Scholarlink

Purpose <p>This study aimed to develop an Amphotericin B nanocrystal formulation (AMB-NCs) using Pluronic<sup>®</sup> F127 as a stabilizer to enhance solubility and bioavailability. The optimized AMB-NCs were incorporated into a dissolving microneedle (DMN) system to improve localized drug delivery and extend the duration of AMB therapy in oral mucosal tissues.</p> Methods <p>AMB nanocrystals (NCs) were prepared using a top-down approach and analyzed for particle size, polydispersity index, drug release, and in vitro antifungal activity. The DMN system, composed of polyvinylpyrrolidone (PVP) and polyvinyl alcohol (PVA), was evaluated for mechanical strength, insertion efficiency, drug content, and dissolution time. Ex vivo and in vivo studies were performed in a fungal infection model.</p> Results <p>Optimized AMB-NCs formulated with 1.0% w/v Pluronic F127 achieved the desired particle size with a polydispersity index below 0.25 and an in vitro drug release rate of 83.82%. When integrated into the DMN system, the formulation exhibited high drug recovery (99.77%) and effective AMB permeation and retention in porcine oral mucosa. In both in vitro and ex vivo Candida albicans infection models, AMB-NCs demonstrated enhanced antifungal activity, achieving a 99% fungal killing rate and a 71% reduction in Candida albicans colonies in vivo after 48&#xa0;h, surpassing the performance of pure AMB and AMB nanocrystals in buccal patches.</p> Conclusion <p>The AMB nanocrystal formulation, integrated into a DMN system, shows promise for improving therapeutic outcomes for oral candidiasis through transmucosal delivery. Further studies are warranted to evaluate stability, safety, and user comfort before clinical trials.</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

Amphotericin B nanocrystals integrated with bilayer dissolving microneedles: a new strategy for transmucosal delivery of amphotericin B to improve the effectiveness of oral candidiasis therapy

  • 期刊论文

  • 发表日期：

    2025年2月10日

查看全文
  • Muh. Bisfain Asaf,
  • Khairiyah,
  • Irfan Kurniawan,
  • Nurafni Annisa Achmad,
  • Rachmatya W. Tuna,
  • Achmad Himawan,
  • Latifah Rahman,
  • Aliyah,
  • Rina Agustina,
  • Juan Dominguez-Robles,
  • Sartini,
  • Andi Dian Permana

摘要

Purpose

This study aimed to develop an Amphotericin B nanocrystal formulation (AMB-NCs) using Pluronic® F127 as a stabilizer to enhance solubility and bioavailability. The optimized AMB-NCs were incorporated into a dissolving microneedle (DMN) system to improve localized drug delivery and extend the duration of AMB therapy in oral mucosal tissues.

Methods

AMB nanocrystals (NCs) were prepared using a top-down approach and analyzed for particle size, polydispersity index, drug release, and in vitro antifungal activity. The DMN system, composed of polyvinylpyrrolidone (PVP) and polyvinyl alcohol (PVA), was evaluated for mechanical strength, insertion efficiency, drug content, and dissolution time. Ex vivo and in vivo studies were performed in a fungal infection model.

Results

Optimized AMB-NCs formulated with 1.0% w/v Pluronic F127 achieved the desired particle size with a polydispersity index below 0.25 and an in vitro drug release rate of 83.82%. When integrated into the DMN system, the formulation exhibited high drug recovery (99.77%) and effective AMB permeation and retention in porcine oral mucosa. In both in vitro and ex vivo Candida albicans infection models, AMB-NCs demonstrated enhanced antifungal activity, achieving a 99% fungal killing rate and a 71% reduction in Candida albicans colonies in vivo after 48 h, surpassing the performance of pure AMB and AMB nanocrystals in buccal patches.

Conclusion

The AMB nanocrystal formulation, integrated into a DMN system, shows promise for improving therapeutic outcomes for oral candidiasis through transmucosal delivery. Further studies are warranted to evaluate stability, safety, and user comfort before clinical trials.