Facile route to versatile nanoplatforms for drug delivery by one-pot self-assembly.
There is still unmet demand for developing powerful approaches to produce polymeric nanoplatforms with versatile functions and broad applications, which are essential for the successful bench-to-bedside translation of polymeric nanotherapeutics developed in the laboratory. We have discovered a facile, convenient, cost-effective and easily scalable one-pot strategy to assemble various lipophilic therapeutics bearing carboxyl groups into nanomedicines, through which highly effective cargo loading and nanoparticle formation can be achieved simultaneously. Besides dramatically improving water solubility, the assembled nanopharmaceuticals showed significantly higher bioavailability and much better therapeutic activity. These one-pot assemblies may also serve as nanocontainers to effectively accommodate other highly hydrophobic drugs such as paclitaxel (PTX). PTX nanomedicines thus formulated display strikingly enhanced in vitro antitumor activity and can reverse the multidrug resistance of tumor cells to PTX therapy. The special surface chemistry offers these assembled entities the additional capability of efficiently packaging and efficaciously transfecting plasmid DNA, with a transfection efficiency markedly higher than that of commonly used positive controls. Consequently, this one-pot assembly approach provides a facile route to multifunctional nanoplatforms for simultaneous delivery of multiple therapeutics with improved therapeutic significance.
Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Chongqing 400038, People's Republic of China.
Xing
X
Zhou
Department of Pharmacy, Hospital 309 of PLA, Beijing 100091, People's Republic of China.
Ling
L
Che
Department of Gastroenterology, Daping Hospital, Third Military Medical University, Chongqing 400042, People's Republic of China.
Yanling
Y
Wei
Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Chongqing 400038, People's Republic of China.
Yin
Y
Dou
Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Chongqing 400038, People's Republic of China.
Sha
S
Chen
Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Chongqing 400038, People's Republic of China.
Hongmei
H
He
Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Chongqing 400038, People's Republic of China.
Hao
H
Gong
Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Chongqing 400038, People's Republic of China. Electronic address: lpsh008@yahoo.com.cn.
Xiaohui
X
Li
Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Chongqing 400038, People's Republic of China. Electronic address: jxzhang1980@gmail.com.
Jianxiang
J
Zhang
D000818:Animals; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D006801:Humans; D008297:Male; D036103:Nanotechnology; D051381:Rats; D017207:Rats, Sprague-Dawley
Drug delivery; Gene therapy; Nanomedicine; Nanoparticle; Self-assembly