A facile method for anti-cancer drug encapsulation into polymersomes with a core-satellite structure

Abstract

Polymersomes possess the self-assembly vesicular structure similar to liposomes. Although a variety of comparisons between polymersomes and liposomes in the aspects of physical properties, preparation and applications have been elaborated in many studies, few focus on their differences in drug encapsulation, delivery and release in vitro and in vivo. In the present work, we have provided a modified direct hydration method to encapsulate anti-cancer drug paclitaxel (PTX) into PEG- b -PCL constituted polymersomes (PTX@PS). In addition to advantages including narrow particle size distribution, high colloid stability and moderate drug-loading efficiency, we find that the loaded drug aggregate in small clusters and reside through the polymersome membrane, representing a unique core-satellite structure which might facilitate the sustained drug release. Compared with commercial liposomal PTX formulation (Lipusu ® ), PTX@PS exhibited superb tumor cell killing ability underlain by multiple pro-apoptotic mechanisms. Moreover, endocytic process of PTX@PS significantly inhibits drug transporter P-gp expression which could be largely activated by free drug diffusion. In glioma mice models, it has also confirmed that PTX@PS remarkably eradicate tumors, which renders polymersomes as a promising alternative to liposomes as drug carriers in clinic.

Cupric-polymeric nanoreactors integrate into copper metabolism to promote chronic diabetic wounds healing

“…To address the overexposure risks induced by CuONPs, polymersomes fabricated by an amphiphilic block copolymer PEG- b -PCL, were employed to incorporate CuONPs to form cupric-polymeric nanoreactors (CuO@PS) via a modified direct hydration method [ 35 , 37 ], by which block polymers and payloads self-assembled into a polymersome in aqueous solution under benign conditions (50 °C, 2 h). In contrast to classical methods such as solvent-exchange or thin film hydration [ 40 ], the direct hydration method would allow CuONPs to directly load into the hydrophilic core of polymersomes without any organic solvents contaminated ( Scheme 1 A).…”

“…Poly (ethylene glycol)-block-poly (ε-caprolactone) (PEG- b -PCL, PEG Mw = 2000, PCL Mw = 4300) was synthesized based on our previous work [ 35 ]; Copper (II) acetate, Poly (ethylene glycol) 550 (PEG 550), hydrogen peroxide (H 2 O 2 , 30 %), Ferrous chloride (FeCl 2 ), Rhodamine B were purchased form Macklin, China; Sephadex G-50 was bought from Shanghai Yuanye Bio-Technology, China; phosphotungstic acid hydrate, lipopolysaccharide (LPS), Pluronic F-127, fluorescein isothiocyanate (FITC), Bis(cyclohexanone)oxaldihydrazone (BCO) and Streptozotocin (STZ) were purchased from Sigma Aldrich, USA. O 2 .- scavenging assay kit (WST-8 method), cell counting kit-8 (CCK-8) were purchased from Abbkine Scientific, China.…”

Polymersomes as the Next Attractive Generation of Drug Delivery Systems: Definition, Synthesis and Applications

“…In this method, an organic phase is created by dissolving block copolymers in an adequate organic solvent. After that, an aqueous solution is gradually added to the mixture, and polymers are dispersed in the aqueous phase, resulting in self-assembled structures [86]. An organic solvent can be poly(ethylene glycol) dimethyl ether with 500 Da (PEG 500 DME), which yields polymersomes with high encapsulation efficiencies [87], or oligo(ethylene glycol) (OEG) [8], a nontoxic solvent with low molecular weight [88].…”

Progress in the Treatment of Central Nervous System Diseases Based on Nanosized Traditional Chinese Medicine

“…Notably, it downregulated the expression of the drug transporter P‐glycoprotein during passive transcellular diffusion, thus overcoming drug resistance. [ 350 ]…”