Scholarlink

Purpose <p>This study aimed to develop mucoadhesive polymeric nanoparticles of fexofenadine hydrochloride for ocular delivery to improve precorneal retention, corneal permeation, and therapeutic efficacy in allergic conjunctivitis. The work addressed limitations of conventional eye drops, including rapid elimination and poor bioavailability.</p> Methods <p>Nanoparticles were prepared using a modified nanoprecipitation method with Eudragit RL 100 and polyvinyl alcohol (PVA). Formulations were evaluated for particle size, PDI, zeta potential, entrapment efficiency, and morphology (SEM, DLS). In vitro release studies and kinetic modelling were performed to assess release behaviour. Mucoadhesion was measured via mucin binding, while ex vivo permeation across excised goat cornea assessed transcorneal transport. Hemolysis assays evaluated biocompatibility.</p> Results <p>The optimised formulation (F4) exhibited a particle size of 165.9 nm, PDI of 0.232, and zeta potential of −14.8 mV, with 71% entrapment efficiency. SEM confirmed spherical particles (91–97 nm in dry state), with DLS showing hydrated swelling to 215.6 nm. The formulation demonstrated sustained release (~90% in 6 h) following non-Fickian kinetics. Mucoadhesion was strong, with 84.10% mucin binding. Ex vivo studies revealed a permeability coefficient of 1.09 cm/h, nearly ten times higher than that of a pure drug solution. Hemolysis remained below 5%, confirming safety.</p> Conclusion <p>The developed mucoadhesive nanoparticulate system offers a promising platform for controlled and enhanced ocular delivery of fexofenadine hydrochloride, capable of improving drug retention and permeability. However, in vivo pharmacokinetic and therapeutic evaluations are warranted to confirm the ex vivo findings and establish clinical applicability.</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

Mucoadhesive Polymeric Nanoparticles of Fexofenadine Hydrochloride for Ocular Delivery: Formulation, Characterisation, and Enhanced Permeation Studies

  • 期刊论文

  • 发表日期：

    2025年12月20日

查看全文
  • Pallavi Sarkar,
  • Madhuri Desavathu,
  • Smita Jain,
  • Ashwini Kumar Mishra,
  • Ravi Sankara Reddy,
  • Pankaj Kumar Sah

摘要

Purpose

This study aimed to develop mucoadhesive polymeric nanoparticles of fexofenadine hydrochloride for ocular delivery to improve precorneal retention, corneal permeation, and therapeutic efficacy in allergic conjunctivitis. The work addressed limitations of conventional eye drops, including rapid elimination and poor bioavailability.

Methods

Nanoparticles were prepared using a modified nanoprecipitation method with Eudragit RL 100 and polyvinyl alcohol (PVA). Formulations were evaluated for particle size, PDI, zeta potential, entrapment efficiency, and morphology (SEM, DLS). In vitro release studies and kinetic modelling were performed to assess release behaviour. Mucoadhesion was measured via mucin binding, while ex vivo permeation across excised goat cornea assessed transcorneal transport. Hemolysis assays evaluated biocompatibility.

Results

The optimised formulation (F4) exhibited a particle size of 165.9 nm, PDI of 0.232, and zeta potential of −14.8 mV, with 71% entrapment efficiency. SEM confirmed spherical particles (91–97 nm in dry state), with DLS showing hydrated swelling to 215.6 nm. The formulation demonstrated sustained release (~90% in 6 h) following non-Fickian kinetics. Mucoadhesion was strong, with 84.10% mucin binding. Ex vivo studies revealed a permeability coefficient of 1.09 cm/h, nearly ten times higher than that of a pure drug solution. Hemolysis remained below 5%, confirming safety.

Conclusion

The developed mucoadhesive nanoparticulate system offers a promising platform for controlled and enhanced ocular delivery of fexofenadine hydrochloride, capable of improving drug retention and permeability. However, in vivo pharmacokinetic and therapeutic evaluations are warranted to confirm the ex vivo findings and establish clinical applicability.