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<p>The objective of this study was to enhance the transdermal delivery of citalopram HBr (CTP) by incorporating it into novasomes (Citalosomes) prepared via probe sonication. Previous studies have shown limited transdermal absorption and short-term therapeutic effects of conventional citalopram formulations, representing a research gap that this study aims to address. The influence of cholesterol-to-surfactant ratio and oleic acid content on formulation characteristics was investigated. Particle size, zeta potential, and entrapment efficiency (EE%) were assessed using dynamic light scattering (DLS) and UV-spectrophotometry, respectively. Results showed that increasing cholesterol concentration enhanced vesicle rigidity and structural characteristics but reduced EE%. Meanwhile, optimizing the oleic acid to surfactant ratio improved membrane fluidity and significantly increased encapsulation efficiency. The optimized novasomal vesicle formulation (Citalosome 2) exhibited a vesicle size of 282.66 ± 5.85 nm, PDI 0.228 ± 0.028, zeta potential of 9.1 ± 0.26 mV, and EE% of 36.42 ± 2.09. Attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy and differential scanning calorimetry (DSC) analysis confirmed the presence of the drug in an amorphous state without any chemical interaction within the formulation. Transmission electron microscopy (TEM) images demonstrated spherical morphology and suitable dispersion of vesicles. In vitro skin permeation studies using a carbopol-based gel indicated higher transdermal absorption of the drug from Citalosome 2 gel compared to plain CTP gel (<i>p</i> &lt; 0.05). The Citalosome system also showed a sustained release profile over 24 h. Cytotoxicity evaluation on HFF cells confirmed low toxicity (&gt; 88% viability). Furthermore, in vivo analgesic and anti-inflammatory assessments (hot-plate, formalin, and paw edema tests) using the same carbopol-based gel revealed prolonged and improved antinociceptive and anti-inflammatory responses of Citalosome 2 gel compared to control formulations (<i>p</i> &lt; 0.05). Histological analysis demonstrated decrease in inflammation following topical application. These findings suggest that Citalosome 2 may serve as a promising vesicular carrier for transdermal citalopram delivery, with the potential to improve its analgesic efficacy.</p>

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Preparation and evaluation of citalopram novasomal vesicles as a transdermal analgesic drug delivery

  • 期刊论文

  • 发表日期：

    2026年3月24日

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  • Fereshte Haftan,
  • Katayoun Morteza-Semnani,
  • Jafar Akbari,
  • Mohammad Seyedabadi,
  • Maryam Ghasemi,
  • Majid Saeedi

摘要

The objective of this study was to enhance the transdermal delivery of citalopram HBr (CTP) by incorporating it into novasomes (Citalosomes) prepared via probe sonication. Previous studies have shown limited transdermal absorption and short-term therapeutic effects of conventional citalopram formulations, representing a research gap that this study aims to address. The influence of cholesterol-to-surfactant ratio and oleic acid content on formulation characteristics was investigated. Particle size, zeta potential, and entrapment efficiency (EE%) were assessed using dynamic light scattering (DLS) and UV-spectrophotometry, respectively. Results showed that increasing cholesterol concentration enhanced vesicle rigidity and structural characteristics but reduced EE%. Meanwhile, optimizing the oleic acid to surfactant ratio improved membrane fluidity and significantly increased encapsulation efficiency. The optimized novasomal vesicle formulation (Citalosome 2) exhibited a vesicle size of 282.66 ± 5.85 nm, PDI 0.228 ± 0.028, zeta potential of 9.1 ± 0.26 mV, and EE% of 36.42 ± 2.09. Attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy and differential scanning calorimetry (DSC) analysis confirmed the presence of the drug in an amorphous state without any chemical interaction within the formulation. Transmission electron microscopy (TEM) images demonstrated spherical morphology and suitable dispersion of vesicles. In vitro skin permeation studies using a carbopol-based gel indicated higher transdermal absorption of the drug from Citalosome 2 gel compared to plain CTP gel (p < 0.05). The Citalosome system also showed a sustained release profile over 24 h. Cytotoxicity evaluation on HFF cells confirmed low toxicity (> 88% viability). Furthermore, in vivo analgesic and anti-inflammatory assessments (hot-plate, formalin, and paw edema tests) using the same carbopol-based gel revealed prolonged and improved antinociceptive and anti-inflammatory responses of Citalosome 2 gel compared to control formulations (p < 0.05). Histological analysis demonstrated decrease in inflammation following topical application. These findings suggest that Citalosome 2 may serve as a promising vesicular carrier for transdermal citalopram delivery, with the potential to improve its analgesic efficacy.