Motion sickness is a common condition that occurs when the inner ear and brain receive conflicting information about the direction of body motion. This signal transmission discrepancy can cause nausea, vomiting, or dizziness. Cinnarizine is an effective drug for treating motion sickness. However, its poor solubility, poor bioavailability, and short duration of action contribute to low patient compliance. Nano-lipid carriers are a promising technology for improving the solubility and bioavailability of poorly water-soluble drugs by forming prolonged-release lipid carriers. This study aimed to develop cinnarizine-loaded nano-lipid carriers (CN-NLCs) to enhance cinnarizine solubility, thereby enabling effective prevention and treatment of nausea and vomiting. CN-NLCs were prepared through high-speed shear hot homogenization followed by ultrasonication. Two solid lipids (Tefose 1500 and Tefose 63) were employed, while oleic acid served as the liquid lipid due to the high solubilising capacity of cinnarizine. Compatibility studies were evaluated by FTIR spectroscopy. In-vitro drug release studies were performed using dialysis bags. The morphology and particle association of CN-NLCs were examined via scanning electron microscopy (SEM). FTIR studies confirmed that there is no physical interaction between the drug and excipients.CN-NLCs prepared formulas had a high encapsulation efficiency of 92% ± 3.57 and a drug loading efficiency of 8.2% ± 0.32. In addition to studying the drug release from the prepared nanoparticles, the drug release curve showed prolonged release of cinnarizine from the nanoparticles compared to free cinnarizine (85% and 40% after 24 h, respectively).CN-NLCs were characterised morphologically; scanning electron microscopy images showed spherical nanoparticles without aggregation, ranging from 191 ± 64.6 nm to 388 ± 78.1 nm, with a narrow size distribution. The preparation of cinnarizine-loaded lipid nanocarriers has improved solubility and prolonged its duration of action to 24 h, facilitating better patient compliance with a single daily dose and achieving an acceptable nano-sized carrier for cinnarizine.

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Analysis of the Effect of Incorporating Tefose® 1500 and Tefose® 63 in Nanostructured Lipid Carriers for Enhanced Encapsulation and Prolonged Release of Cinnarizine

  • Rania Al-Hamwi,
  • Hind El-Zein

摘要

Motion sickness is a common condition that occurs when the inner ear and brain receive conflicting information about the direction of body motion. This signal transmission discrepancy can cause nausea, vomiting, or dizziness. Cinnarizine is an effective drug for treating motion sickness. However, its poor solubility, poor bioavailability, and short duration of action contribute to low patient compliance. Nano-lipid carriers are a promising technology for improving the solubility and bioavailability of poorly water-soluble drugs by forming prolonged-release lipid carriers. This study aimed to develop cinnarizine-loaded nano-lipid carriers (CN-NLCs) to enhance cinnarizine solubility, thereby enabling effective prevention and treatment of nausea and vomiting. CN-NLCs were prepared through high-speed shear hot homogenization followed by ultrasonication. Two solid lipids (Tefose 1500 and Tefose 63) were employed, while oleic acid served as the liquid lipid due to the high solubilising capacity of cinnarizine. Compatibility studies were evaluated by FTIR spectroscopy. In-vitro drug release studies were performed using dialysis bags. The morphology and particle association of CN-NLCs were examined via scanning electron microscopy (SEM). FTIR studies confirmed that there is no physical interaction between the drug and excipients.CN-NLCs prepared formulas had a high encapsulation efficiency of 92% ± 3.57 and a drug loading efficiency of 8.2% ± 0.32. In addition to studying the drug release from the prepared nanoparticles, the drug release curve showed prolonged release of cinnarizine from the nanoparticles compared to free cinnarizine (85% and 40% after 24 h, respectively).CN-NLCs were characterised morphologically; scanning electron microscopy images showed spherical nanoparticles without aggregation, ranging from 191 ± 64.6 nm to 388 ± 78.1 nm, with a narrow size distribution. The preparation of cinnarizine-loaded lipid nanocarriers has improved solubility and prolonged its duration of action to 24 h, facilitating better patient compliance with a single daily dose and achieving an acceptable nano-sized carrier for cinnarizine.