Evaluation of thermoresponsive properties and biocompatibility of polybenzofulvene aggregates for leuprolide delivery

In this study, a polybenzofulvene derivative named poly-6-MOEG-9-BF3k, was evaluated as polymeric material for the production of injectable thermoresponsive nano-aggregates able to load low molecular weight peptidic drug, like the anticancer leuprolide. Thermoresponsive behavior of poly-6-MOEG-9-BF3k was studied in aqueous media by evaluating scattering intensity variations by means of DLS in function of temperature. Zeta potential measurements and SEM observations were also carried out. Moreover, critical aggregation temperature of the poly-6-MOEG-9-BF3k polymer was evaluated by pyrene fluorescence analysis. Then, the ability of prepared thermoresponsive aggregates to protect this model oligopeptide drug and regulate its release rate in function of external temperature was evaluated in vitro. Finally, biocompatibility of poly-6-MOEG-9-BF3k aggregates was tested in vitro on a healthy cell line (human bronchial epithelial cell: 16-HBE) and in vivo on rat animal model upon subcutaneous administration. (C) 2012 Elsevier B.V. All rights reserved.