Publication: In vitro antisense activity of chitosan/AsODN complexes
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Date
2009
Authors
Enneli, Burcu
Özabaş Turan, S.
Uslu, B.
Akbuğa, J.
Journal Title
Journal ISSN
Volume Title
Publisher
İstanbul Kültür Üniversitesi
Abstract
In this study, the complex forms of AsODNs
(phosphodiester and phosphorothioate forms)
were prepared by using a cationic polymer called
chitosan. The effect of chitosan mol wts and
chitosan/AsODN ratio on the complex properties
was studied. Afterwards, the physicochemical
properties such as zeta-potential and particle size
of complexes were measured and the in vitro
antisense activities of the appropriate
formulations were investigated. Full complexation
was observed with phosphorothioate AsODN at
the ratio of 10:1 (+/-), however phosphodiester
AsODN could not be formed full complex with
chitosan. The antisense activity of 100:1
(chitosan/AsODN) complexes which have
approximately 200 nm particle size, was measured
based on the inhibition of β-galactosidase by the
antisense containing formulations into the b-Gal
transfected HeLa cell lines. Eventually, both of these complex forms protected AsODNs from
potential enzymatic degradations. In 100:1 (+/-)
complex formulations, high antisense activity (88-
90%) was observed. As a result, chitosan can be
considered as a suitable carrier especially for
phosphorothioate modified AsODNs. Molecular
weight of chitosan and chitosan/AsODN mass
ratio had no importance in in vitro inhibition. This
study can form the basis for the forthcoming
studies related with carrier systems of AsODNs
that will be done with chitosan polymer
Description
Keywords
Antisense oligonucleotide, chitosan, complex, carrier, gene expression