Theranostics 2021; 11(13):6334-6354. doi:10.7150/thno.59342


Multifunctional nanoplatforms co-delivering combinatorial dual-drug for eliminating cancer multidrug resistance

Xiao Wei1✉#, Mingzhu Song1,2#, Weijie Li1, Jing Huang1, Guang Yang3✉, Yi Wang4✉

1. School of Preclinical Medicine, Chengdu University, Chengdu 610106, P. R. China.
2. Evidence-Based Medicine Center, West China Hospital, Sichuan University, Chengdu, 610041, P. R. China.
3. College of Medicine, Southwest Jiaotong University, Chengdu 610031, P. R. China.
4. School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, P. R. China.
#These authors contributed equally to this work.

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Wei X, Song M, Li W, Huang J, Yang G, Wang Y. Multifunctional nanoplatforms co-delivering combinatorial dual-drug for eliminating cancer multidrug resistance. Theranostics 2021; 11(13):6334-6354. doi:10.7150/thno.59342. Available from

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Clinically, the primary cause of chemotherapy failure belongs to the occurrence of cancer multidrug resistance (MDR), which directly leads to the recurrence and metastasis of cancer along with high mortality. More and more attention has been paid to multifunctional nanoplatform-based dual-therapeutic combination to eliminate resistant cancers. In addition to helping both cargoes improve hydrophobicity and pharmacokinetic properties, increase bioavailability, release on demand and enhance therapeutic efficacy with low toxic effects, these smart co-delivery nanocarriers can even overcome drug resistance. Here, this review will not only present different types of co-delivery nanocarriers, but also summarize targeted and stimuli-responsive combination nanomedicines. Furthermore, we will focus on the recent progress in the co-delivery of dual-drug using such intelligent nanocarriers for surmounting cancer MDR. Whereas it remains to be seriously considered that there are some knotty issues in the fight against MDR of cancers via using co-delivery nanoplatforms, including limited intratumoral retention, the possible changes of combinatorial ratio under complex biological environments, drug release sequence from the nanocarriers, and subsequent free-drug resistance after detachment from the nanocarriers. It is hoped that, with the advantage of continuously developing nanomaterials, two personalized therapeutic agents in combination can be better exploited to achieve the goal of cooperatively combating cancer MDR, thus advancing the time to clinical transformation.

Keywords: co-delivery, dual-drug, multifunctional nanoplatform, multidrug resistance, cancer therapy