Important note: Information in this article was accurate in 2000. The state of the art may have changed since the publication date.
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Eur J Pharm Sci. 1999 Dec;9(2):163-70. Unique Identifier : AIDSLINE MED/20089035
Berton M; Allemann E; Stein CA; Gurny R; School of Pharmacy, University of Geneva, quai E.-Ansermet; CH-1211, Geneva, Switzerland.
Abstract: Antisense oligonucleotides, and particularly those with phosphorothioate backbones, have emerged as potential gene specific therapeutic agents and are currently undergoing evaluation in clinical trials for a variety of diseases. In the area of HIV-1 therapeutics, targeting of oligonucleotides to infected cells, such as macrophages, would be highly desirable. The present study was designed to prepare and characterize oligonucleotide-loaded nanoparticles for this purpose. Due to their hydrophilic characteristics, oligonucleotides are difficult to entrap in polymeric particles. Here, the oligonucleotides were first complexed with cetyltrimethylammonium bromide. The oligonucleotide-loaded nanoparticles were prepared by the emulsification-diffusion method and subsequently purified. In comparison with previous studies, a high oligonucleotide-loading was achieved; 2.5, 5 and 10% oligonucleotide loading were assessed. If the initial oligonucleotide content was 4%, this method produced a final oligonucleotide loading of 1.9% with an entrapment efficiency of 47%. The integrity of the oligonucleotide and of the polymer, in the final freeze-dried product, was retained.
Copyright © 2000 - National Library of Medicine. Reproduced under license with the National Library of Medicine, Bethesda, MD.
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