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Nucleic Acids Research, 2000, Vol. 28, No. 16 3134-3142
© 2000 Oxford University Press

The spherulitesTM: a promising carrier for oligonucleotide delivery

Nathalie Mignet1,2, Armelle Brun2, Corinne Degert2, Brigitte Delord3, Didier Roux3, Claude Hélène1, René Laversanne2 and Jean-Christophe François1,*

1Laboratoire de Biophysique, Muséum National d’Histoire Naturelle, INSERM U201, CNRS UMR 8646, 43 rue Cuvier, 75231 PARIS Cedex 05, France, 2Capsulis, S.A, Château Bersol, Bâtiment 1, 218/228 Avenue du Haut-Lévêque, 33600 PESSAC, France and 3Centre de Recherche Paul Pascal, Avenue du Dr A. Schweitzer, 33600 PESSAC, France

Concentric multilamellar microvesicles, named spherulitesTM, were evaluated as an oligonucleotide carrier. Up to 80% oligonucleotide was encapsulated in these vesicles. The study was carried out on two different spheruliteTM formulations. The spheruliteTM size and stability characteristics are presented. Delivery of encapsulated oligonucleotide was performed on a rat hepatocarcinoma and on a lymphoblastoid T cell line, both expressing the luciferase gene. We showed that spherulitesTM were able to transfect both adherent and suspension cell lines and deliver the oligonucleotide to the nucleus. Moreover, 48–62% luciferase inhibition was obtained in the rat hepatocarcinoma cell line when the antisense oligonucleotide targeted to the luciferase coding region was encapsulated at 500 nM concentration in spherulitesTM of different compositions.

* To whom correspondence should be addressed. Tel: +33 140 793 708; Fax: +33 140 793 705; Email: francois@cimrs1.mnhn.fr


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