Nanocrystal technologies in biomedical science: From the bench to the clinic

Pardhi, Ekta; Vasave, Ravindra; Srivastava, Vaibhavi; Yadav, Rati; Mehra, Neelesh Kumar

doi:10.1016/j.drudis.2024.103913

Cited by 1 publication

(1 citation statement)

References 96 publications

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“…[14][15][16] Stabilizer is generally required to prevent aggregation between high-energy crystal surfaces during size reduction during nanocrystals preparation. 17,18 However, there is no systematic screening rule for the types, dosage and prescription of stabilizers for flavonoid NCs, so the screening of stabilizers is mainly based on the exclusion method at present. 12,19 On the other hand, the commonly used stabilizers for nanosuspensions including sodium dodecyl sulfate and Tween 80 have the drawbacks of poor biocompatibility and chronic toxicity.…”

Section: Introductionmentioning

confidence: 99%

Combined Hydroxyethyl Starch Luteolin Nanocrystals for Effective Anti-Hyperuricemia Effect in Mice Model

Luo,

Wang,

Fang

et al. 2024

IJN

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Introduction Although flavonoid compounds exhibit various pharmacological activities, their clinical applications are restricted by low oral bioavailability owing to their poor solubility. Nanocrystals (NCs) represent an excellent strategy for enhancing the oral bioavailability of flavonoids. Hydroxyethyl starch (HES), a biomaterial compound used as a plasma expander, could be an ideal stabilizer material for preparing flavonoid NCs. Methods HES was used to stabilize flavonoid nanocrystals (NCs), using luteolin (LUT) as a model drug. After full characterization, the freeze-drying and storage stability, solubility, intestinal absorption, pharmacokinetics, and in vivo anti-hyperuricemic effect of the optimized HES-stabilized LUT NCs (LUT-HES NCs) were investigated. Results Uniformed LUT-HES NCs were prepared with mean particle size of 191.1±16.8 nm, zeta potential of about −23 mV, drug encapsulation efficiency of 98.52 ± 1.01%, and drug loading of 49.26 ± 0.50%. The freeze-dried LUT-HES NCs powder showed good re-dispersibility and storage stability for 9 months. Notably, compared with the coarse drug, LUT-HES NCs exhibited improved saturation solubility (7.49 times), increased drug dissolution rate, enhanced Caco-2 cellular uptake (2.78 times) and oral bioavailability (Fr=355.7%). Pharmacodynamic studies showed that LUT-HES NCs remarkably lowered serum uric acid levels by 69.93% and ameliorated renal damage in hyperuricemic mice. Conclusion HES is a potential stabilizer for poorly soluble flavonoid NCs and provides a promising strategy for the clinical application of these compounds. LUT-HES NCs may be an alternative or complementary strategy for hyperuricemia treatment.

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