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National Institute of Environmental Health Sciences

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Your Environment. Your Health.

Publication Detail

Title: Exosomal formulation of anthocyanidins against multiple cancer types.

Authors: Munagala, Radha; Aqil, Farrukh; Jeyabalan, Jeyaprakash; Agrawal, Ashish K; Mudd, Ashley M; Kyakulaga, Al Hassan; Singh, Inder P; Vadhanam, Manicka V; Gupta, Ramesh C

Published In Cancer Lett, (2017 May 01)

Abstract: Over the last two decades, berries and berry bioactives, particularly anthocyanins and their aglycones anthocyanidins (Anthos) have demonstrated excellent anti-oxidant, anti-proliferative, apoptotic and anti-inflammatory properties. However, their physicochemical and pharmacokinetic limitations such as, low permeability, and poor oral bioavailability are considered as unfavorable properties for development as drugs. Therefore there is a need to develop systems for efficient systemic delivery and robust bioavailability. In this study we prepared nano-formulation of bilberry-derived Anthos using exosomes harvested from raw bovine milk. Exosomal formulation of Anthos enhanced antiproliferative and anti-inflammatory effects compared with the free Anthos against various cancer cells in vitro. Our data also showed significantly enhanced therapeutic response of exosomal-Anthos formulation compared with the free Anthos against lung cancer tumor xenograft in nude mice. The Anthos showed no signs of gross or systemic toxicity in wild-type mice. Thus, exosomes provide an effective alternative for oral delivery of Anthos that is efficacious, cost-effective, and safe, and this regimen can be developed as a non-toxic, widely applicable therapeutic agent.

PubMed ID: 28202351 Exiting the NIEHS site

MeSH Terms: A549 Cells; Administration, Oral; Animals; Anthocyanins/chemistry; Anthocyanins/pharmacology*; Anti-Inflammatory Agents/administration & dosage; Anti-Inflammatory Agents/chemistry; Anti-Inflammatory Agents/pharmacology*; Antineoplastic Agents, Phytogenic/administration & dosage; Antineoplastic Agents, Phytogenic/chemistry; Antineoplastic Agents, Phytogenic/pharmacology*; Cell Proliferation/drug effects; Dose-Response Relationship, Drug; Drug Carriers*; Drug Compounding; Exosomes/chemistry*; Female; HCT116 Cells; Humans; MCF-7 Cells; Male; Mice, Nude; Milk/chemistry*; Milk/toxicity; Nanoparticles; Time Factors; Tumor Burden/drug effects; Xenograft Model Antitumor Assays

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