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Abstract

Lipid-based nanocarriers have emerged as advanced systems for the delivery of natural compounds with limited aqueous solubility and restricted biomedical applicability. Brazilian green propolis extract (PROP) is a complex mixture rich in bioactive molecules with recognized antioxidant, antimicrobial, and antitumor properties. However, its therapeutic use remains limited by poor solubility and instability under physiological conditions.

In this study, nanostructured lipid carriers (NLCs) were designed to encapsulate PROP in order to improve its physicochemical stability, provide controlled release, and enhance biological activity. The formulations were produced by emulsification-ultrasonication using solid and liquid lipids combined with surfactants. The nanoparticles exhibited mean sizes between 110 and 130 nm, polydispersity index (PDI < 0.200), and negative zeta potential (-12 mV). Encapsulation efficiency was close to 100%, and the systems remained stable for up to six months under storage.

In vitro release studies using a dialysis model demonstrated a sustained release profile for the encapsulated extract, in contrast to the rapid diffusion observed for free propolis. Cytotoxicity assays (MTT) against human melanoma A375 cells revealed that nanoencapsulation potentiated the antitumor activity of PROP, allowing significant effects at lower concentrations compared with the non-encapsulated extract.

Overall, the findings indicate that lipid-based nanocarriers are effective platforms for encapsulating green propolis, enabling improved stability, controlled release, and enhanced therapeutic efficacy. These results reinforce the potential of NLCs as innovative nanomaterials for biomedical and pharmaceutical applications of natural products.

This work was supported by CAPES, FAPESP, and CNPq (311368/2022-0).

 

References:

1. L.D. de Moura, L.N.M. Ribeiro, F. V. de Carvalho, G.H. Rodrigues da Silva, P.C. Lima Fernandes, S.Q. Brunetto, C.D. Ramos, L.A. Velloso, D.R. de Araújo, E. de Paula, Docetaxel and lidocaine co-loaded (Nlc-in-hydrogel) hybrid system designed for the treatment of melanoma, Pharmaceutics 13 (2021). https://doi.org/10.3390/pharmaceutics13101552.

2. R.H. Müller, M. Radtke, S.A. Wissing, Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and dermatological preparations, in: Adv. Drug Deliv. Rev., 2002. https://doi.org/10.1016/S0169-409X(02)00118-7.

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Institutions
  • 1 Universidade Estadual Paulista (Unesp)
Track
  • 3. Drug design and delivery
Keywords
NANOCARRIERS
DRUG DELIVERY
GREEN PROPOLIS
MELANOMA CELLS
NANOPARTICLES