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<p>The present investigation aimed to develop, and optimize telmisartan-loaded colon-targeted liposomes (TelLp). Optimized TelLp were coated with thiolated chitosan (Tc), a mucoadhesive and biodegradable polymer, and Eudragit S100 (E-Tc-TelLp), a pH-sensitive polymer. Liposomes were prepared using the thin-film hydration technique. A three-factor central composite design was employed for optimization of TelLp, with three independent variables: the amounts of egg phosphatidylcholine, cholesterol, and telmisartan in the formulation. The effects of these variables on two response variables, particle size distribution (PSD) and percentage entrapment efficiency (% EE), were assessed. The optimized TelLp exhibited a PSD of 256.2 ± 12.23&#xa0;nm, a zeta potential (ZP) of -21.5 ± 1.3 mV, and % EE of 68.89 ± 4.11&#xa0;%. Moreover, the PSD, ZP, and % EE of E-Tc-TelLP was found to be 416.6 ± 23.64&#xa0;nm, -37.6 ± 1.12, and % EE of 66.76 ± 2.42&#xa0;%, respectively. The in vitro dissolution studies of E-Tc-TelLp demonstrated drug release of 42.79 ± 2.23&#xa0;% in pH 1.2 and 82.43 ± 5.9&#xa0;% in pH 7.4 over 72&#xa0;h, respectively. Sustained release was observed at pH 7.4. The E-Tc-TelLp showed significant amelioration in inflammation in an oxazolone (OXA)-induced inflammatory bowel disease (IBD) animal model, as evidenced through the improvements in the disease activity index (DAI), colon length and weight, and histopathological evaluation. Furthermore, statistically significant reduction in inflammatory markers, including C-reactive protein (CRP) and lactate dehydrogenase (LDH), was observed in telmisartan-treated animal groups.</p> Graphical Abstract <p></p>

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Novel Colon-Targeted Liposomes of Telmisartan as a Potential Therapeutic Modality for the Treatment of Inflammatory Bowel Disease

  • 期刊论文

  • 发表日期：

    2025年12月17日

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  • Dhiraj P. Sonje,
  • Kalpesh R. Patil,
  • Suraj R. Chaudhari,
  • Chetna B. Rajput,
  • Sambhaji S. Khot,
  • Harshal P. Patil,
  • Chandragouda R. Patil,
  • Prajwala R. Khapale,
  • Ashok S. Narute,
  • Pravin S. Chinchole,
  • Nilesh Kulkarni

摘要

The present investigation aimed to develop, and optimize telmisartan-loaded colon-targeted liposomes (TelLp). Optimized TelLp were coated with thiolated chitosan (Tc), a mucoadhesive and biodegradable polymer, and Eudragit S100 (E-Tc-TelLp), a pH-sensitive polymer. Liposomes were prepared using the thin-film hydration technique. A three-factor central composite design was employed for optimization of TelLp, with three independent variables: the amounts of egg phosphatidylcholine, cholesterol, and telmisartan in the formulation. The effects of these variables on two response variables, particle size distribution (PSD) and percentage entrapment efficiency (% EE), were assessed. The optimized TelLp exhibited a PSD of 256.2 ± 12.23 nm, a zeta potential (ZP) of -21.5 ± 1.3 mV, and % EE of 68.89 ± 4.11 %. Moreover, the PSD, ZP, and % EE of E-Tc-TelLP was found to be 416.6 ± 23.64 nm, -37.6 ± 1.12, and % EE of 66.76 ± 2.42 %, respectively. The in vitro dissolution studies of E-Tc-TelLp demonstrated drug release of 42.79 ± 2.23 % in pH 1.2 and 82.43 ± 5.9 % in pH 7.4 over 72 h, respectively. Sustained release was observed at pH 7.4. The E-Tc-TelLp showed significant amelioration in inflammation in an oxazolone (OXA)-induced inflammatory bowel disease (IBD) animal model, as evidenced through the improvements in the disease activity index (DAI), colon length and weight, and histopathological evaluation. Furthermore, statistically significant reduction in inflammatory markers, including C-reactive protein (CRP) and lactate dehydrogenase (LDH), was observed in telmisartan-treated animal groups.

Graphical Abstract