The influence of liposomal formulation on the incorporation and retention of PNA oligomers

[Display omitted] •The delivery of Peptide Nucleic Acid can be increased by encapsulation into liposomes.•Liposomal formulation are optimized to improve stability, drug loading and retention.•PNA oligomers are encapsulated into DOPG based liposomes with high efficiency. Liposomal formulations compos...

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Bibliographic Details
Published in:Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2016-09, Vol.145, p.462-469
Main Authors: Ringhieri, Paola, Avitabile, Concetta, Saviano, Michele, Morelli, Giancarlo, Romanelli, Alessandra, Accardo, Antonella
Format: Article
Language:English
Subjects:
Biomaterials
Cholesterol
Cholesterol - chemistry
DOPG
Drug Compounding
Drug Delivery Systems - methods
Encapsulation
Formulation
Formulations
Insertion
Liposome
Liposomes
Liposomes - chemistry
Oligomers
Optimization
Peptide nucleic acid
Peptide Nucleic Acids - chemistry
Phosphatidylglycerols - chemistry
Phospholipids
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Summary:[Display omitted] •The delivery of Peptide Nucleic Acid can be increased by encapsulation into liposomes.•Liposomal formulation are optimized to improve stability, drug loading and retention.•PNA oligomers are encapsulated into DOPG based liposomes with high efficiency. Liposomal formulations composed of phospholipids with different unsaturation degrees, head groups and at different cholesterol content have been tested for the encapsulation of Peptide Nucleic Acid (PNA) oligomers. The best loading capability (177μg, ER%=87.2) was obtained for pure liposomes of phosphatidylglycerol (DOPG) with negatively charged head group. The insertion of a 10–20% of cholesterol in DOPG based liposomes provides a slight decrease (∼160μg) of the PNA loading. On the other hand, the cholesterol addition (20–30%) slows down the PNA’s release (∼27%) in fetal bovine serum from the liposomal formulation. Based on the encapsulation and the release properties, PEGylated DOPG liposomes with a percentage of cholesterol of 10–20% are the optimal formulation for the loading of PNA-a210.
ISSN:0927-7765
1873-4367
DOI:10.1016/j.colsurfb.2016.05.034