Characterization of complexes of an antisense oligonucleotide with protamine and poly-l-lysine salts

Thiolated Polycarbophil as an Adjuvant for Permeation Enhancement in Nasal Delivery of Antisense Oligonucleotides

“…To improve their stability against nuclease digestion various chemical modifications have been evaluated such as replacing the phosphodiester backbone with a raised nuclease resistant phosphorothioate backbone (PTO‐ODNs) 4. In previous studies, the development of ODN delivery systems with suitable polycationic carriers or cationic liposomes was a potential way to extrinsically protect the ODNs from enzymatic metabolism 5. The coadministration of thiolated polymers or designated thiomers such as polycarbophil‐cysteine (PCP‐Cys) is another promising strategy to improve the bioavailability and above‐mentioned unfavorable properties of ODNs.…”

Protamine nanoparticles

“…4 The interaction of protamine salts and ODN was investigated to determine the physico-chemical characteristics of the resulting complex systems and to analyze the infl uence of permeation enhancers (sodium chenodeoxycholate and sodium caprate) on the dissociation of the complexes. 5 Zeta potential data confi rmed the conductometric equivalence points and explained the good physical stability of charged complexes when compared with neutral complexes (+/−25 mV for protamine sulfate complexes). Moreover, incorporation of sodium chenodeoxycholate promoted complex dissociation, while sodium caprate inhibited dissociation.…”

“…Moreover, incorporation of sodium chenodeoxycholate promoted complex dissociation, while sodium caprate inhibited dissociation. 5 For effi cient transfection of HIV-1 target cells, protamine was used to complex ODN and phosphorothioate (PTO) analogues to form nanoparticles with diameters of about 180 nm and surface charges in the range of −18 to +30 mV. 6 The uptake of these nanoparticles was signifi cantly improved as compared with naked oligonucleotides.…”

Development of novel HDL-mimicking α-tocopherol-coated nanoparticles to encapsulate nerve growth factor and evaluation of biodistribution

“…By neutralizing the charges on proteins and improving lipophilicity, the ion-pair agents can facilitate the encapsulation of the proteins into lipid-based NPs. Protamines and poly-l-lysine (PLL) are the polycationic carriers used to form complex with macromolecules [19–21]. The complexation helped condense macromolecules and protect them from enzymatic degradation.…”