1 research outputs found
Development and characterization of polymeric nanoparticles itraconazole
Submitted by Marlene Santos ([email protected]) on 2014-12-16T19:58:48Z
No. of bitstreams: 2
Dissertação - Percília de Andrade Lucena - 2014.pdf: 1506404 bytes, checksum: c895c029b3a1ac62acf42cd19fad7214 (MD5)
license_rdf: 23148 bytes, checksum: 9da0b6dfac957114c6a7714714b86306 (MD5)Approved for entry into archive by Luciana Ferreira ([email protected]) on 2014-12-22T10:32:36Z (GMT) No. of bitstreams: 2
Dissertação - Percília de Andrade Lucena - 2014.pdf: 1506404 bytes, checksum: c895c029b3a1ac62acf42cd19fad7214 (MD5)
license_rdf: 23148 bytes, checksum: 9da0b6dfac957114c6a7714714b86306 (MD5)Made available in DSpace on 2014-12-22T10:32:36Z (GMT). No. of bitstreams: 2
Dissertação - Percília de Andrade Lucena - 2014.pdf: 1506404 bytes, checksum: c895c029b3a1ac62acf42cd19fad7214 (MD5)
license_rdf: 23148 bytes, checksum: 9da0b6dfac957114c6a7714714b86306 (MD5)
Previous issue date: 2014-03-19Polymeric nanoparticles have been used as carriers of drugs that are able to
increase the efficacy of many active ingredients. Among the nanocarriers include
nanocapsules (NCs), which are vesicular structures containing oil inside surrounded
by a polymer wall and nanospheres (NSs) that are impregnated with polymer
matrices drug throughout its surface. These structures have many applications such
as optimizing drug delivery and reducing the toxic potential of drugs. Itraconazole
family of a drug Azole has a broad spectrum of action against fungi and has
appropriate pharmacokinetic characteristics for a drug. Thus, this study aims to
develope and characterize nanostructured systems containing Itraconazole.
Polymeric nanoparticles were obtained by the nanoprecipitation technique,
lyophilized, characterized, and evaluated physical-chemically incorporated into
mucoadhesive topical formulation. Nanocapsules containing Itraconazole showed
encapsulation efficiency rate of 99 ± 6.9%, a mean diameter of 190 ± 10.1 nm, PDI
0.1 ± 0:06 and zeta potential -15 ± 2.5 mV. The nanospheres exhibited rate of
encapsulation efficiency of 97 ± 2.8%, mean diameter 120 ± 0.8 nm, 0.1 ± 0.01 PDI
and zeta potential -10 ± 3.5 mV. Lyophilization was carried out with 10% trehalose +
10% sucrose, achieving satisfactory results. The drug release after 30 days at 37 °C
was 99% for the NCs and 92% for the NEs. The mucoadhesive topical formulation
has in its composition 60% Poloxamer 188, 20% polyethylene glycol 400 and 5mg
nanostructured itraconazole were incorporated homogeneously. The results indicate
that the formulation of Itraconazole in polymeric nanoparticles has potential for in vivo
use in the topical treatment of fungal infections.Nanopartículas poliméricas têm sido utilizadas como carreadores de fármacos
capazes de aumentar a eficácia de muitos insumos ativos. Dentre os
nanocarreadores, destacam-se: nanocápsulas (NCs), que são estruturas
vesiculares, contendo óleo no interior, circundadas por uma parede polimérica e
nanoesferas (NEs) que são matrizes poliméricas impregnadas com fármaco por toda
sua superfície. Essas estruturas possuem diversas aplicações como otimizar a
entrega de fármacos e reduzir o potencial tóxico. O Itraconazol um fármaco da
família dos azóis possui um amplo espectro de ação contra fungos e apresenta
características farmacocinéticas apropriadas para um fármaco. Sendo assim, o
presente trabalho tem como objetivo desenvolver e caracterizar sistemas
nanoestruturados contendo Itraconazol. As nanopartículas poliméricas foram obtidas
através da técnica da nanoprecipitação, liofilizadas, caracterizadas, avaliadas físicoquimicamente
e incorporadas em formulação tópica mucoadesiva. As nanocápsulas
contendo Itraconazol apresentaram taxa de eficiência de encapsulação de 99±6.9%,
diâmetro médio de 190±10.1 nm, PDI 0.1±0.06 e potencial zeta -15±2.5 mV. As
nanoesferas exibiram taxa de eficiência de encapsulação de 97±2.8%, diâmetro
médio de 120±0.8 nm, PDI 0.1±0.01 e potencial zeta -10±3.5 mV. A liofilização foi
realizada com 10% de trealose + 10% de sacarose, alcançando resultados
satisfatórios. A liberação do fármaco após 30 dias a 37°C foi de 99% para as NCs e
92% para as NEs. A formulação tópica mucoadesiva possui em sua composição
60% Poloxamer 188 e 20% de Polietilenoglicol 400 e 5mg de itraconazol
nanoestruturado foram incorporados homogeneamente. Os resultados indicam que a
formulação de itraconazol em nanopartículas poliméricas apresenta potencial para
utilização in vivo no tratamento tópico de infecções fúngicas