ORIGINAL RESEARCH article
Front. Bioeng. Biotechnol.
Sec. Nanobiotechnology
Volume 13 - 2025 | doi: 10.3389/fbioe.2025.1617022
This article is part of the Research TopicThe Role of Nano-Therapeutics in Precision Cancer MedicineView all articles
PLGA NANOPARTICLES FOR CAPSAICIN DELIVERY: ENHANCED ENCAPSULATION EFFICIENCY AND PRO-APOPTOTIC ACTIVITY IN HEPG2 CELLS
Provisionally accepted
Chiara Mulè1,2
Tania Mariastella Caputo1,2
Antonio Montefusco3,4
Antonio Massimiliano Romanelli1,2
Ivana Caputo3,4
Gaetana Paolella3,4*
Anna Aliberti1,2Andrea Cusano1,2*- 1University of Sannio, Benevento, Italy
- 2Dipartimento di Ingegneria, Università del Sannio, Benevento, Campania, Italy
- 3University of Salerno, Fisciano, Campania, Italy
- 4Department of Chemistry and Biology, fisciano, Italy
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Capsaicin (trans-8-methyl-N-vanillyl-6-nonenamide) (Cap) is a lipophilic alkaloid derived from Capsicum annuum. It was observed that Cap has an antitumoral activity in several cancer types, in particular in liver, colon and breast cancer. Actually, the use of Cap in the cancer therapy is limited by its very low bioavailability, a short half-life and side effects as mouth and stomach irritations and burning sensation. To overcome these limitations, the Cap has been encapsulated in carriers in order to reduce the adverse effect and to help the delivery in the cancer cells. In this study, we synthesized Poly(lactic co-glycolic acid) (PLGA) nanoparticles (NPs) to encapsulate Cap (PLGA-Cap) optimizing the synthetic strategy and improving its efficiency and safety. This is the first time that PLGA-Cap NPs was tested on HepG2 cells line for Hepatocellular carcinoma (HCC) therapy. Several NPs characterizations were conducted to study their physicochemical properties and the best condition in terms of size, PDI and encapsulation efficiency was reached. Our preparation showed the highest Encapsulation Efficiency (96%) reported by the literature, showing an improvement of 21% compared to what is actually reported. In vitro experiments revealed that PLGA-Cap formulation induced similar biological effects in terms of cell viability compared to free Cap, moreover, HepG2 cancer cells treated with PLGA-Cap exhibited increased caspase 3 activity and reactive oxigen species (ROS) generation respect to those treated with free Cap. In conclusion we demonstrated that our preparation showed an improvement in encapsulation parameters and in pro-apoptotic and anticancer activity in HepG2 cells.
Keywords: Capsaicin, PLGA nanoparticles, HepG2, Apoptosis, Cap encapsulation efficiency, Drug delivery
Received: 23 Apr 2025; Accepted: 04 Jul 2025.
Copyright: © 2025 Mulè, Caputo, Montefusco, Romanelli, Caputo, Paolella, Aliberti and Cusano. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
* Correspondence:
Gaetana Paolella, University of Salerno, Fisciano, 84084, Campania, Italy
Andrea Cusano, University of Sannio, Benevento, Italy
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