1. The influence of liposomal formulation on the incorporation and retention of PNA oligomers
- Author
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Concetta Avitabile, Alessandra Romanelli, Antonella Accardo, Paola Ringhieri, Michele Saviano, Giancarlo Morelli, Ringhieri, Paola, Avitabile, Concetta, Saviano, Michele, Morelli, Giancarlo, Romanelli, Alessandra, and Accardo, Antonella
- Subjects
Peptide Nucleic Acids ,0301 basic medicine ,Drug Compounding ,02 engineering and technology ,03 medical and health sciences ,chemistry.chemical_compound ,Drug Delivery Systems ,Colloid and Surface Chemistry ,Physical and Theoretical Chemistry ,Phospholipids ,Phosphatidylglycerol ,Degree of unsaturation ,Liposome ,Chromatography ,Peptide nucleic acid ,Cholesterol ,Peptide Nucleic Acid ,Phosphatidylglycerols ,Surfaces and Interfaces ,General Medicine ,021001 nanoscience & nanotechnology ,030104 developmental biology ,Formulation ,chemistry ,Biochemistry ,Liposomes ,DOPG ,lipids (amino acids, peptides, and proteins) ,0210 nano-technology ,Fetal bovine serum ,Biotechnology - Abstract
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 (177 ?g, 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 (~160 ?g) 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.
- Published
- 2016
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