Drug Delivery | VOL. 23

5-Fluorouracil enteric-coated nanoparticles for improved apoptotic activity and therapeutic index in treating colorectal cancer

Publication Date Oct 12, 2016


5-Fluorouracil (5-FU) is one among the anti-cancer agents in FOLFORINOX treatment along with oxaliplatin and irinotecan for the treatment of colorectal cancer. Despite its potential activity on the tumor cells, it lacks site specificity partly attributed by its biodistribution to healthy cells resulting in toxic effects to healthy cells. Therefore, we have formulated 5-fluorouracil enteric-coated nanoparticles (5-FUEC) to localize the drug in the colon area that enables its prolonged presence in target area in a sustained manner. The current work emphasizes on enhanced anti-cancer activity of 5-FUEC sequencing its apoptotic activity on HCT 116 colorectal cancer cell lines in vitro. MTT assay exhibited 5.5-fold decrease in IC50 value of nanoparticles comparable to 5-FU. Nuclear fragmentation with irregular edges in nucleus of cells justified its improved activity. Furthermore, flow cytometric analysis confirms the majority of cells gated in early apoptotic (39.75%) and late apoptotic phase (36.25%). Acridine orange/ethidium bromide staining (AO/EB) exhibited cells with red fluorescence (indicating apoptosis) comparable to the control and 5-FU. γ-Scintigraphic studies determined the applicability and feasibility of the enteric coating with mean gastric emptying time, mean intestinal transit time and mean colon arrival time of 1.89 ± 0.03, 2.15 ± 0.05 and 4.03 ± 0.27 h, respectively. Moreover, nanoparticulate approach was found significant in reducing tumor size and volume in xenograft tumor models in vivo along with sustained ...


Mean Intestinal Transit Time Mean Gastric Emptying Time Colorectal Cancer Reducing Tumor Size Irregular Edges Nanoparticulate Approach Prolonged Presence Xenograft Tumor Models Bromide Staining Nuclear Fragmentation

Round-ups are the summaries of handpicked papers around trending topics published every week. These would enable you to scan through a collection of papers and decide if the paper is relevant to you before actually investing time into reading it.

Coronavirus Research Articles published between Jan 30, 2023 to Feb 05, 2023

R DiscoveryFeb 06, 2023
R DiscoveryArticles Included:  5

The Coronavirus Disease 2019 (COVID-19), caused by Severe Acute Respiratory Syndrome Coronavirus type 2 (SARS-CoV-2), belongs to emerging and reemergi...

Read More

Climate change Research Articles published between Jan 30, 2023 to Feb 05, 2023

R DiscoveryFeb 06, 2023
R DiscoveryArticles Included:  3

Introduction: The IOC and the Olympic Games have made a visible transition toward sustainability in the last two decades. While the IOC has acknowledg...

Read More

Gender Equality Research Articles published between Jan 30, 2023 to Feb 05, 2023

R DiscoveryFeb 06, 2023
R DiscoveryArticles Included:  5

Gender inequity in Science, Technology, Engineering, and Medicine (STEM) fields, including parasitology, continues to limit the participation of women...

Read More

Coronavirus Pandemic

You can also read COVID related content on R COVID-19

R ProductsCOVID-19


Creating the world’s largest AI-driven & human-curated collection of research, news, expert recommendations and educational resources on COVID-19

COVID-19 Dashboard

Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on “as is” basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The Copyright Law.