Abstract：
:The development of new nonviral vectors characterized by high transfection efficiency and low cytotoxicity remains an important challenge in the field of gene delivery. Unsymmetrical bolaamphiphiles (bolas) appear as new emerging candidates for this application. In this work, new unsymmetrical bolas, bearing neutral lactonic acid and cationic ornithine residues at the two ends of a hydrophobic spacer, were synthesized and their properties were compared to analogues bearing a gluconic acid residue. The new bolas showed DNA binding and condensation at higher N/P ratios than their gluconic analogues, probably due to their larger neutral head group. Whereas the size of the complexes of the new bolas with DNA (bolaplexes) increased with N/P, as a result of charge neutralization, their formulations with DOPE at high N/P were of small size (ca. 200 nm). These DOPE formulations showed high transfection efficiency in different cell lines (HeLa, COS-7 and HepG2), close to that of jetPEI. Their cytotoxicity was relatively low, which allowed repetitive transfection in vitro. Fluorescence imaging showed that the bolaplexes bind rapidly to cell surface and internalize mainly through endocytosis. This work suggests a new type of efficient nonviral vectors based on bolaamphiphiles.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Jain N,Goldschmidt V,Oncul S,Arntz Y,Duportail G,Mély Y,Klymchenko ASdoi
10.1016/j.ijpharm.2011.12.026subject
Has Abstractpub_date
2012-02-28 00:00:00pages
392-400issue
2eissn
0378-5173issn
1873-3476pii
S0378-5173(11)01152-5journal_volume
423pub_type
杂志文章abstract：:Microcrystalline cellulose (MCC) is one of the most important excipients due to its outstanding binding and tableting properties. Owing to the absence of high resolution characterization techniques at the single particle scale, 3D (three dimension) microstructure of MCC and its effects on formulation performance remai...
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journal_title：International journal of pharmaceutics
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abstract：:The effect of various surfactants (sodium cholate, sodium taurocholate, Tween 80 and Poloxamer F68) on enhancing the transepithelial permeability of fexofenadine.HCl was evaluated in a human nasal epithelial cell monolayer model. The cytotoxicity of the surfactants on the human nasal epithelial cells was evaluated by ...
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journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
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pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.08.034
更新日期：2013-11-01 00:00:00
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journal_title：International journal of pharmaceutics
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doi：10.1016/j.ijpharm.2007.07.004
更新日期：2008-02-04 00:00:00
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pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.09.022
更新日期：2007-02-22 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00075-7
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journal_title：International journal of pharmaceutics
pub_type： 临床试验,杂志文章
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.08.059
更新日期：2014-11-20 00:00:00
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pub_type： 杂志文章,评审
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更新日期：2013-04-15 00:00:00
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更新日期：2010-05-31 00:00:00
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更新日期：2015-04-30 00:00:00
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更新日期：2011-11-25 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2012-09-15 00:00:00
abstract：:In this paper, a fast forming nano-composite hydrogel was developed for potential application in ocular drug delivery. The optical transmission (OT) as well as rheological properties of nano-composite hydrogel was characterized. The developed nano-composite hydrogel given a high diclofenac micelles loading and provide...
journal_title：International journal of pharmaceutics
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更新日期：2013-05-01 00:00:00
