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Purpose <p>Cutaneous leishmaniasis (CL) is a group of parasitic diseases caused by flagellated protozoa. Artemisinin (ART) has been widely investigated as an anti-promastigote in <i>Leishmania</i> species. The anti-promastigote activity of ART is limited due to low aqueous solubility (61.83 ± 4.33&#xa0;µg/mL) and hindered permeation.</p> Methods and Results <p>Henceforth, in the current study, a Quality-by-Design (QbD)-based approach was employed to engineer artemisinin nanoemulsion (ART-NE) with improved physicochemical characteristics. The ART-NE yielded a droplet diameter of 131.3 ± 0.73&#xa0;nm with a PDI of 0.155 ± 0.01. The transmission electron microscopy (TEM) photomicrograph displayed spherical droplets of uniform size of ART-NE. The ex vivo percutaneous permeation parameters, such as steady state flux and permeability coefficient of ART-NE, were calculated to be 101.48 ± 0.30&#xa0;µg/cm<sup>2</sup>/h and 62.33 ± 0.18 (x10<sup>− 3</sup> cm/h), respectively. Next, ART-NE depicted a relatively low IC<sub>50</sub> of 11.87 ± 4.22-µM as compared to ART solution (40.25 ± 9.76 µM) and ART suspension (151.4 ± 57.6 µM) with 3.39-fold and 12.75-fold reductions, respectively, against <i>L. donovani.</i> Furthermore, the selectivity index (SI) was calculated to determine their relative toxicity. The higher SI indicates higher efficacy of the treatment modality as compared to host cells. ART displayed a higher IC<sub>50</sub> than CC<sub>50</sub>, resulting in an SI &lt; 1 (0.35). In contrast, ART-NE and blank nanoemulsion (blank NE) exhibited SI of 3.13 and 2.97, respectively. The high SI of ART-NE may be attributed to higher permeation, augmented solubility, and endocytic uptake by the <i>L. donovani</i> strain.</p> Conclusion <p>In conclusion, ART-NE is an innovative drug delivery cargo that must be further established in an authenticated preclinical model of CL under rigorous in vivo parameters for translational research.</p>

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Quality-by-design Assisted Laboratory Scale Up of Artemisinin Nanoemulsion Augmented Drug Delivery, Cytotoxicity and Cellular Uptake in Leishmania donovani Parasite, a Causative Agent for Cutaneous Leishmaniasis

  • 期刊论文

  • 发表日期：

    2026年6月22日

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  • Atul Mourya,
  • Madhulika Namdeo,
  • Shristi Arya,
  • Samiksha Thote,
  • Soham Loharkar,
  • Gopal Bajad,
  • Soyal Sayyed,
  • Radheyshyam Maurya,
  • Jitender Madan

摘要

Purpose

Cutaneous leishmaniasis (CL) is a group of parasitic diseases caused by flagellated protozoa. Artemisinin (ART) has been widely investigated as an anti-promastigote in Leishmania species. The anti-promastigote activity of ART is limited due to low aqueous solubility (61.83 ± 4.33 µg/mL) and hindered permeation.

Methods and Results

Henceforth, in the current study, a Quality-by-Design (QbD)-based approach was employed to engineer artemisinin nanoemulsion (ART-NE) with improved physicochemical characteristics. The ART-NE yielded a droplet diameter of 131.3 ± 0.73 nm with a PDI of 0.155 ± 0.01. The transmission electron microscopy (TEM) photomicrograph displayed spherical droplets of uniform size of ART-NE. The ex vivo percutaneous permeation parameters, such as steady state flux and permeability coefficient of ART-NE, were calculated to be 101.48 ± 0.30 µg/cm2/h and 62.33 ± 0.18 (x10− 3 cm/h), respectively. Next, ART-NE depicted a relatively low IC50 of 11.87 ± 4.22-µM as compared to ART solution (40.25 ± 9.76 µM) and ART suspension (151.4 ± 57.6 µM) with 3.39-fold and 12.75-fold reductions, respectively, against L. donovani. Furthermore, the selectivity index (SI) was calculated to determine their relative toxicity. The higher SI indicates higher efficacy of the treatment modality as compared to host cells. ART displayed a higher IC50 than CC50, resulting in an SI < 1 (0.35). In contrast, ART-NE and blank nanoemulsion (blank NE) exhibited SI of 3.13 and 2.97, respectively. The high SI of ART-NE may be attributed to higher permeation, augmented solubility, and endocytic uptake by the L. donovani strain.

Conclusion

In conclusion, ART-NE is an innovative drug delivery cargo that must be further established in an authenticated preclinical model of CL under rigorous in vivo parameters for translational research.