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<p>In-situ nasal gel for treating Cerebral Arteriosclerosis (CA) has been developed to deliver tolperisone directly to the brain, bypassing the blood-brain barrier (bbb) and first-pass metabolism, resulting improving CNS bioavailability. A 3<sup>2</sup> factorial design was employed to optimize the formulation using varying thermosensitive polymer (Poloxamer 407) and mucoadhesive polymer (HPMC/K4M) concentrations to evaluate the gelation temperature and mucoadhession. Nasal thermogelling System exhibit significant results in the range, % drug content 95.14 ± 0.29–98.70 ± 0.5, gelation time &lt;1 min, gelation temperature 32 ± 0.32–36.2 ± 0.29, gel strength &lt; 36 ± 0.22 seconds, and mucoadhesive strength &lt;3621 ± 30 dyn/cm<sup>2</sup>. The cumulative % tolperisone release for formulations F3, F6, and F9, each with different HPMC:K4M concentrations (0.2%, 0.4%, 0.6% w/v) but a constant 20% w/v of Poloxamer 407, was 87.8%, 82.65%, and 74.65%, respectively, after 8 h. This indicates that higher HPMC K4M concentrations resulted in reduced drug release. At lower HPMC K4M concentrations, higher flux values were observed, and at higher concentrations, flux increased due to polymer cross-linking. Optimized batches F3, F6, and F9 initially showed higher flux of 0.481 ± 0.023, 0.441 ± 0.019, and 0.316 ± 0.015, respectively. The histopathological analysis confirmed the formulation’s safety, demonstrating its potential for targeted and effective CA treatment with lower systemic toxicity than oral administration.</p> Graphical Abstract <p></p>

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Design and characterization of a nasal thermogelling system loaded with tolperisone for the treatment of cerebral arteriosclerosis through the nose to brain delivery system

  • 期刊论文

  • 发表日期：

    2025年9月1日

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  • Vishal B. Gaikwad,
  • Paresh R. Mahaparale,
  • Mohd Sayeed Shaikh,
  • Rijawan R. Pathan,
  • Sonali P. Mahaparale

摘要

In-situ nasal gel for treating Cerebral Arteriosclerosis (CA) has been developed to deliver tolperisone directly to the brain, bypassing the blood-brain barrier (bbb) and first-pass metabolism, resulting improving CNS bioavailability. A 32 factorial design was employed to optimize the formulation using varying thermosensitive polymer (Poloxamer 407) and mucoadhesive polymer (HPMC/K4M) concentrations to evaluate the gelation temperature and mucoadhession. Nasal thermogelling System exhibit significant results in the range, % drug content 95.14 ± 0.29–98.70 ± 0.5, gelation time <1 min, gelation temperature 32 ± 0.32–36.2 ± 0.29, gel strength < 36 ± 0.22 seconds, and mucoadhesive strength <3621 ± 30 dyn/cm2. The cumulative % tolperisone release for formulations F3, F6, and F9, each with different HPMC:K4M concentrations (0.2%, 0.4%, 0.6% w/v) but a constant 20% w/v of Poloxamer 407, was 87.8%, 82.65%, and 74.65%, respectively, after 8 h. This indicates that higher HPMC K4M concentrations resulted in reduced drug release. At lower HPMC K4M concentrations, higher flux values were observed, and at higher concentrations, flux increased due to polymer cross-linking. Optimized batches F3, F6, and F9 initially showed higher flux of 0.481 ± 0.023, 0.441 ± 0.019, and 0.316 ± 0.015, respectively. The histopathological analysis confirmed the formulation’s safety, demonstrating its potential for targeted and effective CA treatment with lower systemic toxicity than oral administration.

Graphical Abstract