RT Journal Article
T1 Improved antitumor activity through a tyramidyl maslinic acid derivative. Design and validation as drug-loaded electrospun polymeric nanofibers
A1 Luque, Cristina
A1 Fernández, María de la Cabeza
A1 Fuentes-Ríos, David
A1 Cepero, Ana
A1 Contreras-Cáceres, Rafael
A1 Doña, Manuel
A1 Perazzoli, Gloria
A1 Lozano-Chamizo, Laura
A1 Filice, Marco
A1 Marciello, Marzia
A1 González-Rumayor, Victor
A1 López-Romero, Juan Manuel
A1 Cabeza, Laura
A1 Melguizo, Consolación
A1 Prados, José
K1 Quimioterapia
K1 Antineoplásicos
K1 Polímeros
K1 Mamas - Cáncer
K1 Cáncer colorrectal
AB Among the most harmful tumors detected in the human body, such as breast, colon, brain or pancreas, breast (BC) and colorectal cancer (CRC) are the first and third most frequent cancer worldwide, respectively. The current existing chemotherapeutic treatments present serious side effects due to their intravenous administration can induce cytotoxicity in healthy cells. Thus, new treatment methods based on drug-loaded polymeric nanofibers (NFs) have gained significant potential for their use in localized cancer chemotherapy. Here, a deep in vitro comparative analysis between maslinic acid (MA) and a tyramine-maslinic acid (TMA) derivative is initially performed. This analysis includes a proliferation, and a cell cycle assay, and a genotoxicity, antiangiogenic and apoptosis study. Then, the TMA derivative has been incorporated into electrospun polymeric NFs obtaining an implantable dressing material with antitumor activity. Two types of patches containing TMA-loaded polymericNFs of poly(caprolactone) (PCL), and a mixture of polylactic acid/poly(4-vinylpyridine) (PLA/PVP) were fabricated by the electrospinning technique. The characterization of the drug-loaded NFs showed an encapsulation capacity of 0.027 mg TMA/mg PCL and 0.024 mg TMA/mg PLA/PVP. Then, the cytotoxic activity of both polymeric systems was tested in CRC (T84), BC (MCF-7) and a no tumor (L929) cell lines exposed to TMA-loaded NFs and blank NFs for 48 h. Moreover, cell cycle assay, genotoxicity, angiogenesis and apoptosis tests were carried out to study the mechanism of action of TMA. Blank NFs showed no-toxicity in all cell lines tested and both drug-loaded NFs significantly reduced cell proliferation (relative proliferation of ≈44 % and ≈25 % respectively). Therefore, TMA was less genotoxic than MA, and reduced VEGFA expression in MCF-7 cells (1.32 and 2.12-fold for MA and TMA respectively). TMA-loaded NFs constitute a promising biocompatible nanoplatform for treatment of tumors as CRC or BC.
PB Elsevier
YR 2023
FD 2023
LK https://hdl.handle.net/10630/40459
UL https://hdl.handle.net/10630/40459
LA eng
NO Cristina Luque, María de la Cabeza Fernández, David Fuentes-Rios, Ana Cepero, Rafael Contreras-Cáceres, Manuel Doña, Gloria Perazzoli, Laura Lozano-Chamizo, Marco Filice, Marzia Marciello, Victor Gonzalez-Rumayor, Juan Manuel López-Romero, Laura Cabeza, Consolación Melguizo, José Prados, Improved antitumor activity through a tyramidyl maslinic acid derivative. Design and validation as drug-loaded electrospun polymeric nanofibers, European Journal of Pharmaceutics and Biopharmaceutics, Volume 193, 2023, Pages 241-253, ISSN 0939-6411, https://doi.org/10.1016/j.ejpb.2023.11.011
DS RIUMA. Repositorio Institucional de la Universidad de Málaga
RD 25 ene 2026