Biological Therapy of Cancer

Avendaño, Carmen; Menéndez, J. Carlos

doi:10.1016/b978-0-444-62649-3.00012-0

Cited by 1 publication

(1 citation statement)

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“…1 The current possible treatments fall between one of the following categories: surgical therapy, radiotherapy, chemotherapy, hormone therapy, immunotherapy, and gene therapy. 2 Even though perceptible progression with all of these categories is marked, recent investigations focus on the discovery of more anticancer drugs and biotechnology products. 3 These include, but not restricted to the exploration of novel alkylating agents, antimetabolites, anti-microtubules, topoisomerase inhibitors, and cytotoxic antibiotics that are adhering with the stated goal of cancer chemotherapy.…”

Section: Introductionmentioning

confidence: 99%

Enhanced anticancer activity and oral bioavailability of ellagic acid through encapsulation in biodegradable polymeric nanoparticles

Mady¹,

Shaker²

2017

IJN

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Despite the fact that various studies have investigated the clinical relevance of ellagic acid (EA) as a naturally existing bioactive substance in cancer therapy, little has been reported regarding the efficient strategy for improving its oral bioavailability. In this study, we report the formulation of EA-loaded nanoparticles (EA-NPs) to find a way to enhance its bioactivity as well as bioavailability after oral administration. Poly(ε-caprolactone) (PCL) was selected as the biodegradable polymer for the formulation of EA-NPs through the emulsion–diffusion–evaporation technique. The obtained NPs have been characterized by measuring particle size, zeta potential, Fourier transform infrared, differential scanning calorimetry, and X-ray diffraction. The entrapment efficiency and the release profile of EA was also determined. In vitro cellular uptake and cytotoxicity of the obtained NPs were evaluated using Caco-2 and HCT-116 cell lines, respectively. Moreover, in vivo study has been performed to measure the oral bioavailability of EA-NPs compared to free EA, using New Zealand white rabbits. NPs with distinct shape were obtained with high entrapment and loading efficiencies. Diffusion-driven release profile of EA from the prepared NPs was determined. EA-NP-treated HCT-116 cells showed relatively lower cell viability compared to free EA-treated cells. Fluorometric imaging revealed the cellular uptake and efficient localization of EA-NPs in the nuclear region of Caco-2 cells. In vivo testing revealed that the oral administration of EA-NPs produced a 3.6 times increase in the area under the curve compared to that of EA. From these results, it can be concluded that incorporation of EA into PCL as NPs enhances its oral bioavailability and activity.

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Section: Introductionmentioning

confidence: 99%