Characterization and anticancer potential of ferulic acid-loaded chitosan nanoparticles against ME-180 human cervical cancer cell lines

Abstract

Ferulic acid (FA) is a widely distributed hydroxycinnamic acid found in various cereals and fruits exhibiting potent antioxidant and anticancer activities. However, due to low solubility and permeability, its availability to biological systems is limited. Non-toxic chitosan-tripolyphosphate pentasodium (CS-TPP) nanoparticles (NPs) are used to load sparingly soluble molecules and drugs, increasing their bioavailability. In the present work, we have encapsulated FA into the CS-TPP NPs to increase its potential as a therapeutic agent. Different concentrations of FA were tested to obtain optimum sized FA-loaded CS-TPP nanoparticles (FA/CS-TPP NPs) by ionic gelation method. Nanoparticles were characterized by scanning electron microscopy, Fourier transformation infrared spectroscopy (FTIR), thermogravimetric analyses and evaluated for their anticancer activity against ME-180 human cervical cancer cell lines. The FTIR spectra confirmed the encapsulation of FA and thermal analysis depicted its degradation profile. A concentration-dependent relationship between FA encapsulation efficiency and FA/ CS-TPP NPs diameter was observed. Smooth and spherical FA-loaded cytocompatible nanoparticles with an average diameter of 125 nm were obtained at 40 lM FA conc. The cytotoxicity of 40 lM FA/CS-TPP NPs against ME-180 cervical cancer cell lines was found to be higher as compared to 40 lM native FA. Apoptotic morphological changes as cytoplasmic remnants and damaged wrinkled cells in ME-180 cells were visualized using scanning electron microscopic and fluorescent microscopic techniques. Data concluded that chitosan enveloped FA nanoparticles could be exploited as an excellent therapeutic drug against cancer cells proliferation.

Nanosystems for the Encapsulation of Natural Products: The Case of Chitosan Biopolymer as a Matrix

“…Chitosan is one of the most widely used encapsulating agents and several reports have been published recently especially for polyphenolic compounds [ 138 ], most of them using the ionotropic gelation method with TPP ( Table 1 ) [ 99 , 101 , 134 , 135 , 138 , 139 , 141 , 142 , 143 , 144 ].…”

“…Ferulic acid ( Figure 4 ) has been encapsulated in chitosan nanoparticles showing improved pharmacokinetic profile [ 145 ] and a range of therapeutic effects [ 142 ] such as lowering high glycemic blood levels and avoiding secondary complications associated with the synthetic drugs in rats [ 146 ] as well as antifungal activity [ 101 ]. Panwara et al [ 141 ] encapsulated ferulic acid in chitosan byionic cross-linking of chitosan with TPP. Smooth and spherical ferulic acid-loaded nanoparticles (NPs) were prepared of an average diameter up to 125 nm which could be exploited as a therapeutic agent against cancer cells proliferation.…”

<p>Improving the solubility and in vitro cytotoxicity (anticancer activity) of ferulic acid by loading it into cyclodextrin nanosponges</p>

“…In Japan, FA has been approved as a sunscreen due to its photoprotective properties 8. The antioxidant activity of FA is related to its phenolic nucleus and unsaturated side chain which contributes to the formation of resonance compounds and acts as an antiproliferative agent 5…”

“…Breast cancer is the first reason of cancer mortality in women. The major strategy for the recovery and treatment of cancer is radiotherapy but because of its undesirable efficacy on normal tissues and also other limitations, such as chemoresistance, immune escape, metastasis, and recurrence, researchers are trying to find new drugs from natural plant-based sources 5,6…”

Ferulic Acid and Naturally Occurring Compounds Bearing a Feruloyl Moiety: A Review on Their Structures, Occurrence, and Potential Health Benefits

“…There are numerous reports describing the anticancer activities of FA. Of particular interest are a number of recent studies that report the cytotoxicity of this molecule toward the human breast (Kampa and others ; Indap and others ; Serafim and others ), Caco‐2 colon (Janicke and others ), histiocytic lymphoma U937 (Chiang and others ), osteosarcoma (Wang and others ), human cervical ME‐180 (Panwar and others ), and melanoma (Yang and others ) cancer cell lines. One of the different routes for the anticancer action of FA and derivatives is the stimulation of uridine diphosphate (UDP) glucuronosyltransferases (UGTs) in the liver, contributing to a better detoxification of potentially carcinogenic compounds and, subsequently, to the prevention of gastrointestinal cancer (van der Logt and others ).…”