Tumor pH-sensitive PLLA-based Microsphere with Acid Cleavable Acetal Bonds on Backbone for Efficient Localized Chemotherapy.

Tumor pH-sensitive PLLA-based Microsphere with Acid Cleavable Acetal Bonds on Backbone for Efficient Localized Chemotherapy. Biomacromolecules. 2018 Jun 08;: Authors: Li J, Zhang X, Zhao M, Wu L, Luo K, Pu Y, He B Abstract Nanoparticles- and microspheres-based drug delivery systems (DDSs) have attracted wide attention in cancer therapy; those DDSs that are responsive to tumor environment can selectively identify tumor and normal tissues and therefore have shown enhanced anticancer efficacy and alleviated systemic toxicity. Here, tumor pH-sensitive polymeric microsphere, which is prepared by multiblock poly(L-lactide) with pH-sensitive acetal bonds in the backbone, are employed to efficiently load water-soluble anticancer drug doxorubicin hydrochloride (DOX∙HCl, drug loading content: ~10%). The pH-sensitive DOX-loaded hollow microspheres were in the size range 2-10 m and exhibited acid-accelerated degradation of polymer matrix and drug release, and thereby efficient in vitro cancer cell inhibition. The microspheres were further intratumorally injected into breast tumor-bearing mice and the in vivo anticancer experiment showed that pH-sensitive DOX-loaded microsphere showed better antitumor efficiency and prolonged life-span than its counterpart that does not have pH-responsive property. Moreover, negligible organ toxicity, especially cardiotoxicity that generally exists in DOX-involved chemotherapy where DOX is administrated by i...
Source: Biomacromolecules - Category: Biochemistry Authors: Tags: Biomacromolecules Source Type: research