title: The influence of liposomal formulation on the incorporation and retention of PNA oligomers.
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 (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.
authors.affiliation: Department of Pharmacy, University of Naples "Federico II", via Mezzocannone 16, 80134 Napoli, Italy; Interuniversity Research Centre on Bioactive Peptides (CIRPeB), via Mezzocannone 16, 80134 Napoli, Italy.
authors.forename: Paola
authors.initials: P
authors.lastname: Ringhieri
authors.affiliation: Institute of Biostructure and Bioimaging (IBB), CNR, via Mezzocannone 16, 80134 Napoli, Italy.
authors.forename: Concetta
authors.initials: C
authors.lastname: Avitabile
authors.affiliation: Institute of Crystallography (IC), CNR, Via Amendola 122, 70126 Bari, Italy.
authors.forename: Michele
authors.initials: M
authors.lastname: Saviano
authors.affiliation: Department of Pharmacy, University of Naples "Federico II", via Mezzocannone 16, 80134 Napoli, Italy; Interuniversity Research Centre on Bioactive Peptides (CIRPeB), via Mezzocannone 16, 80134 Napoli, Italy.
authors.forename: Giancarlo
authors.initials: G
authors.lastname: Morelli
authors.affiliation: Department of Pharmacy, University of Naples "Federico II", via Mezzocannone 16, 80134 Napoli, Italy; Interuniversity Research Centre on Bioactive Peptides (CIRPeB), via Mezzocannone 16, 80134 Napoli, Italy. Electronic address: alessandra.romanelli@unina.it.
authors.forename: Alessandra
authors.initials: A
authors.lastname: Romanelli
authors.affiliation: Department of Pharmacy, University of Naples "Federico II", via Mezzocannone 16, 80134 Napoli, Italy; Interuniversity Research Centre on Bioactive Peptides (CIRPeB), via Mezzocannone 16, 80134 Napoli, Italy. Electronic address: antonella.accardo@unina.it.
authors.forename: Antonella
authors.initials: A
authors.lastname: Accardo
mesh_terms: D002784:Cholesterol / Q000737:chemistry; D004339:Drug Compounding; D016503:Drug Delivery Systems / Q000379:methods; D008081:Liposomes / Q000737:chemistry*; D020135:Peptide Nucleic Acids / Q000737:chemistry*; D010715:Phosphatidylglycerols / Q000737:chemistry*; D010743:Phospholipids
chemical_list: D008081:Liposomes; D020135:Peptide Nucleic Acids; D010715:Phosphatidylglycerols; D010743:Phospholipids; D002784:Cholesterol
keywords: Cholesterol; DOPG; Formulation; Liposome; Peptide nucleic acid