Polymeric nanocapsular baicalin: Chemometric optimization, physicochemical characterization and mechanistic anticancer approaches on breast cancer cell lines

Abstract

Baicalin is a multi-purpose flavonoid known for its anticancer properties, but its application is hindered by its low water solubility and bioavailability. Polymeric nanocapsules were proposed in this work as a promising system for enhancing baicalin delivery, and potentiating its anticancer properties. The characterization of nanocapsules was augmented with chemometric analysis, and the selected formulations were tested on two breast cancer cell lines (MCF-7 and MDA-MB-231), with mechanistic anticancer elucidation using MTT assay, confocal microscopy uptake, flow cytometry, mechanism of cell death, reactive oxygen species production, caspase 3/7 activity and death biomarker expression using quantitative real time PCR. Results showed that baicalin nanocapsules displayed favorable pharmaceutical properties; with the formulation variables affecting their properties elucidated using chemometric factorial analysis. Nanocapsules enhanced the anticancer activity of baicalin up to 216 times for MCF-7 cells and 31 times for MDA-MB-231 after 24 hr incubation. Cellular internalization of the fluorescently labeled nanocapsules was confirmed after 4 hr incubation for both cell lines. Apoptosis was the dominant cell death mechanism, with significant up-regulation of P53 in baicalin nanocapsules treated cells. Data here presented drive to further preclinical studies to investigate the delivery of baicalin polymeric nanocapsules and their anti-cancer activity.

The Promotional Effect of Hollow MnO2 with Brucea Javanica Oil Emulsion (BJOE) on Endometrial Cancer Apoptosis

“…The utilization of nanoparticle-based drug delivery approaches to treat cancer cells has played a vital role in overcoming the limitations of traditional therapeutic approaches [27]. For instance, it was illustrated that the application of a carbohydrate coated iron oxide nanoparticle-ferumoxytol (FDA approved) as an iron supplement has been widespread for curing several diseases like chronic kidney disease, IDA, and cancer [28][29][30]. As depicted in the results, our developed H-MnO 2 -PEG nanoplatform with efficient tumor-homing capacity could effectively release the chemotherapeutic drug upon responsive to tumor acidic microenvironment with respect to endometrial cancer.…”

Baicalin regulates macrophages polarization and alleviates myocardial ischaemia/reperfusion injury via inhibiting JAK/STAT pathway

“…Baicalin, a flavonoid active substance derived from the roots of Scutellaria baicalensis Georgi (Lamiaceae), has been used to treat various of diseases such as cancer (I El-Gogary et al. 2019 ), osteoarthritis (Wang et al. 2018 ), nephritis and hepatitis (Cai et al.…”

Nobiletin-loaded composite penetration enhancer vesicles restore the normal miRNA expression and the chief defence antioxidant levels in skin cancer

“…Nobiletin formulations were stored in sealed vials at 4 ± 1 °C for 3 months 9 , 48 , 49 . After this period, samples were re-assessed for their particle size, polydispersity indices, zeta potential and entrapment efficiency percentages to assess their stability.…”