Cargando…

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

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-coat...

Descripción completa

Detalles Bibliográficos
Autores principales: Liu, Zhe-Peng, Cui, Lei, Yu, Deng-Guang, Zhao, Zhuan-Xia, Chen, Lan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3998863/
https://www.ncbi.nlm.nih.gov/pubmed/24790437
http://dx.doi.org/10.2147/IJN.S59516
_version_ 1782313424458350592
author Liu, Zhe-Peng
Cui, Lei
Yu, Deng-Guang
Zhao, Zhuan-Xia
Chen, Lan
author_facet Liu, Zhe-Peng
Cui, Lei
Yu, Deng-Guang
Zhao, Zhuan-Xia
Chen, Lan
author_sort Liu, Zhe-Peng
collection PubMed
description 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.
format Online
Article
Text
id pubmed-3998863
institution National Center for Biotechnology Information
language English
publishDate 2014
publisher Dove Medical Press
record_format MEDLINE/PubMed
spelling pubmed-39988632014-04-30 Electrosprayed core–shell solid dispersions of acyclovir fabricated using an epoxy-coated concentric spray head Liu, Zhe-Peng Cui, Lei Yu, Deng-Guang Zhao, Zhuan-Xia Chen, Lan Int J Nanomedicine Original Research 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. Dove Medical Press 2014-04-16 /pmc/articles/PMC3998863/ /pubmed/24790437 http://dx.doi.org/10.2147/IJN.S59516 Text en © 2014 Liu et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.
spellingShingle Original Research
Liu, Zhe-Peng
Cui, Lei
Yu, Deng-Guang
Zhao, Zhuan-Xia
Chen, Lan
Electrosprayed core–shell solid dispersions of acyclovir fabricated using an epoxy-coated concentric spray head
title 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_short 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
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3998863/
https://www.ncbi.nlm.nih.gov/pubmed/24790437
http://dx.doi.org/10.2147/IJN.S59516
work_keys_str_mv AT liuzhepeng electrosprayedcoreshellsoliddispersionsofacyclovirfabricatedusinganepoxycoatedconcentricsprayhead
AT cuilei electrosprayedcoreshellsoliddispersionsofacyclovirfabricatedusinganepoxycoatedconcentricsprayhead
AT yudengguang electrosprayedcoreshellsoliddispersionsofacyclovirfabricatedusinganepoxycoatedconcentricsprayhead
AT zhaozhuanxia electrosprayedcoreshellsoliddispersionsofacyclovirfabricatedusinganepoxycoatedconcentricsprayhead
AT chenlan electrosprayedcoreshellsoliddispersionsofacyclovirfabricatedusinganepoxycoatedconcentricsprayhead