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<p>Nanotechnology is a promising tool to enhance the therapeutic efficacy of chemotherapy by improving drug solubility, stability, and bioavailability. Among various nano-based drug delivery systems, nanogels exhibit a high drug-loading capacity, stimuli-responsive release mechanisms, and the ability to penetrate tumor tissues effectively, therefore offering precise and sustained delivery with minimal off-target effects. In this study, a self-assembled gelatin-polyoxyethylene stearyl ether (GB) nanogel was developed as a potential nanoformulation to improve the poor solubility, rapid degradation, and instability of bare curcumin. Gelatin was used as a functional agent to increase both the drug loading efficiency and biocompatibility of polyoxyethylene stearyl ether (Brij S100) based nanogels. By chemically binding amine groups of gelatin and p-nitrophenyl chloroformate-Brij derivative, different self-assembled amphiphilic GB nanostructures are achieved by varying the grafting ratio of gelatin and Brij. The GB loading cucurmin nanogels (GB/Cur) were successfully synthesized and evaluated through <sup>1</sup>H-NMR, FT–IR, and DLS measurements. It was found that the grafting ratio of 1:6 (gelatin:Brij mass ratio) results to the optimal particles with small size (127&#xa0;nm), high stability (over 96&#xa0;h), and drug loading efficacy (70%). In addition, the GB (1:6)/Cur system had the lowest Cur release at both pH 7.4 and pH 5.5 levels, in which the Cur was triggeredly released at the tumor microenvironment (pH 5.5). The in vitro results demonstrated that GB nanogels exhibited excellent biocompatibility on healthy cells (HDF), while the GB/Cur nanogel showed superior anti-cancer activity against MCF-7 cells. Therefore, this GB nanogel system has great potential in cancer treatment, through significantly improving the therapeutic efficacy and reducing the side effects of chemotherapy. </p> Graphical abstract <p>pH-responsive gelatin-Brij nanogel to improve the bioavailability and stability of curcumin for targeted cancer therapy</p> <p></p>

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Gelatinized-polyoxyethylene (100) stearyl ether nanoformulation for enhancing distribution, bioavailability and stability of curcumin in cancer therapy

  • 期刊论文

  • 发表日期：

    2025年6月5日

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  • Dinh-Chuong Pham,
  • Van Du Cao,
  • Anh Quan Hoang,
  • Thanh Phu Nguyen,
  • Quang-Hieu Tran,
  • Hoang Duy Nguyen,
  • Binh An Pham,
  • Dinh Trung Nguyen,
  • Ngoc Quyen Tran,
  • Phuong Le Thi

摘要

Nanotechnology is a promising tool to enhance the therapeutic efficacy of chemotherapy by improving drug solubility, stability, and bioavailability. Among various nano-based drug delivery systems, nanogels exhibit a high drug-loading capacity, stimuli-responsive release mechanisms, and the ability to penetrate tumor tissues effectively, therefore offering precise and sustained delivery with minimal off-target effects. In this study, a self-assembled gelatin-polyoxyethylene stearyl ether (GB) nanogel was developed as a potential nanoformulation to improve the poor solubility, rapid degradation, and instability of bare curcumin. Gelatin was used as a functional agent to increase both the drug loading efficiency and biocompatibility of polyoxyethylene stearyl ether (Brij S100) based nanogels. By chemically binding amine groups of gelatin and p-nitrophenyl chloroformate-Brij derivative, different self-assembled amphiphilic GB nanostructures are achieved by varying the grafting ratio of gelatin and Brij. The GB loading cucurmin nanogels (GB/Cur) were successfully synthesized and evaluated through 1H-NMR, FT–IR, and DLS measurements. It was found that the grafting ratio of 1:6 (gelatin:Brij mass ratio) results to the optimal particles with small size (127 nm), high stability (over 96 h), and drug loading efficacy (70%). In addition, the GB (1:6)/Cur system had the lowest Cur release at both pH 7.4 and pH 5.5 levels, in which the Cur was triggeredly released at the tumor microenvironment (pH 5.5). The in vitro results demonstrated that GB nanogels exhibited excellent biocompatibility on healthy cells (HDF), while the GB/Cur nanogel showed superior anti-cancer activity against MCF-7 cells. Therefore, this GB nanogel system has great potential in cancer treatment, through significantly improving the therapeutic efficacy and reducing the side effects of chemotherapy.

Graphical abstract

pH-responsive gelatin-Brij nanogel to improve the bioavailability and stability of curcumin for targeted cancer therapy