Molecularly imprinted polymers
have exhibited good performance
as carriers on drug loading and sustained release. In this paper,
vinblastine (VBL)-loaded polymeric nanoparticles (VBL–NPs)
were prepared by a one-step molecular imprinting process, avoiding
the waste and incomplete removal of the template, and evaluated as
targeting carriers for VBL delivery after modification. Using acryloyl
amino acid comonomers and disulfide cross-linkers, VBL–NPs
were synthesized and then conjugated with poly(ethylene glycol)–folate.
The dynamic size of the obtained VBL–NPs–PEG–FA
was 258.3 nm (PDI = 0.250), and the encapsulation efficiency was 45.82
± 1.45%. The nanoparticles of VBL–NPs–PEG–FA
were able to completely release VBL during 48 h under a mimic tumor
intracellular condition (pH 4.5, 10 mM glutathione (GSH)), displaying
significant redox responsiveness, whereas the release rates were much
slower in the mimic body liquid (pH 7.4, 2 μM GSH) and tumor
extracellular environment (pH 6.5, 2 μM GSH). Furthermore, the
carriers NPs–PEG–FA, prepared without VBL, showed satisfactory
intrinsic hemocompatibility, cellular compatibility, and tumor-targeting
properties: they could rapidly and efficiently accumulate to folate
receptor positive Hela cells and then internalized via receptor-mediated
endocytosis, and the retention in tumor tissues could last for over
48 h. Interestingly, VBL–NPs–PEG–FA could evidently
increase the accumulation of VBL in tumor tissues while decreasing
the distribution of VBL in organs, exert similar anticancer efficacy
against Hela tumors in the xenograft model of nude mice to VBL injection,
and significantly improve the abnormality of liver and spleen observed
in VBL injection. VBL–NPs–PEG–FA has the potential
to be the delivery carrier for VBL by enhancing the tumor-targeting
efficacy of VBL and decreasing toxicity to normal tissues.