The Bifunctional Liposomes Constructed by Poly(2-ethyl-oxazoline)-cholesteryl Methyl Carbonate: an Effectual Approach to Enhance Liposomal Circulation Time, pH-Sensitivity and Endosomal Escape

Abstract

PEtOzylated liposomes exhibits excellent long-circulating and pH-sensitive properties. Our results suggest that PEtOz is a promising biomaterial for the modification of liposome in drug delivery.

Design and evaluation of pH-sensitive liposomes constructed by poly(2-ethyl-2-oxazoline)-cholesterol hemisuccinate for doxorubicin delivery

“…PEtOz2000 and CHEMS were synthesized as previously described [13,27]. The synthesis of PEtOz-CHEMS is shown in Fig.…”

“…Researchers have used PEtOz to synthesize block or graft copolymers [10][11][12], or modify the liposomes [13]. PEtOz is very suitable to the pH-sensitive drug delivery for endosome and other weak acid sites in the tumor tissue.…”

“…Therefore, the PEtOz-modified DDS have a high research value for anticancer drugs and genes [14,15]. Similar to PEG, PEtOz also can increase the stability of liposomes in vitro and in vivo [13,[16][17][18]. Thus, PEtOz can be used as a substitute of PEG for liposome applications.…”

“…Thus, PEtOz can be used as a substitute of PEG for liposome applications. Therefore, long circulating, pH-sensitive liposomes can be obtained when liposomes are modified by PEtOz [13,19].…”

“…However, the high cost and poor stability of phospholipids make industrialization difficult. Cholesterol possesses more excellent properties than DSPE, such as a wide variety of sources, highly stable physical and chemical properties, and low cost [13,20,21], and cholesterol hemisuccinate (CHEMS) has been selected as the lipid fragment to connect with PEG in much literature [20,21]. In this study CHEMS was chosen as the lipid anchor to link with PEtOz.…”