissue-mimetic
softness.
Currently,
materials
involve
solvents
chemical
reactions,
leading
to
uncontrolled
swelling,
leaching
unreacted
moieties,
side
reactions
tissue.
To
address
this
issue,
poly(ethylene
glycol)
(PEG)
amorphous
block
crystallizable
poly(lactic
acid)
(PLA)
grafted
chains
(A-g-B)
were
synthesized,
controlled
length
arranged
along
the
backbone
at
spacing.
The
densely
PEG
brush
is
leveraged
architecturally
control
both
rate
degree
PLA
grafts,
offering
tunability
mechanical
properties
as
function
architecture
time
in
single-component
system
covering
broad
range
aggregation
states
comprising
fluid-,
paste-,
elastomer-like
behaviors
modulus
ranging
from
1
50
kPa.
PLA-g-PEG
pastes
are
particularly
interesting,
they
combine
injectability
time-controlled
formation
shape-persistent
constant
temperature.
This
molecular
paste
platform
may
advance
reconstructive
surgery,
drug
depots,
tissue
engineering.
Nanomedicine,
Journal Year:
2025,
Volume and Issue:
unknown, P. 1 - 18
Published: Jan. 31, 2025
Advancements
in
tissue
regeneration,
particularly
bone
regeneration
is
key
area
of
research
due
to
potential
novel
therapeutic
approaches.
Efforts
reduce
reliance
on
autologous
and
allogeneic
grafts
have
led
the
development
biomaterials
that
promote
synchronized
controlled
healing.
However,
use
growth
factors
limited
by
their
short
half-life,
slow
penetration,
large
molecular
size
toxicity.
These
suggest
traditional
delivery
methods
may
be
inadequate
hence,
address
these
challenges,
new
strategies
are
being
explored.
approaches
include
bioactive
substances
within
advanced
systems
enable
precise
spatiotemporal
control.
Dual-release
composite
scaffolds
offer
a
promising
solution
reducing
need
for
multiple
surgical
interventions
simplifying
treatment
process.
allow
sustained
drug
release,
enhancing
repair
while
minimizing
drawbacks
conventional
methods.
This
review
explores
various
dual-drug
release
systems,
discussing
modes
action,
types
drugs
used
mechanisms
improve
regeneration.