| Summary: | Pentagamavunon-0 (PGV-0) is a new drug derived from curcumin which
is synthesised by modification the β-diketone group into cyclic monoketone.
PGV-0 possesses anti inflammatory effect of 40% and does not show ulcerogenic
effect. However, PGV-0 has a poor bioavailability due to its low absorption.
Nanoparticle formulation is a strategy which can be used to increase the solubility
of PGV-0 so that the absorption and the bioavailability increase. The aim of the
current study was to develop PGV-0 nanoparticles, to examine the anti
inflammatory activity in vivo, and to determine the enzymatic affinity of PGV-0
nanoparticles.
PGV-0 nanoparticles were formulated based on ionic gelation between
chitosan, PGV-0, and TPP as cross linker. PGV-0 nanoparticles were
characterised for the particle size, polydispersity index, zeta potential,
morphology, entrapment efficiency, and its stability in artificial gastrointestinal
fluid. The anti inflammatory activity was examined on carrageenan induced paw
edema in rats. The enzymatic affinity was tested by calculating the inhibitory
effect of COX-1 and COX-2.
The size of PGV-0 nanoparticles was 159.77 nm with polydispersity
index of 0.529 and zeta potential 3.41 mV. The morphology of PGV-0
nanoparticles were spherical. PGV-0 nanoparticles have shown high entrapment
efficiency (99.30 ± 0.08%) and a high stability in both artificial gastric and
intestinal fluid of 99.51 ± 0.03% and 99.52 ± 0.04%. respectively. PGV-0
nanoparticles which contain PGV-0 5 mg/kgBW have shown an anti
inflammatory effect of 60.63%. PGV-0 nanoparticles have shown affinity
enzymatic selective to COX-2. From the study, it is shown that PGV-0
nanoparticles obtained by ionic gelation using chitosan can increase the anti
inflammatory activity of PGV-0.
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