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Purpose <p>Cigarette smoking leads to the cause of mortality. Current smoking cessation often fails to prevent cravings. Intranasal drugs offer a rapid alternative, but existing nasal sprays require frequent dosing, affecting patient adherence. We developed sustained-release nicotine-encapsulated chitosan nanoparticles (NHT-loaded CSNPs) to prolong nicotine effects.</p> Methods <p>NHT CSNPs were synthesized using ionic gelation. Their size and zeta potential were determined. Stability studies were conducted for 90 days. In <i>vitro</i> release kinetics and cytotoxicity were assessed. Pharmacokinetic properties of the NHT-loaded CSNPs were performed in male Sprague Dawley rats.</p> Results <p>The NHT: CS: Sodium Tripolyphosphate (NHT: CS: TPP) ratio of 1:4:4 resulted in the lowest particle size of 120.36 ± 3.23&#xa0;nm, the zeta potential of 36.06 ± 1.70 mV, the encapsulation efficiency of 96.16 ± 0.76%, and the loading capacity of 29.26 ± 1.09%. The NPs showed sustained release activity. The NHT-loaded CSNPs were stable for 90 days, with fibroblast and Calu-3 cell viability &gt; 50%. In vivo studies revealed a lower area under the curve (AUC) and longer half-life (T½) compared to NHT, indicating safety and sustained release.</p> Conclusion <p>In conclusion, the optimized formulation exhibited sustained-release properties with potential use in future smoking cessation research.</p>

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Nicotine Chitosan Nanoparticles for Sustained Release Intranasal Delivery: Development, Evaluation and Pharmacokinetics Studies

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年1月12日

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  • Wasan Alwahsh,
  • Shariza Sahudin,
  • Hatim Alkhatib,
  • Mohammad Bostanudin,
  • Hanish singh Jayasingh Chellammal,
  • Mohammad Alwahsh

摘要

Purpose

Cigarette smoking leads to the cause of mortality. Current smoking cessation often fails to prevent cravings. Intranasal drugs offer a rapid alternative, but existing nasal sprays require frequent dosing, affecting patient adherence. We developed sustained-release nicotine-encapsulated chitosan nanoparticles (NHT-loaded CSNPs) to prolong nicotine effects.

Methods

NHT CSNPs were synthesized using ionic gelation. Their size and zeta potential were determined. Stability studies were conducted for 90 days. In vitro release kinetics and cytotoxicity were assessed. Pharmacokinetic properties of the NHT-loaded CSNPs were performed in male Sprague Dawley rats.

Results

The NHT: CS: Sodium Tripolyphosphate (NHT: CS: TPP) ratio of 1:4:4 resulted in the lowest particle size of 120.36 ± 3.23 nm, the zeta potential of 36.06 ± 1.70 mV, the encapsulation efficiency of 96.16 ± 0.76%, and the loading capacity of 29.26 ± 1.09%. The NPs showed sustained release activity. The NHT-loaded CSNPs were stable for 90 days, with fibroblast and Calu-3 cell viability > 50%. In vivo studies revealed a lower area under the curve (AUC) and longer half-life (T½) compared to NHT, indicating safety and sustained release.

Conclusion

In conclusion, the optimized formulation exhibited sustained-release properties with potential use in future smoking cessation research.