Abstract：
:Intranasal administration of mucus-penetrating nanoparticles is an emerging trend to increase drug delivery to the brain. In order to overcome rapid nasal mucociliary clearance, low epithelial permeation, and local enzymatic degradation, we investigated the influence of PEGylation on nose-to-brain delivery of polycaprolactone (PCL) nanoparticles (PCL-NPs) encapsulating bexarotene, a potential neuroprotective compound. PEGylation with 1, 3, 5, and 10% PCL-PEG did not affect particle diameter or morphology. Upon incubation with artificial nasal mucus, only 5 and 10% of PCL-PEG coating were able to ensure NP stability and homogeneity in mucus. Rapid mucus-penetrating ability was observed for 98.8% of PCL-PEG5% NPs and for 99.5% of PCL-PEG10% NPs. Conversely, the motion of non-modified PCL-NPs was markedly slower. Fluorescence microscopy showed that the presence of PEG on NP surface did not reduce their uptake by RMPI 2650 cells. Fluorescence tomography images evidenced higher translocation into the brain for PCL-PEG5% NPs. Bexarotene loaded into PCL-PEG5% NPs resulted in area under the curve in the brain (AUCbrain) 3 and 2-fold higher than that for the drug dispersion and for non-PEGylated NPs (p < 0.05), indicating that approximately 4% of the dose was directly delivered to the brain. Combined, these results indicate that PEGylation of PCL-NPs with PCL-PEG5% is able to reduce NP interactions with the mucus, leading to a more efficient drug delivery to the brain following intranasal administration. Graphical abstract.
journal_name
Drug Deliv Transl Resjournal_title
Drug delivery and translational researchauthors
de Oliveira Junior ER,Santos LCR,Salomão MA,Nascimento TL,de Almeida Ribeiro Oliveira G,Lião LM,Lima EMdoi
10.1007/s13346-020-00816-2subject
Has Abstractpub_date
2020-12-01 00:00:00pages
1688-1699issue
6eissn
2190-393Xissn
2190-3948pii
10.1007/s13346-020-00816-2journal_volume
10pub_type
杂志文章abstract：:Atopic dermatitis (AD) is a chronically relapsing eczematous skin disease characterised by frequent episodes of rashes, severe flares, and inflammation. Till date, there is no absolute therapy for the treatment of AD; however, topical corticosteroids (TCs) are the majorly prescribed class of drugs for the management o...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0480-1
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journal_title：Drug delivery and translational research
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更新日期：2020-06-25 00:00:00
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journal_title：Drug delivery and translational research
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journal_title：Drug delivery and translational research
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journal_title：Drug delivery and translational research
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更新日期：2017-08-01 00:00:00
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journal_title：Drug delivery and translational research
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journal_title：Drug delivery and translational research
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journal_title：Drug delivery and translational research
pub_type： 杂志文章
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更新日期：2018-10-01 00:00:00
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journal_title：Drug delivery and translational research
pub_type： 杂志文章,评审
doi：10.1007/s13346-015-0266-7
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journal_title：Drug delivery and translational research
pub_type： 杂志文章
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更新日期：2011-04-01 00:00:00
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journal_title：Drug delivery and translational research
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更新日期：2019-04-01 00:00:00
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journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-020-00708-5
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journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-010-0007-x
更新日期：2011-02-01 00:00:00
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journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0557-x
更新日期：2018-10-01 00:00:00
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journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0533-5
更新日期：2018-10-01 00:00:00
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journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-012-0063-5
更新日期：2012-04-01 00:00:00
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journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-013-0143-1
更新日期：2013-06-01 00:00:00
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journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0522-8
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journal_title：Drug delivery and translational research
pub_type： 杂志文章
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更新日期：2012-02-01 00:00:00
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journal_title：Drug delivery and translational research
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journal_title：Drug delivery and translational research
pub_type： 杂志文章,评审
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journal_title：Drug delivery and translational research
pub_type： 杂志文章,评审
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journal_title：Drug delivery and translational research
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journal_title：Drug delivery and translational research
pub_type： 杂志文章,评审
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journal_title：Drug delivery and translational research
pub_type： 杂志文章
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journal_title：Drug delivery and translational research
pub_type： 杂志文章
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更新日期：2014-06-01 00:00:00
abstract：:The promise of RNA interference (RNAi) technology in cancer therapeutics aims to deliver small interfering RNA (siRNA) for silencing of gene expression in cell type-specific pathway. However, the challenge for the delivery of stable siRNA is hindered by an immune-hostile tumor microenvironment and physiological barrie...
journal_title：Drug delivery and translational research
pub_type： 杂志文章,评审
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更新日期：2017-04-01 00:00:00
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journal_title：Drug delivery and translational research
pub_type： 杂志文章
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更新日期：2021-01-11 00:00:00
abstract：:The objective of the present work was to formulate a novel stable delivery system which would not only overcome the solubility issue of silymarin, but also help to increase the therapeutic value by better permeation, anticancer action and reduced toxicity. This was envisaged through the recent developments in nanotech...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
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更新日期：2016-10-01 00:00:00
