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Purpose <p>Current research is focused on the preparation of pH-responsive microparticles using naturally occurring swellable polysaccharide, i.e., glucuronoxylan (GX), for zero-order drug release.</p> Methods <p>Nine different formulations were prepared by varying the concentrations of sodium alginate (Na-Alg), GX, and crosslinker, i.e., ferrous sulphate. The microparticles were characterized through Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). The flowability parameters, drug loading (DL), encapsulation efficiency (EE), and particle size were calculated. The dynamic swelling and swelling kinetics of microparticles at pH 1.2, 6.8, and 7.4, and in deionized water (DW), and pH-responsive on/off switching (swelling/deswelling) at pH 7.4/1.2 were determined. The esomeprazole release study was conducted under the conditions (pH and transit time) that mimic the gastrointestinal tract (GIT).</p> Results <p>The SEM images showed the wrinkled and porous surfaces of the microparticles. The DL, EE, and particle size of all the formulations are in the range from 31 to 49%, 43–73%, and 625–890&#xa0;μm, respectively. The swelling of microparticles followed the pattern: DW &gt; pH 7.4 &gt; pH 6.8 &gt; pH 1.2 and showed on/off switching behaviour at pH 7.4/1.2. The negligible drug release was observed at pH 1.2. Whereas, a sustained release was witnessed at pH 6.8 for 8–12&#xa0;h, followed the significant zero-order kinetics and super case-II transport mechanism.</p> Conclusion <p>The DL, EE, and drug release are dependent and directly proportional to the concentration of GX and the crosslinker. This novel ferrous sulphate crosslinked Na-Alg and GX-based microparticle can be a potential pH-responsive drug delivery system for acid-labile drugs.</p>

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Formulation Design of Glucuronoxylan-Based Stimuli-Responsive Microparticles for Zero-Order Drug Delivery

  • 期刊论文

  • 发表日期：

    2026年2月5日

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  • Saleha Babar,
  • Fatima Akbar Sheikh,
  • Syed Nasir Abbas Bukhari,
  • Muhammad Tahir Haseeb,
  • Arshad Ali,
  • Nisar Ul Khaliq,
  • Ranya Abdulrahman Alafar,
  • Mohamed Abdelwahab Abdelgawad,
  • Ameeduzzafar Zafar,
  • Naveed Ahmad

摘要

Purpose

Current research is focused on the preparation of pH-responsive microparticles using naturally occurring swellable polysaccharide, i.e., glucuronoxylan (GX), for zero-order drug release.

Methods

Nine different formulations were prepared by varying the concentrations of sodium alginate (Na-Alg), GX, and crosslinker, i.e., ferrous sulphate. The microparticles were characterized through Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). The flowability parameters, drug loading (DL), encapsulation efficiency (EE), and particle size were calculated. The dynamic swelling and swelling kinetics of microparticles at pH 1.2, 6.8, and 7.4, and in deionized water (DW), and pH-responsive on/off switching (swelling/deswelling) at pH 7.4/1.2 were determined. The esomeprazole release study was conducted under the conditions (pH and transit time) that mimic the gastrointestinal tract (GIT).

Results

The SEM images showed the wrinkled and porous surfaces of the microparticles. The DL, EE, and particle size of all the formulations are in the range from 31 to 49%, 43–73%, and 625–890 μm, respectively. The swelling of microparticles followed the pattern: DW > pH 7.4 > pH 6.8 > pH 1.2 and showed on/off switching behaviour at pH 7.4/1.2. The negligible drug release was observed at pH 1.2. Whereas, a sustained release was witnessed at pH 6.8 for 8–12 h, followed the significant zero-order kinetics and super case-II transport mechanism.

Conclusion

The DL, EE, and drug release are dependent and directly proportional to the concentration of GX and the crosslinker. This novel ferrous sulphate crosslinked Na-Alg and GX-based microparticle can be a potential pH-responsive drug delivery system for acid-labile drugs.