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Medchem & Toxicology 2018
Page 96
Journal of Organic & Inorganic Chemistry
ISSN: 2472-1123
A n n u a l C o n g r e s s o n
Medicinal Chemistry,
Pharmacology and toxicology
J u l y 3 0 - 3 1 , 2 0 1 8
Am s t e r d a m , N e t h e r l a n d s
W
e have designed a microemulsion (ME) containing Ketoprofen (KET) for anti-inflammatory effect evaluated using the rat
paw edema model. The ME was prepared by adding propylene glycol (PG) loaded with 1% KET/water (3:1, w/w), to a mixture
of sorbitan monooleate and polysorbate 80 (47.0%) at 3:1 (w/w) and canola oil (38.0%). The physicochemical characterization of
KET-loaded ME involved particle size and zeta potential determination, entrapment efficiency, calorimetric analysis, and in vitro
drug release. The in vivo anti-inflammatory study employed male Wistar rats. Measurement of the foot volume was performed
using a caliper immediately before and 2, 4, and 6 h after injection of Aerosil. KET-loaded ME showed particle size around 20
nm, with zeta potential at -16 mV and entrapment efficiency at 70%. Moreover, KET was converted to the amorphous state
when loaded in the formulation and it was shown that the drug was slowly released from the ME. Finally, the in vivo biological
activity was similar to that of the commercial gel, but ME better controlled edema at 4 h. These results demonstrated that the ME
formulation is an alternative strategy for improving KET skin permeation for anti-inflammatory effect. Furthermore, our findings
are promising considering that the developed ME was loaded with only 1% KET, and the formulation was able to keep a similar
release profile and in vivo effect compared to the commercial gel with 2.5% KET. Therefore, the KET-loaded developed herein ME
is likely to have a decreased side effect compared with that of the commercial gel, but both presented the same efficacy.
wasigame@gmail.comMicroemulsion for improved skin delivery and in vivo
anti-inflammatory effect
Praca FSG
1
, Bentley MVLB
1
and Medina WSG
2
1
University of Sao Paulo, Brazil
2
University of Padre Albino, Brazil
J Org Inorg Chem 2018, Volume 4
DOI: 10.21767/2472-1123-C3-009