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

Abstract

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 (IC50 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.

Liposomal formulation of a new antifungal hybrid compound provides protection against Candida auris in the ex vivo skin colonization model

“…Morphological analysis was performed using a Tecnai G2 20 TWIN transmission electron microscope (FEI, Hillsboro, OR, USA) as described in ( 33 ).…”

The baicalein amorphous solid dispersion to enhance the dissolution and bioavailability and effects on growth performance, meat quality, antioxidant capacity and intestinal flora in Taihang chickens

“…Baicalein ( BAI ),which is a natural flavonoid derived from the traditional Chinese herb, Scutellaria baicalensis (aka Huangqin) ( Markowski et al, 2023 ), has antioxidant ( Bayram et al, 2023 ), anti-inflammatory ( Holanda et al, 2022 ), antibacterial ( Yun et al, 2012 )and other pharmacological effects. The total antioxidant capacity ( T-AOC ) activity, total superoxide dismutase ( T-SOD ) and glutathione peroxidase ( GSH-Px ) level in liver of broilers was significantly increased by inclusion of BAI, suggested that dietary supplementation of BAI can improve the antioxidant ability of broilers ( Zhou et al, 2019 ).…”

Evaluation of the Antitumor Activity of Quaternary Ammonium Surfactants

“…One possibility is the use of soft analogs [15]. Another promising method to reduce toxicity is the use of nanomedicines in the form of liposomes, which provide a platform for encapsulating hydrophobic, hydrophilic, and amphiphilic compounds [16][17][18][19]. Liposomes are carriers for enhanced bioavailability and sustained release.…”