Fabrication of rosuvastatin-loaded polymeric nanocapsules: a promising modality for treating hepatic cancer delineated by apoptotic and cell cycle arrest assessment

Abstract

Nanotechnology has provided several advantages for the treatment of cancer. Polymeric nanocapsules (PNCs) were proven promising in the treatment of different cancer types, such as hepatic cancer. Meanwhile, the exploration of novel indications of old molecules with the purpose of cancer treatment has been widely reported. Among the promising therapeutic moieties, rosuvastatin (RV) was delineated as a potential anticancer drug. Hence, the target of the presented manuscript was to develop PNCs loaded with RV to overcome its delivery challenges and augment its anticancer activity. RV PNCs were fabricated by the nanoprecipitation method using poly-lactide-co-glycolide (PLGA) polymer, and were characterized for the size, polydispersity index (PDI), charge, entrapment efficiency EE%, in vitro release, stability, and morphology. Furthermore, their anticancer activity was tested on HepG2 cells using MTT assay, followed by elucidating the cytotoxic activity using flow cytometry. Results showed that RV PNCs displayed particle size ranging from 186 to 239 nm, average PDI, and negative zeta potential with sufficient stability for 3 months. PNCs were able to load RV at high EE% reaching 82.6% and sustain its release for eight hours. RV PNCs were superior in their anticancer activity on HepG2 cells, as delineated from the viability study and further elucidated by enhanced apoptosis in addition to cell cycle arrest at G2/M phase, suggesting their promise in treatment of hepatic cancer.

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

“…Baicalin nanocapsules were successfully prepared as a novel delivery system for the anticancer baicalin. The utilized polymer (PLGA) was commonly used in the preparation of nanocapsules delivering anticancer molecules 18–20 , owing to its biodegradable properties 38,39 . The oily core of the nanocapsules was constituted by a corn oil pegylated ester (Labrafil M2125 CS), providing the highest solubility for baicalin, based on a preliminary conducted solubility study (data not shown).…”

“…The free drug was separated from the encapsulated drug using centrifugal concentration 20 at 6000 rpm for 30 minutes (Hermle cooling centrifuge, Germany) using Nanosep tubes. The amount of baicalin in the filtrate was calculated using HPLC (Agilent, USA), following a previously validated reverse phase method 28,29 .…”

“…A promising biodegradable nanoparticulate system which was proven effective in cancer treatment is polymeric nanocapsules 18–20 . Polymeric nanocapsules are composed of a polymeric coat and a lipophilic oily core, stabilized with hydrophilic and lipophilic surfactants 21 .…”

Exploring the unique anticancer properties of curcumin nanoparticles

“…The properties of the Nano emulsion (particle size and charge) were remeasured after 3 months storage at room temperature, to assess the stability of the prepared formulation [5].…”

“…Its efficacy was demonstrated in several cancer types, such as lung cancer, breast cancer, prostate cancer, colon cancer, in addition to others [3,4]. Several nanoparticle types were reported to enhance or preserve the anticancer activity of drugs, owing to their ability to enhance cancer cell uptake by their nanometer size [5][6][7][8]. From the promising nanoparticle types are microemulsions, which are composed of oil, water and surfactant/cosurfactant mixture [9][10][11].…”