Arginine end-functionalized poly(L-lysine) dendrigrafts for the stabilization and controlled release of insulin

作者：Sideratou Zili; Sterioti Nikoletta; Tsiourvas Dimitris^*; Tziveleka Leto Aikaterini; Thanassoulas Angelos; Nounesis George; Paleos Constantinos M

来源：Journal of Colloid and Interface Science, 2010, 351(2): 433-441.

DOI：10.1016/j.jcis.2010.07.072

• Insulin
• Biodegradable polymers
• Dendrigrafts
• Protein-polymer interaction

Second generation biodegradable poly(L-lysine) dendrigrafts functionalized with 12-48 arginine end-groups interact, at physiological pH, with insulin affording dendrigraft/insulin complexes as established by dynamic light scattering, zeta-potential, circular dichroism and isothermal titration calorimetry. Binding occurs in two steps; at low dendrigraft/insulin molar ratios (<= 0.07) interaction is accompanied with the endothermic dissociation of insulin dimers, while at higher molar ratios, complexation of insulin monomers with dendrigraft derivatives occurs exothermically. High levels of insulin complexation efficiencies (>99%) were determined for all derivatives. Stabilization of complexed insulin against enzymatic degradation by trypsin and alpha-chymotrypsin is observed especially for the highly arginine end-functionalized dendrigrafts. Insulin release rates in simulated intestinal fluid are being controlled by the number of arginine end-groups and released insulin retains its conformation.

• 出版日期2010-11-15