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Aim <p>The present research aimed to develop controlled-release tablets based on microparticles of losartan potassium using polymers such as Ethocel 7 fine particle (FP), Ethocel 10 FP, Ethocel 100 FP, Eudragit S100, and Carbopol 934 NFP.</p> Methodology <p>Microparticles were prepared using the solvent evaporation and coacervation methods and were evaluated for entrapment efficiency, percentage yield, percentage drug loading, particle size, and surface morphology using scanning electron microscopy. The prepared microparticles were directly compressed into tablets and evaluated for in-vitro dissolution studies. Various kinetic models were applied to analyze drug-release data, and the difference factor (f₁) was used to compare the dissolution profiles with a reference formulation.</p> Results <p>The drug entrapment efficiency of the microparticles ranged from 78.38 ± 0.08% to 91.66 ± 0.17%. The percentage yield ranged from 75.23 ± 0.48% to 87.98 ± 0.32%, while percentage drug loading ranged from 23.67 ± 0.26% to 29.01 ± 0.32%. The particle size of the microparticles ranged from 120.2 ± 0.15 to 156.4 ± 0.23&#xa0;µm, and the particles exhibited rough surface morphology. The controlled-release tablets showed excellent physical characteristics and complied with USP limits. The tablets extended drug release for up to 24&#xa0;h. Comparison studies revealed that the release profile was not within the acceptable f₁ limits (1–15). Drug release followed pseudo-zero-order kinetics and occurred through pseudo-swelling or erosion and anomalous non-Fickian diffusion mechanisms.</p> Conclusion <p>It can be concluded that the novel microparticle-based tablets have the potential to be used as once-daily dosage forms, thereby reducing dosing frequency and improving patient compliance. </p>

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Formulation and Evaluation of Losartan Potassium Microparticles Loaded Controlled-Release Tablets: An In-Vitro Perspective

  • 期刊论文

  • 发表日期：

    2026年4月14日

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  • Kamran Ahmad Khan,
  • Ashfaq Ahmad,
  • Muhammad Israr,
  • Saima Mahmood,
  • Farman Shah,
  • Naveed Ullah,
  • Fida Muhammad,
  • Anam Adil,
  • Sami ul Haq,
  • Haroon Khan

摘要

Aim

The present research aimed to develop controlled-release tablets based on microparticles of losartan potassium using polymers such as Ethocel 7 fine particle (FP), Ethocel 10 FP, Ethocel 100 FP, Eudragit S100, and Carbopol 934 NFP.

Methodology

Microparticles were prepared using the solvent evaporation and coacervation methods and were evaluated for entrapment efficiency, percentage yield, percentage drug loading, particle size, and surface morphology using scanning electron microscopy. The prepared microparticles were directly compressed into tablets and evaluated for in-vitro dissolution studies. Various kinetic models were applied to analyze drug-release data, and the difference factor (f₁) was used to compare the dissolution profiles with a reference formulation.

Results

The drug entrapment efficiency of the microparticles ranged from 78.38 ± 0.08% to 91.66 ± 0.17%. The percentage yield ranged from 75.23 ± 0.48% to 87.98 ± 0.32%, while percentage drug loading ranged from 23.67 ± 0.26% to 29.01 ± 0.32%. The particle size of the microparticles ranged from 120.2 ± 0.15 to 156.4 ± 0.23 µm, and the particles exhibited rough surface morphology. The controlled-release tablets showed excellent physical characteristics and complied with USP limits. The tablets extended drug release for up to 24 h. Comparison studies revealed that the release profile was not within the acceptable f₁ limits (1–15). Drug release followed pseudo-zero-order kinetics and occurred through pseudo-swelling or erosion and anomalous non-Fickian diffusion mechanisms.

Conclusion

It can be concluded that the novel microparticle-based tablets have the potential to be used as once-daily dosage forms, thereby reducing dosing frequency and improving patient compliance.