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<p>This study focuses on the development, characterization, and evaluation of a novel colon-targeted drug delivery system for Irinotecan Hydrochloride (IRN HCl) using nanosuspension-loaded beads. IRN HCl, a BCS Class-II anticancer drug, faces limitations such as poor solubility, systemic side effects, and limited oral bioavailability. The nanosuspension was encapsulated in chitosan-sodium alginate-pectinate beads for ensuring colon-specific release due to microbial degradation of pectin in the colon. Characterization revealed optimal particle size (239&#xa0;nm), zeta potential (22.8&#xa0;mV), and spherical bead morphology. <i>In-vitro</i> cytotoxicity studies on HCT116 cell lines confirmed enhanced anti-cancer efficacy of the nanosuspension compared to plain IRN HCl, with a lower IC<sub>50</sub> value. <i>In- vivo</i> pharmacokinetic and biodistribution studies in rats demonstrated significantly improved bioavailability and targeted drug accumulation in the colon. These findings suggest that this system could improve the therapeutic outcomes of IRN HCl by minimizing systemic toxicity and achieving localized drug delivery.</p>

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Irinotecan Hydrochloride Nanosuspension Loaded Beads for Colon Targeting: In-Vitro and In-Vivo Characterization

  • 期刊论文

  • 发表日期：

    2026年6月1日

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  • Prince Prajapati,
  • Siddharth Thakkar,
  • Hetal Thakkar

摘要

This study focuses on the development, characterization, and evaluation of a novel colon-targeted drug delivery system for Irinotecan Hydrochloride (IRN HCl) using nanosuspension-loaded beads. IRN HCl, a BCS Class-II anticancer drug, faces limitations such as poor solubility, systemic side effects, and limited oral bioavailability. The nanosuspension was encapsulated in chitosan-sodium alginate-pectinate beads for ensuring colon-specific release due to microbial degradation of pectin in the colon. Characterization revealed optimal particle size (239 nm), zeta potential (22.8 mV), and spherical bead morphology. In-vitro cytotoxicity studies on HCT116 cell lines confirmed enhanced anti-cancer efficacy of the nanosuspension compared to plain IRN HCl, with a lower IC50 value. In- vivo pharmacokinetic and biodistribution studies in rats demonstrated significantly improved bioavailability and targeted drug accumulation in the colon. These findings suggest that this system could improve the therapeutic outcomes of IRN HCl by minimizing systemic toxicity and achieving localized drug delivery.