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Abstract

Artepillin C (ARTC), the main phenolic constituent of Brazilian green propolis, has been widely reported for its antioxidant, anti-inflammatory, and anticancer properties [1]. However, its therapeutic application remains limited due to poor aqueous solubility and consequently low bioavailability [2]. In this study, nanostructured lipid carriers (NLCs) were developed as delivery systems for ARTC and green propolis extract. Different lipid matrices and preparation strategies were evaluated through miscibility screening, dynamic light scattering (DLS), and determination of encapsulation efficiency (EE). Among the tested conditions, formulations composed of myristyl myristate, capric/caprylic triglycerides, and Poloxamer 188 exhibited the most favorable physicochemical characteristics, particularly when produced by the emulsification–ultrasonication method, which showed superior performance compared with the solvent injection approach. The optimized formulations displayed mean particle diameters below 120 nm, narrow size distributions (PDI < 0.2), and negative zeta potentials ranging from –12 to –21 mV, maintaining colloidal stability for up to 190 days. Encapsulation efficiencies reached 100% for both ARTC and the propolis extract, as quantified by HPLC. Raman spectroscopy indicated molecular interactions between the incorporated bioactive compounds and the lipid matrix, while X-ray diffraction confirmed the preservation of the crystalline organization of the lipid core after encapsulation. Cryo-TEM imaging revealed spherical nanoparticles with well defined morphology. Overall, these results demonstrate that the developed NLCs constitute a stable and efficient nanocarrier platform for the delivery of ARTC and green propolis, supporting their potential use in therapeutic applications. This work was supported by FAPESP (2018/22214-6 and 2023/01305-1) and CNPq (311368/2022-0). References [1] Zhang, C. ping et al. Natural Product Research 2017, v. 31, 2441–2444. (2017) Authors (M. T. Nguyen-Kim, T. A. Smith), Journal title Year, Volume, Pages. [2] Wu, F., Song, XM., Qiu, YL. et al. Scientific Reports 2020, v. 10, 17277.

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Institutions
  • 1 Universidade Estadual Paulista (Unesp)
  • 2 UNICAMP - Universidade Estadual de Campinas
  • 3 Universidade Estadual de Campinas (UNICAMP) | (State University of Campinas (UNICAMP))
Track
  • 3. Drug design and delivery
Keywords
Artepillin C
Brazilian green propolis
Nanostructured lipid carriers
Encapsulation efficiency
Therapeutic applications