Hyaluronic acid reagent functional chitosan-PEI conjugate with AQP2-siRNA suppressed endometriotic lesion formation

Zhao MD; Cheng JL; Yan JJ; Chen FY; Sheng JZ; Sun DL; J Chen; Miao J; Zhang RJ; Zheng CH; Huang HF

Hyaluronic acid reagent functional chitosan-PEI conjugate with AQP2-siRNA suppressed endometriotic lesion formation

Zhao MD, Cheng JL, Yan JJ, Chen FY, Sheng JZ, Sun DL, J Chen, Miao J, Zhang RJ, Zheng CH, Huang HF

In: International Journal of Nanomedicine, Vol 2016, Iss default, Pp 1323-1336 (2016) · 2016 · W4299058861

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⚙ AI-generated summary by claude@2026-06, 2026-06-08 ⓘ

A hyaluronic acid-functionalized chitosan-polyethylenimine conjugate loaded with AQP2-siRNA significantly reduced endometriotic lesion size and ectopic endometrium CD44 expression in rats without toxic effects.

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⚙ AI-generated deep summary by claude@2026-06, 2026-06-10 ⓘ

This study designed a polymeric nanoparticle gene-delivery system combining hyaluronic acid functionalized chitosan-PEI with AQP2 small interfering RNA (siRNA) to target endometriotic lesions. In rat endometriosis models, the authors compared fluorescence accumulation and lesion outcomes between the HA-functionalized nanoparticle and the non-HA version, reporting greater lesion fluorescence likely due to HA-CD44 binding, along with significant reductions in endometriotic lesion size with atrophy and degeneration of ectopic endometrium after HA/AQP2-siRNA treatment. Ectopic endometrial epithelial cells from treated rats showed lower CD44 expression, and electron microscopy showed no obvious toxic effects on reproductive organs, with the paper not detailing any further limitations in the provided text. This paper is centrally about endometriosis — it tests HA-functionalized chitosan-PEI delivering AQP2-siRNA to suppress endometriotic lesion formation.

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Abstract

Meng-Dan Zhao,1 Jin-Lin Cheng,2 Jing-Jing Yan,1 Feng-Ying Chen,1 Jian-Zhong Sheng,3 Dong-Li Sun,1 Jian Chen,4 Jing Miao,4 Run-Ju Zhang,1 Cai-Hong Zheng,1 He-Feng Huang1,5 1Women’s Hospital, School of Medicine, Zhejiang University, Hangzhou, 2State Key Laboratory for Diagnosis and Treatment of Infectious Diseases, Collaborative Innovation Center for Diagnosis and Treatment of Infectious Diseases, The First Affiliated Hospital, College of Medicine, 3Department of Pathophysiology, School of Medicine, 4The First Affiliated Hospital, College of Medicine, Zhejiang University, Hangzhou, 5International Peace Maternity and Child Health Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai, People’s Republic of China Abstract: To identify a new drug candidate for treating endometriosis which has fewer side effects, a new polymeric nanoparticle gene delivery system consisting of polyethylenimine-grafted chitosan oligosaccharide (CSO-PEI) with hyaluronic acid (HA) and small interfering RNA (siRNA) was designed. There was no obvious difference in sizes observed between (CSO-PEI/siRNA)HA and CSO-PEI/siRNA, but the fluorescence accumulation in the endometriotic lesion was more significant for (CSO-PEI/siRNA)HA compared with CSO-PEI/siRNA due to the specific binding of HA to CD44. In addition, the (CSO-PEI/siRNA)HA nanoparticle gene therapy significantly decreased the endometriotic lesion sizes with atrophy and degeneration of the ectopic endometrium. The epithelial cells of ectopic endometrium from rat models of endometriosis showed a significantly lower CD44 expression than control after treatment with (CSO-PEI/siRNA)HA. Furthermore, observation under an electron microscope showed no obvious toxic effect on the reproductive organs. Therefore, (CSO-PEI/siRNA)HA gene delivery system can be used as an effective method for the treatment of endometriosis. Keywords: chitosan-PEI, hyaluronic acid, AQP2-siRNA, endometriosis, targeted therapy

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