Background <p>Sofosbuvir (SBV) is a BCS class III antiviral drug used to treat hepatitis C, with limitations including poor permeability and rapid clearance. To overcome these potential limitations, a pH sensitive hydrogel microparticle system was formulated.</p> Methods <p>HPMC/chitosan-co-poly (MAA/AMPS) hydrogel microparticles were prepared via free radical polymerization. Formulated batches were subjected to equilibrium swelling, in-vitro drug release, MTT assay, permeability studies and toxicological evaluation. Functional assessments included equilibrium swelling, in vitro release studies, permeability tests, MTT assay, and in vivo toxicological evaluation.</p> Results <p>Optimized batch (HCM 10) depicted maximum pH responsive swelling (90.69%) with augmented drug release (95.45%) in basic pH and insignificant release was reported at acidic pH (8.80%). SBV loading in all developed formulations ranged from 60.31% to 81.02%. Eudragit and sodium lauryl sulfate coating aids in improving permeability of SBV i.e. 56.61% up to 8&#xa0;h. MTT assay and toxicity studies affirms hydrogel safety.</p> Conclusion <p>The formulated HPMC/chitosan-co-poly (MAA/AMPS) hydrogel microparticles promising for pH sensitive delivery of SBV thereby improving permeability as well as promising for sustained SBV release.</p>

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Sofosbuvir containing ph-responsive hydrogel microparticulate system: design, characterization, and biocompatibility assessment

  • Muhammad Aun,
  • Muhammad Umar Ashraf,
  • Salim Albukhaty,
  • Umaira Rehman,
  • Asif Mahmood,
  • Asma Razzaq,
  • Hira Ijaz,
  • Rai Muhammad Sarfraz,
  • Mohamed M. Salem,
  • Areej Alsubaie,
  • Mounir M. Bekhit

摘要

Background

Sofosbuvir (SBV) is a BCS class III antiviral drug used to treat hepatitis C, with limitations including poor permeability and rapid clearance. To overcome these potential limitations, a pH sensitive hydrogel microparticle system was formulated.

Methods

HPMC/chitosan-co-poly (MAA/AMPS) hydrogel microparticles were prepared via free radical polymerization. Formulated batches were subjected to equilibrium swelling, in-vitro drug release, MTT assay, permeability studies and toxicological evaluation. Functional assessments included equilibrium swelling, in vitro release studies, permeability tests, MTT assay, and in vivo toxicological evaluation.

Results

Optimized batch (HCM 10) depicted maximum pH responsive swelling (90.69%) with augmented drug release (95.45%) in basic pH and insignificant release was reported at acidic pH (8.80%). SBV loading in all developed formulations ranged from 60.31% to 81.02%. Eudragit and sodium lauryl sulfate coating aids in improving permeability of SBV i.e. 56.61% up to 8 h. MTT assay and toxicity studies affirms hydrogel safety.

Conclusion

The formulated HPMC/chitosan-co-poly (MAA/AMPS) hydrogel microparticles promising for pH sensitive delivery of SBV thereby improving permeability as well as promising for sustained SBV release.