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<p>Colorectal cancer is a global health care burden, and the development of localized drug delivery to the colon continues to be an area of formulation interest for improving site-specific drug exposure. The purpose of this manuscript was to develop a colon-directed drug delivery system using folic acid-conjugated chitosan nanoparticles (FA-CS NPs) as a formulation strategy for local delivery of Imatinib mesylate. Synthesis of nanoparticles was done through ionic gelation and optimization through Box-Behnken design. Optimized FA-CS NPs had the following characteristics: particle size of 205.2&#xa0;nm, PDI of 0.194, zeta potential of + 17.7 mV, and entrapment efficiency of 77.71%. These nanoparticles were encapsulated into core tablets and subsequently coated with Eudragit S100, HPMC K15M, and Eudragit E100 sequentially to obtain delayed and colon-oriented release behavior under the tested in vitro conditions. In vitro release showed limited drug release at gastric pH, low drug release at intestinal pH, and over 96% release in the final enzyme-assisted colonic-stage medium. The IMT-FA-CS-NP nanoparticle system demonstrated qualitative cellular uptake and greater in vitro cytotoxic effect than the free drug in HT-29 cells under the tested conditions. The colon-targeted nanoparticle-integrated tablet should be interpreted as a proof-of-concept formulation platform rather than a validated therapeutic option for colorectal cancer; therefore, additional in vivo pharmacokinetic, biodistribution, efficacy, and safety studies will be necessary to establish translational relevance.</p> Graphical Abstract <p></p>

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Folic Acid–Conjugated Chitosan Nanoparticles for Colon-Targeted Delivery of Imatinib Mesylate

  • 期刊论文

  • 发表日期：

    2026年5月21日

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  • Bansari B. Patel,
  • Vinodkumar D. Ramani,
  • Yash D. Dudhawala,
  • Riya K. Mehta,
  • Devesh U. Kapoor

摘要

Colorectal cancer is a global health care burden, and the development of localized drug delivery to the colon continues to be an area of formulation interest for improving site-specific drug exposure. The purpose of this manuscript was to develop a colon-directed drug delivery system using folic acid-conjugated chitosan nanoparticles (FA-CS NPs) as a formulation strategy for local delivery of Imatinib mesylate. Synthesis of nanoparticles was done through ionic gelation and optimization through Box-Behnken design. Optimized FA-CS NPs had the following characteristics: particle size of 205.2 nm, PDI of 0.194, zeta potential of + 17.7 mV, and entrapment efficiency of 77.71%. These nanoparticles were encapsulated into core tablets and subsequently coated with Eudragit S100, HPMC K15M, and Eudragit E100 sequentially to obtain delayed and colon-oriented release behavior under the tested in vitro conditions. In vitro release showed limited drug release at gastric pH, low drug release at intestinal pH, and over 96% release in the final enzyme-assisted colonic-stage medium. The IMT-FA-CS-NP nanoparticle system demonstrated qualitative cellular uptake and greater in vitro cytotoxic effect than the free drug in HT-29 cells under the tested conditions. The colon-targeted nanoparticle-integrated tablet should be interpreted as a proof-of-concept formulation platform rather than a validated therapeutic option for colorectal cancer; therefore, additional in vivo pharmacokinetic, biodistribution, efficacy, and safety studies will be necessary to establish translational relevance.

Graphical Abstract