TY - JOUR
T1 - pH-responsive hyaluronate-anchored extracellular vesicles to promote tumor-targeted drug delivery
AU - Lee, Hyuk
AU - Park, Hongsuk
AU - Noh, Gwang Jin
AU - Lee, Eun Seong
N1 - Publisher Copyright:
© 2018 Elsevier Ltd
PY - 2018/12/15
Y1 - 2018/12/15
N2 - pH-Responsive drug vehicles targeting the specific extracellular pH of tumors have served as potent tools to overcome the limitation (e.g., low tumor seletivity) in antitumor drug delivery system. Here, we describe the advantage of pH-responsive extracellular vesicles (HDEA@EVs) containing the hyaluronic acid grafted with 3-(diethylamino)propylamine (HDEA) and a model antitumor drug, doxorubicin (DOX). We demonstrated their physicochemical characteristics through in vitro cell endocytosis, in vitro tumor cell toxicity, in vivo biodistribution, and in vivo tumor regression efficacy experiments. Because the HDEA@EVs efficiently responded to extracellular tumor pH (pH 6.5) and actively bound to CD44 receptors on HCT-116 tumor cells, the EVs selectively inhibited CD44+ tumor cell growth in vitro, and CD44+ tumor development in vivo. From these results, we conclude that HDEA@EVs can help in designing effective strategies for pharmacologic intervention in tumor therapy.
AB - pH-Responsive drug vehicles targeting the specific extracellular pH of tumors have served as potent tools to overcome the limitation (e.g., low tumor seletivity) in antitumor drug delivery system. Here, we describe the advantage of pH-responsive extracellular vesicles (HDEA@EVs) containing the hyaluronic acid grafted with 3-(diethylamino)propylamine (HDEA) and a model antitumor drug, doxorubicin (DOX). We demonstrated their physicochemical characteristics through in vitro cell endocytosis, in vitro tumor cell toxicity, in vivo biodistribution, and in vivo tumor regression efficacy experiments. Because the HDEA@EVs efficiently responded to extracellular tumor pH (pH 6.5) and actively bound to CD44 receptors on HCT-116 tumor cells, the EVs selectively inhibited CD44+ tumor cell growth in vitro, and CD44+ tumor development in vivo. From these results, we conclude that HDEA@EVs can help in designing effective strategies for pharmacologic intervention in tumor therapy.
KW - CD44 receptor
KW - Extracellular tumor pH
KW - Extracellular vesicle
KW - Tumor therapy
KW - pH-Responsive hyaluronic acid
UR - http://www.scopus.com/inward/record.url?scp=85053054755&partnerID=8YFLogxK
U2 - 10.1016/j.carbpol.2018.08.141
DO - 10.1016/j.carbpol.2018.08.141
M3 - Article
C2 - 30287007
AN - SCOPUS:85053054755
SN - 0144-8617
VL - 202
SP - 323
EP - 333
JO - Carbohydrate Polymers
JF - Carbohydrate Polymers
ER -