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<p>One of the main challenges in using antibiotics to treat Inflammatory Bowel Disease (IBD), especially Crohn’s Disease (CD), is the direct delivery of the drug to the inflamed site of the intestine, which inevitably leads to an increased dosage and systemic side effects. Concerning these challenges, Starch based Nano-Porous (SNP) aerogels were developed due to their efficiency in delivering drugs to achieve the desired therapeutic effect while minimizing potential side effects. Specifically, after incorporating clarithromycin into SNP aerogels, pH-sensitive aerogels were developed using a trehalose coating to remain intact in the acidic stomach environment and prevent early drug release. The formulated drug-loaded aerogels were characterized and evaluated in terms of their physicochemical properties, solid-state behavior, mucoadhesive and cytotoxicity properties. The results showed that an average pore size of 150&#xa0;nm based on Scanning Electron Microscopy (SEM) and drug loading capacity was 83.23%. Brunauer-Emmett-Telletr (BET) analysis demonstrated a significant decrease in specific surface area and total pore volume after drug loading and coating. Spectroscopic analysis using Fourier Transform Infrared Spectroscopy (FTIR) confirmed the presence of trehalose and clarithromycin in the coated aerogels. Additionally, the amorphous nature of the loaded drug was confirmed by X-ray Diffraction (XRD). The release graphs of clarithromycin loaded in aerogels showed that the trehalose coating limits drug release in mimicked acidic pH environments. Mucoadhesive properties have been given to the final formulation. Trehalose coated aerogels exhibited greater mucoadhesive strength (11%) than those uncoated (5%). The antibacterial feature of clarithromycin based on the findings of microbiological tests, persist even after undergoing drug loading and coating processes. Furthermore, cytotoxicity studies showed that the trehalose-coated SNP aerogel formulation was cytocompatible in vitro and could be a suitable option as an intestinal drug delivery system.</p> Graphical abstract <p></p>

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Developing mucoadhesive nano-porous aerogels to targeted delivery of clarithromycin for Crohn’s disease infection

  • 期刊论文

  • 发表日期：

    2025年11月4日

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  • Zhila Izadi,
  • Fatemeh Narimani,
  • Amirhossein Merati,
  • Shirin Shojaei,
  • Babak Haghshenas,
  • Roshanak Amirian,
  • Shahla Mirzaeei,
  • Lobat Tayebi,
  • Soroor Sadegh Malvajerd

摘要

One of the main challenges in using antibiotics to treat Inflammatory Bowel Disease (IBD), especially Crohn’s Disease (CD), is the direct delivery of the drug to the inflamed site of the intestine, which inevitably leads to an increased dosage and systemic side effects. Concerning these challenges, Starch based Nano-Porous (SNP) aerogels were developed due to their efficiency in delivering drugs to achieve the desired therapeutic effect while minimizing potential side effects. Specifically, after incorporating clarithromycin into SNP aerogels, pH-sensitive aerogels were developed using a trehalose coating to remain intact in the acidic stomach environment and prevent early drug release. The formulated drug-loaded aerogels were characterized and evaluated in terms of their physicochemical properties, solid-state behavior, mucoadhesive and cytotoxicity properties. The results showed that an average pore size of 150 nm based on Scanning Electron Microscopy (SEM) and drug loading capacity was 83.23%. Brunauer-Emmett-Telletr (BET) analysis demonstrated a significant decrease in specific surface area and total pore volume after drug loading and coating. Spectroscopic analysis using Fourier Transform Infrared Spectroscopy (FTIR) confirmed the presence of trehalose and clarithromycin in the coated aerogels. Additionally, the amorphous nature of the loaded drug was confirmed by X-ray Diffraction (XRD). The release graphs of clarithromycin loaded in aerogels showed that the trehalose coating limits drug release in mimicked acidic pH environments. Mucoadhesive properties have been given to the final formulation. Trehalose coated aerogels exhibited greater mucoadhesive strength (11%) than those uncoated (5%). The antibacterial feature of clarithromycin based on the findings of microbiological tests, persist even after undergoing drug loading and coating processes. Furthermore, cytotoxicity studies showed that the trehalose-coated SNP aerogel formulation was cytocompatible in vitro and could be a suitable option as an intestinal drug delivery system.

Graphical abstract