microencapsulation of rutin increases its therapeutic effect

MICROENCAPSULATION OF RUTIN INCREASES ITS THERAPEUTIC
EFFECT IN INFLAMMATORY PAIN
MEDEIROS, D.C.1; OLIVEIRA, P.C. 2; LEITE, L.F.2; SFEIR, N. 2; MIZOKAMI, S.1;
GEORGETTI S.2; CASAGRANDE R.2; VERRI JR W.1; BARACAT, M. 2
1
Departamento de Ciências Patológicas, Universidade Estadual de Londrina, Londrina,
Parana, Brasil
2
Departamento de Ciências Farmacêuticas, Universidade Estadual de Londrina,
Londrina, Parana, Brasil
Keywords: Delivery systems, microencapsules, rutin, pain therapy
The drug delivery systems are an integral part of current pharmaceutical research for the
creation as well as improvement of existing drugs, representing a crucial step for
modulating drug release. The formation of microcapsules is one of the techniques used
for obtaining this type of release system. The microencapsulation methods, in general,
consist of applying a material on the external surface of a solid particle, conferring
benefits and properties in relation to a non-coated form. The aim of this study was to
develop microcapsules containing rutin, and evaluate the therapeutic efficacy in
vivo. To obtain the rutin microcapsules it was employed the complex coacervation
physicochemical method, obtaining a conjugate pectin/casein with the formation of
microcapsules
and lyophilization. Morphological
evaluation and analysis
of
the size and distribution of the particles of the microcapsules by scanning electron
microscopy and light scattering technique was performed, respectively. The
quantification of the rutin was performed by an exhaustive extraction of the drug
formulation. The in
vitro dissolution testing was performed according to the
specifications of the Brazilian Pharmacopoeia 5th ed, with some adaptations. The
evaluation of in vivo efficacy of microencapsulated rutin was performed in a model
of carrageenan in mice. The microcapsules were spherical and of homogeneous size.
The average particle size was 4,903 μm with a standard deviation of 4,421 μm. Through
exhaustive extraction method it was found that the amount of drug present in the
microcapsules was 96,81%, quantified by DPPH method. There was no significant
release of rutin in the first 120 minutes from the dissolution test, during which time the
microcapsules were exposed to the medium simulating the gastric pH. In a medium
simulating
the intestinal
fluid pH,
the
release of
rutin was
gradual and reached 81.82% at 10h after the start of the test. In a model of inflammatory
pain, microencapsulated
rutin showed greater
efficacy
(64.12%)
than nonmicroencapsulated rutin (27.73%). The process was successful to obtain rutin loaded
microcapsules, and suggest that microencapsulation increased the efficacy of rutin to
reduce inflammatory pain.
Acknowledgments: Universidade Estadual de Londrina, CAPES and Fundação
Araucária