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Submicron cationic emulsions as a new delivery system for oligonucleotides
H Teixeira1, C Dubernet, F Puisieux
1Laboratoire de Physico-chimie, Pharmacotechnie et Biopharmacie, URA CNRS 1218, Faculté de Pharmacie, Université Paris XI, Châtenay-Malabry, France.
Pharmaceutical Research
|February 9, 1999
Summary
Submicron emulsions with stearylamine (SA) effectively deliver oligonucleotides (ON), protecting them from degradation. Further optimization could enhance this promising oligonucleotide delivery system.
Area of Science:
- Biotechnology
- Nanotechnology
- Drug Delivery Systems
Background:
- Oligonucleotides (ON) show therapeutic potential but require effective delivery systems.
- Submicron emulsions offer a versatile platform for encapsulating and delivering therapeutic agents.
Purpose of the Study:
- To evaluate submicron emulsions containing stearylamine (SA) as a delivery system for oligonucleotides (ON).
- To characterize the association efficiency, stability, and interactions of ON within these SA-modified emulsions.
Main Methods:
- Submicron emulsions with varying SA concentrations were prepared using microfluidization.
- Association efficiency, particle size, zeta-potential, and release kinetics were analyzed.
- ON-SA interactions and nuclease stability were investigated using partitioning studies and incubation in cell culture medium.
Main Results:
- Emulsions with SA demonstrated significantly higher ON association efficiency compared to controls.
- SA-containing emulsions protected ON from degradation for up to 3 hours in culture medium.
- ON and SA formed insoluble ion-pairs, with SA migration stabilizing the emulsion interface.
Conclusions:
- Submicron emulsions containing SA are a valuable system for oligonucleotide delivery.
- Further improvements are possible by optimizing the oily phase for SA/ON complex solubility.