Novel Liposomal Formulation of Baicalein for the Treatment of Pancreatic Ductal Adenocarcinoma: Design, Characterization, and Evaluation

Pancreatic cancer (PC) is one of the deadliest cancers so there is an urgent need to develop new drugs and therapies to treat it. Liposome-based formulations of naturally-derived bioactive compounds are promising anticancer candidates due to their potential for passive accumulation in tumor tissues,...

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Bibliographic Details
Published in:Pharmaceutics 2023-01, Vol.15 (1), p.179
Main Authors: Markowski, Adam, Zaremba-Czogalla, Magdalena, Jaromin, Anna, Olczak, Ewa, Zygmunt, Adrianna, Etezadi, Haniyeh, Boyd, Ben J, Gubernator, Jerzy
Format: Article
Language:English
Subjects:
Apoptosis
Ascites
baicalein
Cell cycle
Cyclin-dependent kinases
Disease
Extracellular matrix
Fibroblasts
Flavonoids
hemolysis
Immune system
Kinases
liposomes
Metabolism
Metabolites
Metastasis
Mutation
nanotechnology
Pancreatic cancer
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Summary:Pancreatic cancer (PC) is one of the deadliest cancers so there is an urgent need to develop new drugs and therapies to treat it. Liposome-based formulations of naturally-derived bioactive compounds are promising anticancer candidates due to their potential for passive accumulation in tumor tissues, protection against payload degradation, and prevention of non-specific toxicity. We chose the naturally-derived flavonoid baicalein (BAI) due to its promising effect against pancreatic ductal adenocarcinoma (PDAC) and encapsulated it into a liposomal bilayer using the passive loading method, with an almost 90% efficiency. We performed a morphological and stability analysis of the obtained BAI liposomal formulation and evaluated its activity on two-dimensional and three-dimensional pancreatic cell models. As the result, we obtained a stable BAI-encapsulated liposomal suspension with a size of 100.9 nm ± 2.7 and homogeneity PDI = 0.124 ± 0.02, suitable for intravenous administration. Furthermore, this formulation showed high cytotoxic activity towards AsPC-1 and BxPC-3 PDAC cell lines (IC values ranging from 21 ± 3.6 µM to 27.6 ± 4.1 µM), with limited toxicity towards normal NHDF cells and a lack of hemolytic activity. Based on these results, this new BAI liposomal formulation is an excellent candidate for potential anti-PDAC therapy.
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics15010179