Mangiferin loaded magnetic PCEC microspheres: preparation, characterization and antitumor activity studies in vitro

Abstract

Mangiferin is a promising effective chemopreventive agent against various tumors. However, its clinical use is limited by poor water solubility and low bioavailability. In this article, mangiferin loaded magnetic PCEC microspheres (MG-MS) were designed, characterized and the antitumor activity of MG-MS was evaluated in vitro. The magnetic nanoparticles (MNP) were synthesized via the high-temperature reaction of iron acetylacetonate in phenyl ether in the presence of oleic acid and oleylamine. Poly (ε-caprolactone)-poly (ethyleneglycol)-poly (ε-caprolactone) (PCL-PEG-PCL, PCEC) copolymers were formed by ring-opening copolymerization of ε-CL initiated by PEG-diol using Sn(Oct) as a catalyst and MG-MS were prepared by solvent diffusion method. MNP, PCEC copolymer, and MG-MS were characterized by GPC, TEM, XRD, FT-IR, H-NMP and Malvern Laser Particle Sizer. Meanwhile, the antiproliferative activity in vitro and in vitro release behavior of this microspheres were studied in detail. The results indicate that the obtained magnetic microspheres might have great potential as an effective carrier for mangiferin used in cancer chemotherapy.

Gallic Acid Content and an Antioxidant Mechanism Are Responsible for the Antiproliferative Activity of ‘Ataulfo’ Mango Peel on LS180 Cells

“…Ma, et al [ 26 ] isolated mangiferin from ‘Chaunsa’ mango peel through a solvent partition method using petroleum ether (to remove fatty matter), cold acetone (to separate tannins), and 70% ethanol (to isolate mangiferin), obtaining a higher mangiferin content than has been seen in other mango varieties (“Anwar ratol”, “Langra”, “Dusahri”, and “Desi”). In contrast, Xiao, et al [ 27 ] reported that the highest contents of FP and mangiferin from ‘Chaunsa’ mango peel were obtained using 80% methanol or ethanol (~60 mg GAE; 100–110 µg/g) instead of 80% acetone (~30 mg GAE) or ethyl acetate (~20 mg GAE). However, since mangiferin molecule is insoluble in both hydrophilic and hydrophobic media it should be complexed with other molecules such as phospholipids or polycaprolactone/poly(ethyleneglycol)/polycaprolactone (PCEC) microspheres to enhance its solubility, food release, bioavailability, and other properties [ 11 , 12 ].…”

Mangiferin regulates proliferation and apoptosis in glioma cells by induction of microRNA-15b and inhibition of MMP-9 expression

“…Modern pharmacological and clinical studies have shown that mangiferin has physiological activity and pharmacological effects in many aspects (12). Mangiferin exhibits a significant central nervous system stimulant effect and a glucocorticoid-like anti-inflammatory effect, which can reduce capillary permeability, and its anti-inflammatory response rate is 38% (13). Mangiferin can block the cell cycle of human hepatoma cell line BEL-7404 at the G2/M phase, and we found in our previous study that mangiferin significantly inhibited the proliferation of the K562 chronic myeloid leukemia cell line (14).…”

The potential role of mangiferin in cancer treatment through its immunomodulatory, anti‐angiogenic, apoptopic, and gene regulatory effects

“…More recently, magnetite poly(ε‐caprolactone)‐poly(ethyleneglycol)‐poly(ε‐caprolactone) (PCEC) microspheres were used as a drug delivery system for MF due to their capacity to increase the water solubility . Magnetic polymeric microspheres were found to be an ideal targeted‐drug delivery system and an optimal controlled release system for cancer treatment due to the fact that magnetic polymeric microspheres could increase the drug concentration at target site via magnetic field .…”