Electrosprayed core–shell solid dispersions of acyclovir fabricated using an epoxy- coated concentric spray head

Zhe-Peng Liu,1 Lei Cui,2 Deng-Guang Yu,3 Zhuan-Xia Zhao,1 Lan Chen11School of Medical Instrument and Food Engineering, 2Tin Ka Ping College of Science, 3School of Materials Science and Engineering, University of Shanghai for Science and Technology, Shanghai, People's Republic of ChinaAbstra...

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Autores principales: Liu ZP, Cui L, Yu DG, Zhao ZX, Chen L
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Lenguaje:EN
Publicado: Dove Medical Press 2014
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spelling oai:doaj.org-article:9242cff6238f4014a54778452de7d5812021-12-02T03:11:43ZElectrosprayed core–shell solid dispersions of acyclovir fabricated using an epoxy- coated concentric spray head1178-2013https://doaj.org/article/9242cff6238f4014a54778452de7d5812014-04-01T00:00:00Zhttp://www.dovepress.com/electrosprayed-corendashshell-solid-dispersions-of-acyclovir-fabricate-a16489https://doaj.org/toc/1178-2013 Zhe-Peng Liu,1 Lei Cui,2 Deng-Guang Yu,3 Zhuan-Xia Zhao,1 Lan Chen11School of Medical Instrument and Food Engineering, 2Tin Ka Ping College of Science, 3School of Materials Science and Engineering, University of Shanghai for Science and Technology, Shanghai, People's Republic of ChinaAbstract: A novel structural solid dispersion (SD) taking the form of core–shell microparticles for poorly water-soluble drugs is reported for the first time. Using polyvinylpyrrolidone (PVP) as a hydrophilic polymer matrix, the SDs were fabricated using coaxial electrospraying (characterized by an epoxy-coated concentric spray head), although the core fluids were unprocessable using one-fluid electrospraying. Through manipulating the flow rates of the core drug-loaded solutions, two types of core–shell microparticles with tunable drug contents were prepared. They had average diameters of 1.36±0.67 and 1.74±0.58 µm, and were essentially a combination of nanocomposites with the active ingredient acyclovir (ACY) distributed in the inner core, and the sweeter sucralose and transmembrane enhancer sodium dodecyl sulfate localized in the outer shell. Differential scanning calorimetry and X-ray diffraction results demonstrated that ACY, sodium dodecyl sulfate, and sucralose were well distributed in the PVP matrix in an amorphous state because of favorable second-order interactions. In vitro dissolution and permeation studies showed that the core–shell microparticle SDs rapidly freed ACY within 1 minute and promoted nearly eightfold increases in permeation rate across the sublingual mucosa compared with raw ACY powders.Keywords: core–shell microparticle, solid dispersion, coaxial electrospraying, poorly water-soluble drug, epoxy-coated spray headLiu ZPCui LYu DGZhao ZXChen LDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 1967-1977 (2014)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Liu ZP
Cui L
Yu DG
Zhao ZX
Chen L
Electrosprayed core–shell solid dispersions of acyclovir fabricated using an epoxy- coated concentric spray head
description Zhe-Peng Liu,1 Lei Cui,2 Deng-Guang Yu,3 Zhuan-Xia Zhao,1 Lan Chen11School of Medical Instrument and Food Engineering, 2Tin Ka Ping College of Science, 3School of Materials Science and Engineering, University of Shanghai for Science and Technology, Shanghai, People's Republic of ChinaAbstract: A novel structural solid dispersion (SD) taking the form of core–shell microparticles for poorly water-soluble drugs is reported for the first time. Using polyvinylpyrrolidone (PVP) as a hydrophilic polymer matrix, the SDs were fabricated using coaxial electrospraying (characterized by an epoxy-coated concentric spray head), although the core fluids were unprocessable using one-fluid electrospraying. Through manipulating the flow rates of the core drug-loaded solutions, two types of core–shell microparticles with tunable drug contents were prepared. They had average diameters of 1.36±0.67 and 1.74±0.58 µm, and were essentially a combination of nanocomposites with the active ingredient acyclovir (ACY) distributed in the inner core, and the sweeter sucralose and transmembrane enhancer sodium dodecyl sulfate localized in the outer shell. Differential scanning calorimetry and X-ray diffraction results demonstrated that ACY, sodium dodecyl sulfate, and sucralose were well distributed in the PVP matrix in an amorphous state because of favorable second-order interactions. In vitro dissolution and permeation studies showed that the core–shell microparticle SDs rapidly freed ACY within 1 minute and promoted nearly eightfold increases in permeation rate across the sublingual mucosa compared with raw ACY powders.Keywords: core–shell microparticle, solid dispersion, coaxial electrospraying, poorly water-soluble drug, epoxy-coated spray head
format article
author Liu ZP
Cui L
Yu DG
Zhao ZX
Chen L
author_facet Liu ZP
Cui L
Yu DG
Zhao ZX
Chen L
author_sort Liu ZP
title Electrosprayed core–shell solid dispersions of acyclovir fabricated using an epoxy- coated concentric spray head
title_short Electrosprayed core–shell solid dispersions of acyclovir fabricated using an epoxy- coated concentric spray head
title_full Electrosprayed core–shell solid dispersions of acyclovir fabricated using an epoxy- coated concentric spray head
title_fullStr Electrosprayed core–shell solid dispersions of acyclovir fabricated using an epoxy- coated concentric spray head
title_full_unstemmed Electrosprayed core–shell solid dispersions of acyclovir fabricated using an epoxy- coated concentric spray head
title_sort electrosprayed core–shell solid dispersions of acyclovir fabricated using an epoxy- coated concentric spray head
publisher Dove Medical Press
publishDate 2014
url https://doaj.org/article/9242cff6238f4014a54778452de7d581
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AT yudg electrosprayedcorendashshellsoliddispersionsofacyclovirfabricatedusinganepoxycoatedconcentricsprayhead
AT zhaozx electrosprayedcorendashshellsoliddispersionsofacyclovirfabricatedusinganepoxycoatedconcentricsprayhead
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