Theranostics 2022; 12(5):2028-2040. doi:10.7150/thno.68563 This issue

Research Paper

Self-assembly of nanomicelles with rationally designed multifunctional building blocks for synergistic chemo-photodynamic therapy

Guidong Gong1, Jiezhou Pan1, Yunxiang He1, Jiaojiao Shang1, Xiaoling Wang1, Yaoyao Zhang3, Guolin Zhang2, Fei Wang2✉, Gang Zhao1✉, Junling Guo1,4✉

1. BMI Center for Biomass Materials and Nanointerfaces, College of Biomass Science and Engineering, School of Chemistry Engineering, Sichuan University, Chengdu, Sichuan 610065, China.
2. Center for Natural Products Research, Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu, Sichuan 610041, China.
3. Key Laboratory of Birth Defects and Related of Women and Children of Ministry of Education, The Reproductive Medical Center, Department of Obstetrics and Gynecology, West China Second University Hospital, Sichuan University, Chengdu, Sichuan 610041, China.
4. State Key Laboratory of Polymer Materials Engineering, Sichuan University, Chengdu, Sichuan 610065, China.

This is an open access article distributed under the terms of the Creative Commons Attribution License ( See for full terms and conditions.
Gong G, Pan J, He Y, Shang J, Wang X, Zhang Y, Zhang G, Wang F, Zhao G, Guo J. Self-assembly of nanomicelles with rationally designed multifunctional building blocks for synergistic chemo-photodynamic therapy. Theranostics 2022; 12(5):2028-2040. doi:10.7150/thno.68563. Available from

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Graphic abstract

Rationale: The combination of photosensitizers, oxygen supply agents, and adjuvant therapy drugs in a single nano-drug delivery system for photodynamic therapy (PDT) has been showing great promises to overcome the inherent challenges of PDT for tumor treatment. However, the complicated preparation of integrating multiple components hampers their further developments. Here, we describe a self-assembly nanomicelle with rationally designed building blocks, which shows a high efficiency of synergistic chemo-photodynamic therapy in the animal modal.

Methods: The nanomicelle was prepared by a coordination-driven self-assembly based on a rationally designed ferrocene cyclopalladated compound coupled with photosensitizers and hyaluronic acid (referred to as FCP-Tph/HA). The morphology, targeting drug delivery, pharmacokinetics, hemolysis, and multimodal synergistic therapy of FCP-Tph/HA were investigated.

Results: The formation of nanomicelles presents a low hemolysis rate and a prolonged blood circulation time. FCP-Tph/HA possesses an enhanced antitumor effect in vitro through the specific binding of HA to CD44 and combining chemotherapy with oxygen self-supplying PDT. Simultaneously, the nanomicelle facilitates a significantly improved antitumor efficacy (>90% tumor regression) on a breast cancer model in vivo.

Conclusion: Our results present a modular self-assembled nanomicellar platform with synergistic chemo-photodynamic therapy for challenging PDT-based tumor treatment.

Keywords: Nanomicelle, coordination, self-assembly, oxygen self-supply, chemo-photodynamic therapy.