Scholarlink

Background <p>Azithromycin (ATM) has limitations, such as poor oral bioavailability and gastrointestinal (GI) side effects that restrict its widespread application.</p> Objective <p>To develop a localized hydroxy propyl β-cyclodextrin (HP-βCD) inclusion complex-based in situ pH-responsive mucoadhesive gel of azithromycin (ATM) and evaluate its performance for the treatment of upper respiratory tract infections (URTIs).</p> Methods <p>According to the phase solubility diagram, the ATM HP-βCD complex was prepared and analyzed by FT-IR, DSC, and SEM. Then, using a quality-by-design approach, pH-responsive in-situ gel was prepared. It was characterized in terms of their gelling capacity, pH, spreadability, swelling index, rheological properties and antimicrobial potential.</p> Results <p>ATM HP- βCD complex 20-fold increased solubility of ATM, i.e., 49.84 ± 1.39&#xa0;µg/mL with improved dissolution profile compared to pure ATM. Optimized formulation characterized by its gelation pH (6.7), time (1.59&#xa0;min), and viscosity (1607.9&#xa0;Pa.s). The developed gel showed a good spreadability index (322.6 ± 0.5%), swelling index (98.26 ± 1.54% after 10&#xa0;h) and mucoadhesive strength (589&#xa0;g/cm<sup>2</sup>). Also, it exhibits a sustained drug release profile for 12&#xa0;h(94 ± 1.37%) and a broader zone of <i>Staphylococcus aureus</i> growth inhibition (31 ± 3.54&#xa0;mm).</p> Conclusion <p>The developed mucoadhesive in situ gels demonstrated promising in vivo performance, primarily due to their effective antimicrobial activity. In vivo, local retention studies confirmed that the formulations adhered to the throat mucosa and remained in place for up to 24&#xa0;h after application. The findings presented here suggested that this localized delivery system could serve as a useful strategy for improving the therapeutic effects of ATM against URTIs.</p> Graphical Abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Optimization and preparation of in-situ mucoadhesive gel of azithromycin hydroxypropyl-β-cyclodextrin inclusion complex against upper respiratory tract infections

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年4月29日

查看全文
  • Jitu Halder,
  • Shuvam Mishra,
  • Ivy Saha,
  • Ajit Mishra,
  • Ritu Mahanty,
  • Vineet Kumar Rai,
  • Deepak Pradhan,
  • Rakesh Kumar Sahoo,
  • Salim Manoharadas,
  • Muralidhar Tata,
  • Biswakanth Kar,
  • Goutam Ghosh,
  • Goutam Rath

摘要

Background

Azithromycin (ATM) has limitations, such as poor oral bioavailability and gastrointestinal (GI) side effects that restrict its widespread application.

Objective

To develop a localized hydroxy propyl β-cyclodextrin (HP-βCD) inclusion complex-based in situ pH-responsive mucoadhesive gel of azithromycin (ATM) and evaluate its performance for the treatment of upper respiratory tract infections (URTIs).

Methods

According to the phase solubility diagram, the ATM HP-βCD complex was prepared and analyzed by FT-IR, DSC, and SEM. Then, using a quality-by-design approach, pH-responsive in-situ gel was prepared. It was characterized in terms of their gelling capacity, pH, spreadability, swelling index, rheological properties and antimicrobial potential.

Results

ATM HP- βCD complex 20-fold increased solubility of ATM, i.e., 49.84 ± 1.39 µg/mL with improved dissolution profile compared to pure ATM. Optimized formulation characterized by its gelation pH (6.7), time (1.59 min), and viscosity (1607.9 Pa.s). The developed gel showed a good spreadability index (322.6 ± 0.5%), swelling index (98.26 ± 1.54% after 10 h) and mucoadhesive strength (589 g/cm2). Also, it exhibits a sustained drug release profile for 12 h(94 ± 1.37%) and a broader zone of Staphylococcus aureus growth inhibition (31 ± 3.54 mm).

Conclusion

The developed mucoadhesive in situ gels demonstrated promising in vivo performance, primarily due to their effective antimicrobial activity. In vivo, local retention studies confirmed that the formulations adhered to the throat mucosa and remained in place for up to 24 h after application. The findings presented here suggested that this localized delivery system could serve as a useful strategy for improving the therapeutic effects of ATM against URTIs.

Graphical Abstract