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<p>Migraines inflict the third most brain damage, per the Global Burden of Disease Study. Migraines generate massive unilateral headaches, light and sound sensitivity, and discomfort. Many migraine treatments are triptans, 5HT1B/1D receptor agonists. Popular tryptamine derivative Zolmitriptan (ZTN) is synthetic. Oral ZTN’s low permeability causes delayed onset, 40% absorption, nausea, and limited headache pain alleviation with headache recurrence. The most promising migraine therapy experiment uses QbD nasal-to-brain ZTN via nanostructured lipid carriers (NLCs). Current study aimed to create ZTN NLCs for nose-to-brain QbD drug delivery. ZTN-NLCs were made from compritol HD5 ATO and castor oil as solid and liquid lipids using hot microemulsification and probe sonication. Box Behken design were used to quantify particle size, %EE, and PDI using independent variables lipids, surfactant, and sonication duration. DSC measured ZTN entrapment in NLCs, whereas XRD indicated reduced crystallinity. ANOVA F-tests with P-values &lt; 0.0500 fit all three CQA response variables. Multi-parametric desirability optimization allows nanoformulation design. The yellow center of the overlay figure indicated nanoparticles (~ 160&#xa0;nm), strong entrapment (&gt; 90%), and low PDI (~ 0.3). All variables were adjusted to 1600&#xa0;mg total lipid (A), ~ 1.49% surfactant (B), and 5.72&#xa0;min sonication (C). The overlay plot indicates all three key reactions work well in strong formulations. ZTN-NLCs showed substantial tail flick and hot plate antimigraine response compared to pure ZTN. ZTN NLC preparation may improve drug permeability, bioavailability, and antimigraine effect, making it a targeted technique.</p> Graphical Abstract <p></p>

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Quality by Design Optimization of Zolmitriptan Nanostructured Lipid Carriers for Nose-to-brain Delivery in Migraine

  • 期刊论文

  • 发表日期：

    2025年12月17日

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  • Subhash Deshmane,
  • Vaishnavi Chavan,
  • Snehal Nagpure,
  • Shirish Jain,
  • Himanshu Solanki,
  • Rahul Sarode,
  • Shashikant Bagade,
  • Purushottam Gangane

摘要

Migraines inflict the third most brain damage, per the Global Burden of Disease Study. Migraines generate massive unilateral headaches, light and sound sensitivity, and discomfort. Many migraine treatments are triptans, 5HT1B/1D receptor agonists. Popular tryptamine derivative Zolmitriptan (ZTN) is synthetic. Oral ZTN’s low permeability causes delayed onset, 40% absorption, nausea, and limited headache pain alleviation with headache recurrence. The most promising migraine therapy experiment uses QbD nasal-to-brain ZTN via nanostructured lipid carriers (NLCs). Current study aimed to create ZTN NLCs for nose-to-brain QbD drug delivery. ZTN-NLCs were made from compritol HD5 ATO and castor oil as solid and liquid lipids using hot microemulsification and probe sonication. Box Behken design were used to quantify particle size, %EE, and PDI using independent variables lipids, surfactant, and sonication duration. DSC measured ZTN entrapment in NLCs, whereas XRD indicated reduced crystallinity. ANOVA F-tests with P-values < 0.0500 fit all three CQA response variables. Multi-parametric desirability optimization allows nanoformulation design. The yellow center of the overlay figure indicated nanoparticles (~ 160 nm), strong entrapment (> 90%), and low PDI (~ 0.3). All variables were adjusted to 1600 mg total lipid (A), ~ 1.49% surfactant (B), and 5.72 min sonication (C). The overlay plot indicates all three key reactions work well in strong formulations. ZTN-NLCs showed substantial tail flick and hot plate antimigraine response compared to pure ZTN. ZTN NLC preparation may improve drug permeability, bioavailability, and antimigraine effect, making it a targeted technique.

Graphical Abstract