Synthesis of ß-cyclodextrin-PEG-G molecules to delay tumor growth and application of ß-cyclodextrin-PEG-G aggregates as drug carrier.

ABSTRACT

The clinical use of many chemotherapeutic drugs is considerably greatly limited due to their serious side effects. This problem can be solved by using a low-toxic or nontoxic drug carrier that exhibits excellent performance in entrapping chemotherapeutic drugs. Accordingly, ß-cyclodextrin-PEG-guanosine (ß-CD-PEG-G) molecule was first synthesized. The molecules can self-assemble into negatively charged spherical aggregates (called ß-CD-PEG-G aggregates) that can stably exist in an aqueous solution and entrap doxorubicin (Dox) to form ß-CD-PEG-G-Dox nanomedicine. Dox encapsulation efficiency is approximately 79 ± 6.3%. Dox from ß-CD-PEG-G-Dox nanomedicine exhibits sustained release and pH responsiveness. Cell and animal experiments showed that ß-CD-PEG-G-Dox nanomedicine could effectively induce cancer cell apoptosis to exert antitumor activity. Unexpectively, the animal experiment and tissue sections demonstrated that ß-CD-PEG-G aggregates exhibit certain antitumor activity that could delay the tumor growth. Therefore, the ß-CD-PEG-G molecule has high potential as a drug carrier candidate.