Asymmetrical Polymer Vesicles with a “Stealthy”
Outer Corona and an Endosomal-Escape-Accelerating Inner Corona for
Efficient Intracellular Anticancer Drug Delivery
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Abstract
The efficient intracellular
drug delivery is an important challenge
due to the slow endocytosis and inefficient drug release of traditional
delivery vehicles such as symmetrical polymer vesicles, which have
the same coronas on both sides of the membrane. Presented in this
paper is a noncytotoxic poly(ethylene oxide)-<i>block</i>-poly(caprolactone)-<i>block</i>-poly(acrylic acid) (PEO<sub>113</sub>-<i>b</i>-PCL<sub>132</sub>-<i>b</i>-PAA<sub>15</sub>) triblock copolymer vesicle with an asymmetrical
structure. The biocompatible exterior PEO coronas are designed for
stealthy drug delivery; The pH-responsive interior PAA chains are
designed for rapid endosomal escape and enhanced drug loading efficiency.
The hydrophobic PCL vesicle membrane is for biodegradation. Such asymmetrical
polymer vesicle showed high doxorubicin (DOX) loading efficiency and
good biodegradability under extracellular enzymatic conditions. Compared
with three traditional symmetrical vesicles prepared from PEO<sub>113</sub>-<i>b</i>-PCL<sub>110</sub>, PEO<sub>43</sub>-<i>b</i>-PCL<sub>98</sub>-<i>b</i>-PAA<sub>25</sub>,
and PAA<sub>21</sub>-<i>b</i>-PCL<sub>75</sub> copolymers,
the DOX-loaded asymmetrical PEO<sub>113</sub>-<i>b</i>-PCL<sub>132</sub>-<i>b</i>-PAA<sub>15</sub> polymer vesicles exhibited
rapid endocytosis rate and much faster endosomal escape ability, demonstrating
promising potential applications in nanomedicine