Characterization of PLGA microparticles as a drug carrier for 3-ethoxycarbonyl-2H-benzofuro[3,2-f]-1-benzopyran-2-one. Ultrastructural study of cellular uptake and intracellular distribution

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dc.contributor.authorGomes, Anderson J.
dc.contributor.authorFaustino, Adriana S.
dc.contributor.authorMachado, Antonio Eduardo H.
dc.contributor.authorZaniquelli, Maria Elisabete D.
dc.contributor.authorde Paula Rigoletto, Thais
dc.contributor.authorNain Lunardi, Claure
dc.contributor.authorLunardi, Laurelucia O.
dc.contributor.institutionUniversidade Federal de Uberlândia (UFU)
dc.contributor.institutionUniversidade de São Paulo (USP)
dc.contributor.institutionFac Ciências Farmaceut Ribeirao Preto
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.date.accessioned2014-05-20T15:29:55Z
dc.date.available2014-05-20T15:29:55Z
dc.date.issued2006-11-01
dc.description.abstractHere we describe the application of microparticles (MPs) for the delivery and release of the drug a benzopsoralen. We also evaluated the intracellular distribution and cellular uptake of the drug by using an encapsulation technique for therapeutic optimization. MPs containing the compound 3-ethoxycarbonyl-2H-benzofuro[3,2-f]-1-benzopyran-2-one (psoralen A) were prepared by the solvent evaporation technique, and parameters such as particle size, drug encapsulation efficiency, effect of the encapsulation process on the drug's photochemistry, zeta potential, external morphology, and < i > in vitro </i > release behavior were evaluated. The intracellular distribution of MPs as well as their uptake by tissues were monitored. Size distribution studies using dynamic ligh scattering and scanning electron microscopy revealed that the MPs are spherical in shape with a diameter of 1.4 mu m. They present low tendency toward aggregation, as confirmed by their zeta potential (+10.6 mV). The loading efficiency obtained was 75%. As a consequence of the extremely low diffusivity of the drug in aqueous medium, the drug release profile of the MPs in saline phosphate buffer (pH 7.4) was much slower than that obtained in the biological environment. Among the population of peritoneal phagocytic cells, only macrophages were able to phagocytose poly-d,l-lactic-co-glycolic acid (PLGA) MP. The use of psoralen A in association with ultraviolet light (360 nm) revealed morphological characteristics of cell damage such as cytoplasmic vesiculation, mitochondria condensation, and swelling of both the granular endoplasmatic reticulum and the nuclear membrane. These results indicate that PLGA MP could be a promising delivery system for psoralen in connection with ultraviolet irradiation therapy (PUVA).en
dc.description.affiliationUniversidade Federal de Uberlândia (UFU), Inst Quim, BR-38400089 Uberlandia, MG, Brazil
dc.description.affiliationFac Filosofia Ciências & Letras Ribeirao Pret, Ribeirao Preto, Brazil
dc.description.affiliationFac Ciências Farmaceut Ribeirao Preto, Rio Claro, Brazil
dc.description.affiliationUniv Estadual Julio de Mesquita Filho, Inst Biociencia, Rio Claro, Brazil
dc.description.affiliationUnespUniv Estadual Julio de Mesquita Filho, Inst Biociencia, Rio Claro, Brazil
dc.format.extent447-454
dc.identifierhttp://dx.doi.org/10.1080/10717540600640369
dc.identifier.citationDrug Delivery. Philadelphia: Taylor & Francis Inc., v. 13, n. 6, p. 447-454, 2006.
dc.identifier.doi10.1080/10717540600640369
dc.identifier.issn1071-7544
dc.identifier.urihttp://hdl.handle.net/11449/39385
dc.identifier.wosWOS:000240779800007
dc.language.isoeng
dc.publisherTaylor & Francis Inc
dc.relation.ispartofDrug Delivery
dc.relation.ispartofjcr3.095
dc.relation.ispartofsjr0,748
dc.rights.accessRightsAcesso restrito
dc.sourceWeb of Science
dc.subjectmicroparticlespt
dc.subjectpsoralenpt
dc.subjectPUVA therapypt
dc.subjectultrastructurept
dc.titleCharacterization of PLGA microparticles as a drug carrier for 3-ethoxycarbonyl-2H-benzofuro[3,2-f]-1-benzopyran-2-one. Ultrastructural study of cellular uptake and intracellular distributionen
dc.typeArtigo
dcterms.licensehttp://journalauthors.tandf.co.uk/permissions/reusingOwnWork.asp
dcterms.rightsHolderTaylor & Francis Inc
unesp.author.orcid0000-0001-8712-4417[6]
unesp.author.orcid0000-0002-5804-5717[1]
unesp.author.orcid0000-0003-2734-0892[1]
unesp.author.orcid0000-0001-6200-3686[3]

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