Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Bee Venom-Loaded Niosomes as Innovative Platforms for Cancer Therapy: Formulation Development and In Vitro and Ex Vivo Therapeutical Efficacy and Safety Assessment

Version 1 : Received: 26 February 2024 / Approved: 26 February 2024 / Online: 27 February 2024 (13:33:12 CET)

How to cite: Pinto, M.B.; Pires, P.C.; Calhelha, R.C.; Silva, A.R.; Sousa, M.J.; Vilas-Boas, M.; Falcão, S.I.; Veiga, F.; Makvandi, P.; Paiva-Santos, A.C. Bee Venom-Loaded Niosomes as Innovative Platforms for Cancer Therapy: Formulation Development and In Vitro and Ex Vivo Therapeutical Efficacy and Safety Assessment. Preprints 2024, 2024021508. https://doi.org/10.20944/preprints202402.1508.v1 Pinto, M.B.; Pires, P.C.; Calhelha, R.C.; Silva, A.R.; Sousa, M.J.; Vilas-Boas, M.; Falcão, S.I.; Veiga, F.; Makvandi, P.; Paiva-Santos, A.C. Bee Venom-Loaded Niosomes as Innovative Platforms for Cancer Therapy: Formulation Development and In Vitro and Ex Vivo Therapeutical Efficacy and Safety Assessment. Preprints 2024, 2024021508. https://doi.org/10.20944/preprints202402.1508.v1

Abstract

Despite past efforts towards therapeutical innovation, cancer remains a highly incident and lethal disease, with current treatments many times lacking efficiency and leading to severe side-effects. Hence, it is imperative to develop new, more efficient, and safer therapies. Bee venom has proven to have multiple and synergistic bioactivities, including antitumor effects. Nevertheless, some toxic effects have been associated with its administration. To tackle these issues, in this work, bee venom-loaded niosomes were developed, for cancer treatment. The vesicles had a small (150.4 ± 3.7 nm) and homogeneous (PDI of 0.162 ± 0.008) particle size, and revealed good therapeutic efficacy in in vitro gastric, colorectal, breast, lung, and cervical cancer models, with GI50 values between 12.37 ng/mL and 14.72 ng/mL. Additionally, they also revealed substantial anti-inflammatory activity, with an IC50 of 28.98 ng/mL, effects that have been reported to be complementary to direct antitumor activity. Finally, the niosomes' safety was assessed, both in vitro, on skin, liver and kidney cells, and ex vivo, in a HET-CAM assay, and results showed that compound encapsulation increased its safety. Hence, small and homogeneous bee venom-loaded niosomes were successfully developed, with substantial anticancer and anti-inflammatory effects, making them potentially promising primary or adjuvant cancer therapies.

Keywords

anti-inflammatory; anticancer; antitumor; bee venom; HET-CAM; in vitro; nanosystems; nanotechnology; natural compounds; niosomes

Subject

Chemistry and Materials Science, Nanotechnology

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