Amphiphilic micelles based on chitosan (CS) were applied
as drug
carriers of aceclofenac (ACF) as a potential method to induce its
bioavailability and therapeutic efficiency.
N
-octyl-
N
,
O
-succinyl CS (OSCS), an amphiphilic
CS derivative, was successfully synthesized and loaded physically
by ACF at different pH values and using different dosages of ACF,
forming ACF-loaded polymeric micelles (PMs). The obtained PMs and
ACF-loaded PMs were characterized by different analytical techniques,
including AFM, TEM, DLS, UV–vis spectrophotometry,
1
H NMR spectroscopy, and FT-IR spectroscopy. The pH 5 sample with
a 30% ACF/polymer ratio showed the highest ACF loading capacity (LC)
and entrapment efficiency (EE). In vitro release behaviors of pure
ACF and ACF-loaded PMs at each release point indicated that the release
profile of pH-responsive PMs loaded with ACF demonstrated quicker
release rates (94% after 480 min) compared to the release behavior
noticed for free ACF (59.56% after 480 min). Furthermore, the release
rates exhibit a notable rise when the pH is increased from 1.2 to
4.7. In the carrageenan-induced inflammation model of paw edema in
rats, it has been demonstrated that the injection of ACF-loaded PMs
(at a dose of 10 mg/kg) resulted in a strengthened inflammatory activity
compared to the injection of free ACF at equivalent dosages as well
as at time intervals. However, the use of ACF-loaded PMs for a duration
of 6 h displayed a notable reduction of paw edema, with an inhibition
percentage of 85.09%, in contrast to the 74.9% inhibition percentage
observed for the free ACF medication.