Cross-Linked Pillar[6]arene Nanosponges Fabricated by the Use of a Supra-Amphiphilic Template: Cargo Encapsulation and Overcoming Multidrug Resistance

We report a general fabrication method for water-soluble pillar[ n ]arene nanosponges (NS) by the use of a supra-amphiphilic template. For the first time, a supra-amphiphilic template is used to conveniently control the size of host molecule-based NS. The intrinsic cavity of water-soluble pillar[6]arene could stably encapsulate dyes (acridine orange and indocyanine green) and antitumor drugs (doxorubicin hydrochloride and mitoxantrone) by host–guest interaction. NS could deliver antitumor drugs to cancer cells. Multidrug resistance (MDR) of cancer cells (MCF-7/ADR) is overcome by the use of NS with a ninefold reduction in the IC 50 value compared to that of the free drug (3.4 μM vs 34.4 μM). Mechanistic studies show that stable encapsulation of the antitumor drug is the reason to overcome MDR.