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Intraocular delivery of oligonucleotides
A L Gomes Dos Santos1, A Bochot, E Fattal
1Université Paris-Sud, School of Pharmacy, UMR CNRS 8612, 5 Rue Jean Baptiste Clément, 92296 Chatenay-Malabry, France. elias.fattal@cep.u-psud.fr
Current Pharmaceutical Biotechnology
|February 25, 2005
Summary
Antisense oligonucleotides can treat eye diseases by inhibiting gene expression. Drug delivery systems are crucial to enhance their stability, cellular uptake, and sustained release for effective ocular therapy.
Area of Science:
- Ophthalmology
- Molecular Biology
- Drug Delivery Systems
Background:
- Antisense oligonucleotides inhibit gene expression and show potential for treating ocular diseases like scarring and viral infections.
- Current intravitreal administration faces challenges including poor stability, low intracellular penetration, and rapid elimination, necessitating frequent injections and risking retinal damage.
Purpose of the Study:
- To address the limitations of conventional antisense oligonucleotide delivery for ocular diseases.
- To explore the development of drug delivery systems for improved oligonucleotide stability, intracellular penetration, and sustained release.
Main Methods:
- Development and evaluation of novel drug delivery systems for antisense oligonucleotides.
- Assessment of oligonucleotide stability in biological fluids.
- Measurement of intracellular penetration efficiency.
- Evaluation of sustained release kinetics in the vitreous.
Main Results:
- Drug delivery systems significantly enhance the stability of antisense oligonucleotides in biological fluids.
- Improved intracellular penetration of oligonucleotides into target ocular cells.
- Sustained release of oligonucleotides from the delivery system, prolonging therapeutic activity.
Conclusions:
- Drug delivery systems are essential for overcoming the pharmacokinetic and stability challenges of antisense oligonucleotides in ocular applications.
- These systems offer a promising strategy for long-term, effective treatment of ocular diseases with reduced administration frequency and potential for decreased retinal toxicity.