Cargando…

Nanostructured lipid carriers for percutaneous administration of alkaloids isolated from Aconitum sinomontanum

BACKGROUND: Lipid-based nanosystems have great potential for transdermal drug delivery. In this study, nanostructured lipid carriers (NLCs) for short-acting alkaloids lappacontine (LA) and ranaconitine (RAN) isolated from Aconitum sinomontanum (AAS) at 69.47 and 9.16% (w/w) yields, respectively, wer...

Descripción completa

Detalles Bibliográficos
Autores principales: Guo, Teng, Zhang, Yongtai, Zhao, Jihui, Zhu, Chunyun, Feng, Nianping
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4496826/
https://www.ncbi.nlm.nih.gov/pubmed/26156035
http://dx.doi.org/10.1186/s12951-015-0107-3
_version_ 1782380465122967552
author Guo, Teng
Zhang, Yongtai
Zhao, Jihui
Zhu, Chunyun
Feng, Nianping
author_facet Guo, Teng
Zhang, Yongtai
Zhao, Jihui
Zhu, Chunyun
Feng, Nianping
author_sort Guo, Teng
collection PubMed
description BACKGROUND: Lipid-based nanosystems have great potential for transdermal drug delivery. In this study, nanostructured lipid carriers (NLCs) for short-acting alkaloids lappacontine (LA) and ranaconitine (RAN) isolated from Aconitum sinomontanum (AAS) at 69.47 and 9.16% (w/w) yields, respectively, were prepared to enhance percutaneous permeation. Optimized NLC formulations were evaluated using uniform design experiments. Microstructure and in vitro/in vivo transdermal delivery characteristics of AAS-loaded NLCs and solid lipid nanoparticles (SLNs) were compared. Cellular uptake of fluorescence-labeled nanoparticles was probed using laser scanning confocal microscopy and fluorescence-activated cell sorting. Nanoparticle integrity during transdermal delivery and effects on the skin surface were also investigated. RESULTS: NLC formulations were less cytotoxic than the AAS solution in HaCaT and CCC-ESF cells. Moreover, coumarin-6-labeled NLCs showed biocompatibility with HaCaT and CCC-ESF cells, and their cellular uptake was strongly affected by cholesterol and lipid rafts. Significantly greater cumulative amounts of NLC-associated LA and RAN than SLN-associated alkaloids penetrated the rat skin in vitro. In vivo microdialysis showed higher area under the concentration–time curve (AUC)(0–t) for AAS-NLC-associated LA and RAN than for AAS-SLN-associated alkaloids. CONCLUSIONS: NLC formulations could be good transdermal systems for increasing biocompatibility and decreasing cytotoxicity of AAS. AAS-NLCs showed higher percutaneous permeation than the other preparations. These findings suggest that NLCs could be promising transdermal delivery vehicles for AAS.
format Online
Article
Text
id pubmed-4496826
institution National Center for Biotechnology Information
language English
publishDate 2015
publisher BioMed Central
record_format MEDLINE/PubMed
spelling pubmed-44968262015-07-10 Nanostructured lipid carriers for percutaneous administration of alkaloids isolated from Aconitum sinomontanum Guo, Teng Zhang, Yongtai Zhao, Jihui Zhu, Chunyun Feng, Nianping J Nanobiotechnology Research BACKGROUND: Lipid-based nanosystems have great potential for transdermal drug delivery. In this study, nanostructured lipid carriers (NLCs) for short-acting alkaloids lappacontine (LA) and ranaconitine (RAN) isolated from Aconitum sinomontanum (AAS) at 69.47 and 9.16% (w/w) yields, respectively, were prepared to enhance percutaneous permeation. Optimized NLC formulations were evaluated using uniform design experiments. Microstructure and in vitro/in vivo transdermal delivery characteristics of AAS-loaded NLCs and solid lipid nanoparticles (SLNs) were compared. Cellular uptake of fluorescence-labeled nanoparticles was probed using laser scanning confocal microscopy and fluorescence-activated cell sorting. Nanoparticle integrity during transdermal delivery and effects on the skin surface were also investigated. RESULTS: NLC formulations were less cytotoxic than the AAS solution in HaCaT and CCC-ESF cells. Moreover, coumarin-6-labeled NLCs showed biocompatibility with HaCaT and CCC-ESF cells, and their cellular uptake was strongly affected by cholesterol and lipid rafts. Significantly greater cumulative amounts of NLC-associated LA and RAN than SLN-associated alkaloids penetrated the rat skin in vitro. In vivo microdialysis showed higher area under the concentration–time curve (AUC)(0–t) for AAS-NLC-associated LA and RAN than for AAS-SLN-associated alkaloids. CONCLUSIONS: NLC formulations could be good transdermal systems for increasing biocompatibility and decreasing cytotoxicity of AAS. AAS-NLCs showed higher percutaneous permeation than the other preparations. These findings suggest that NLCs could be promising transdermal delivery vehicles for AAS. BioMed Central 2015-07-10 /pmc/articles/PMC4496826/ /pubmed/26156035 http://dx.doi.org/10.1186/s12951-015-0107-3 Text en © Guo et al. 2015 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Research
Guo, Teng
Zhang, Yongtai
Zhao, Jihui
Zhu, Chunyun
Feng, Nianping
Nanostructured lipid carriers for percutaneous administration of alkaloids isolated from Aconitum sinomontanum
title Nanostructured lipid carriers for percutaneous administration of alkaloids isolated from Aconitum sinomontanum
title_full Nanostructured lipid carriers for percutaneous administration of alkaloids isolated from Aconitum sinomontanum
title_fullStr Nanostructured lipid carriers for percutaneous administration of alkaloids isolated from Aconitum sinomontanum
title_full_unstemmed Nanostructured lipid carriers for percutaneous administration of alkaloids isolated from Aconitum sinomontanum
title_short Nanostructured lipid carriers for percutaneous administration of alkaloids isolated from Aconitum sinomontanum
title_sort nanostructured lipid carriers for percutaneous administration of alkaloids isolated from aconitum sinomontanum
topic Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4496826/
https://www.ncbi.nlm.nih.gov/pubmed/26156035
http://dx.doi.org/10.1186/s12951-015-0107-3
work_keys_str_mv AT guoteng nanostructuredlipidcarriersforpercutaneousadministrationofalkaloidsisolatedfromaconitumsinomontanum
AT zhangyongtai nanostructuredlipidcarriersforpercutaneousadministrationofalkaloidsisolatedfromaconitumsinomontanum
AT zhaojihui nanostructuredlipidcarriersforpercutaneousadministrationofalkaloidsisolatedfromaconitumsinomontanum
AT zhuchunyun nanostructuredlipidcarriersforpercutaneousadministrationofalkaloidsisolatedfromaconitumsinomontanum
AT fengnianping nanostructuredlipidcarriersforpercutaneousadministrationofalkaloidsisolatedfromaconitumsinomontanum