Self-assembly hydrogels as multifunctional drug delivery of paclitaxel for synergistic tumour-targeting and biocompatibility in vitro and in vivo

ObjectivesIn this work, we designed the self-assembly peptide hydrogels to multiply therapeutic agents for improving anticancer effect and lowering adverse reaction of paclitaxel (PTX).MethodsThe folate (FA)-peptide-PTX hydrogels consist of self-assemble peptide hydrogel as nanoscale carrier, FA and RGD peptide as targeting moieties and paclitaxel as anticancer drug. The properties of hydrogels, such as morphology, size distribution, zeta potential and rheology, were investigated. Targeted specificity, biodistribution and anticancer effect were studied both in vitro and in vivo.Key findingsFolate-peptide-PTX hydrogel nanoparticles were spherical in shape with hydrodynamic diameter of approximately 137.3 ± 15.2 nm. The hydrogels could only target monolayer cancer cells but also penetrated the nuclei of cells in vitro. The in-vivo real-time imaging further demonstrated that the hydrogels preferentially accumulated in tumour and sustained release. Compared to free paclitaxel, the FA-peptide-PTX hydrogels had higher anticancer effect and lower side effect.ConclusionsThe dual-targeted drug delivery possessed strong capability of synergistic targeted delivery, long-term drug release and better biocompatibility than paclitaxel both in vitro and in vivo. The results obtained demonstrated a high potential of the proposed drug delivery system in improving the therapeutic efficacy of paclitaxel.