Engineering a Tumor‐Acidity‐Responsive PEG‐Sheddable Nanoassembly for Combating Drug Resistance

Abstract This study presents a simple strategy to develop a tumor‐acidity responsive core‐crosslinked micellar nanoassembly capable of delivering multiple drugs to combat drug resistance. Paclitaxel (PTX) nanocrystals are prepared using D‐α‐tocopherol polyethylene glycol 1000 succinate (TPGS) as an emulsifier and cross‐linked with poly(β‐cyclodextrin) (PCD) to form the core. An acid‐labile prodrug, poly(ethylene glycol)‐doxorubicin (mPEG‐DOX), is utilized as the shell, forming a core‐shell nanoassembly (CSNA) via supramolecular interactions. The CSNA demonstrated high stability in aqueous and serum environments, with triggered shell‐detachment in response to tumor acidity. The nanomedicine exhibited superior inhibition of drug‐resistant cancer cell line MCF‐7/ADR compared to DOX or PTX alone, offering potential to overcome drug resistance in chemotherapy.

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Publication Details

Journal
Macromolecular Chemistry and Physics
Published
2025-05-02
DOI
https://doi.org/10.1002/macp.202400505
Primary Topic
Nanoparticle-Based Drug Delivery
Type
article
Field-Weighted Citation Impact
0.00

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article

Engineering a Tumor‐Acidity‐Responsive PEG‐Sheddable Nanoassembly for Combating Drug Resistance

Rui Dou, Yi Hu, Jin Xie, Jun Chen et al.
Macromolecular Chemistry and Physics
Nanoparticle-Based Drug Delivery
article

Engineering a Tumor‐Acidity‐Responsive PEG‐Sheddable Nanoassembly for Combating Drug Resistance

Rui Dou, Yi Hu, Jin Xie, Jun Chen, Jiayu Zhang, Mengxue Zhou, Hongyu Ren, Jun Ouyang
article en

Abstract

Abstract This study presents a simple strategy to develop a tumor‐acidity responsive core‐crosslinked micellar nanoassembly capable of delivering multiple drugs to combat drug resistance. Paclitaxel (PTX) nanocrystals are prepared using D‐α‐tocopherol polyethylene glycol 1000 succinate (TPGS) as an emulsifier and cross‐linked with poly(β‐cyclodextrin) (PCD) to form the core. An acid‐labile prodrug, poly(ethylene glycol)‐doxorubicin (mPEG‐DOX), is utilized as the shell, forming a core‐shell nanoassembly (CSNA) via supramolecular interactions. The CSNA demonstrated high stability in aqueous and serum environments, with triggered shell‐detachment in response to tumor acidity. The nanomedicine exhibited superior inhibition of drug‐resistant cancer cell line MCF‐7/ADR compared to DOX or PTX alone, offering potential to overcome drug resistance in chemotherapy.

Macromolecular Chemistry and PhysicsVol. 226(13)
Chinese Academy of Medical Sciences & Peking Union Medical College (CN), Peking Union Medical College Hospital (CN), Institute of High Energy Physics (CN), Chinese Academy of Agricultural Sciences (CN), Tea Research Institute (CN), First Affiliated Hospital of Zhengzhou University (CN), University of Chinese Academy of Sciences (CN), Southern Medical University (CN)
National Natural Science Foundation of China, Natural Science Foundation of Beijing Municipality, Peking Union Medical College Hospital, Basic and Applied Basic Research Foundation of Guangdong Province
Openalex Percentile: Top 95%
Nanoparticle-Based Drug Delivery
DOIOpen Access PDFOpenAlex
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