Synthesis, physicochemical characterization, and in vitro evaluation of biodegradable PLGA nanoparticles entrapped to folic acid for targeted delivery of kaempferitrin

Abstract

Polymeric nanoparticles are widely studied in the treatment of colorectal cancer. Kaempferitrin-loaded nontoxic and biodegradable poly(d,l-lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) developed by the solvent emulsion evaporation method by improving its solubility and bioavailability. In order to improve the delivery of kaempferitrin (KM) to cancerous cells, folic acid (FA) combined kaempfertrin PLGA NPs were prepared. The goal of the study was whether PLGA NPs with surface KM and FA could help to prevent colorectal cancer. The synthesis of KM with FA in a nanomedicine could be crucial in the development of colon cancer chemotherapeutics. The physicochemical characteristics of synthesized KM-entrapped PLGA NPs were investigated by XRD, FTIR, zeta potential, and TEM. The KM + FA + PLGA NPs showed particle size with 132.9 ± 1.4 nm, zeta potential -15.0 ± 1.73 mV, encapsulation efficiency 67.92 ± 4.8, and drugloading capacity 0.463 ± 0.173. In vitro cytotoxicity study on HT-29 cell lines using the MTT assay, the apoptotic study revealed that KM + FA + PLGA NPs have an enhanced cytotoxic effect compared to the KM + PLGA NPs drug solution. These findings suggested that KM + FA + PLGA NPs could be an effective chemotherapeutic drug delivery system in colon adenocarcinoma HT-29 cells.

Targeting the Gut: A Systematic Review of Specific Drug Nanocarriers

“…Folate receptor, a glycosyl-phosphatidyl-inositol anchored on the cell surface, is overexpressed in most cancers, enabling their targeting by functionalization of the nanocarrier with folic acid (FA) [ 240 , 241 , 242 , 243 , 244 , 245 ]. Functionalization with FA improved the specific delivery to cancer cells and also had a combined chemo/magnetothermal therapeutic effect [ 90 , 202 , 246 , 247 , 248 , 249 , 250 , 251 ].…”

“…In such a disease, several membrane proteins are known to be overexpressed and can be used as targets to enable specific drug delivery. This is the case with CD44, EGFR, or the folate receptor, among others [ 22 , 226 , 231 , 240 , 241 , 242 , 243 , 244 , 245 ] ( Table 2 ). The only strategy that seems to allow specific binding to the gut epithelium, independently of its physiological or pathological condition, involves WGA.…”

Research Advances of Lipid Nanoparticles in the Treatment of Colorectal Cancer

“…Folate-bound Poly (lactic-co-glycolic acid) (PLGA) NPs loaded with kaempferitrin demonstrated enhanced cytotoxicity against colorectal cancer cells. 130 A recent study analyzing four biomarkers in colorectal cancer tissues from 280 patients via immunohistochemistry revealed increased expression of FR-α (37.1%) compared to normal tissues, along with elevated levels of carcinoembryonic antigen (CEA) (98.8%), tumor-associated glycoprotein-72 (79%), and epidermal growth factor receptor (EGFR) (32.8%) in CRC, highlighting CEA’s potential as a future LNP drug target for CRC. 128 CD44 is a common marker of cancer stem cells (CSCs) in colon cancer and is also highly expressed.…”

Theranostics Nanomedicine Applications for Colorectal Cancer and Metastasis: Recent Advances

“…Antibodies, peptides, sugar chains, and nucleic acid aptamers are just a few examples of probe molecules that can precisely attach to the target molecule and are connected to the carrier surface by chemical or physical means. Utilizing ligands that bind to tumor cells can boost the percentage of nano-drugs that reach the target [80].…”