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Volume 71
Issue 3
10.3797/scipharm.aut-03-17
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Article

Development and In Vitro Evaluation of a Mucoadhesive Oral Deliverv System for Antisense Oliaonucleotides

by
Andreas Bernkop-Schnürch
*,
Julia Telsnig
and
Margit Hornof
Institute of Pharmaceutical Technology and Biopharmaceutics, Center of Pharmacy, University of Vienna, Althanstr. 14, A-I 090 Vienna, Austria
*
Author to whom correspondence should be addressed.
Sci. Pharm. 2003, 71(3), 165-177; https://doi.org/10.3797/scipharm.aut-03-17
Submission received: 26 May 2003 / Revised: 24 June 2003 / Accepted: 24 June 2003 / Published: 1 July 2003
Versions Notes

Abstract

It was the aim of this study to develop an oral phosphorothioate oligodeoxynucleotide (PS-ODN) drug delivery system and to evaluate its properties in vitro. Results demonstrated that the 16-mer phosphorothioate oligonucleotide used was completely stable towards enzymatic degradation by secreted and membrane bound intestinal enzymes. Permeation studies with freshly excised intestinal mucosa showed a comparatively high uptake of the PS-ODN with an apparent permeability coefficient (Papp) of 8.35 ± 1.24 x 10-6 cm/sec. The PS-ODN was incorporated in a poly(acrylic acid)-cysteine carrier matrix system exhibiting high cohesive and mucoadhesive properties. Release studies demonstrated that a controlled and sustained PS-ODN release out of this delivery system could be achieved. Because of these features, the dosage form developed within this study seems to represent a promising novel tool for oral PS-ODN delivery.
Keywords: antisense oligonucleotides; mucoadhesive polymers; oral drug delivery; thiomers antisense oligonucleotides; mucoadhesive polymers; oral drug delivery; thiomers

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MDPI and ACS Style

Bernkop-Schnürch, A.; Telsnig, J.; Hornof, M. Development and In Vitro Evaluation of a Mucoadhesive Oral Deliverv System for Antisense Oliaonucleotides. Sci. Pharm. 2003, 71, 165-177. https://doi.org/10.3797/scipharm.aut-03-17

AMA Style

Bernkop-Schnürch A, Telsnig J, Hornof M. Development and In Vitro Evaluation of a Mucoadhesive Oral Deliverv System for Antisense Oliaonucleotides. Scientia Pharmaceutica. 2003; 71(3):165-177. https://doi.org/10.3797/scipharm.aut-03-17

Chicago/Turabian Style

Bernkop-Schnürch, Andreas, Julia Telsnig, and Margit Hornof. 2003. "Development and In Vitro Evaluation of a Mucoadhesive Oral Deliverv System for Antisense Oliaonucleotides" Scientia Pharmaceutica 71, no. 3: 165-177. https://doi.org/10.3797/scipharm.aut-03-17

APA Style

Bernkop-Schnürch, A., Telsnig, J., & Hornof, M. (2003). Development and In Vitro Evaluation of a Mucoadhesive Oral Deliverv System for Antisense Oliaonucleotides. Scientia Pharmaceutica, 71(3), 165-177. https://doi.org/10.3797/scipharm.aut-03-17

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