Polymersomes: Synthesis and Applications

Abstract

Compartmentalization, that is the separation into discrete compartments deputed to absolve precise functions, is paramount for most biological systems. Natural cells possess suitable structures called membranes, formed by amphiphilic molecules. In an effort to mimic and improve these structures and exploit them for research, diagnostic and therapeutic purposes, about 20 years ago the polymersome technology was born. Polymersomes are self‐assembled structures formed by synthetic amphiphilic block copolymers. Their physicochemical characteristics make them extremely attractive nanosystems for loading and delivering all sorts of cargos, ranging from small drug molecules and reporters to proteins to DNA, all the way up to the actual generation of artificial cell organelles. In this chapter, we will discuss different aspects related to this technology, ranging from synthetic polymer chemistry up to polymersome production and cargo encapsulation approaches, and eventually concluding with their physicochemical behavior and latest biological applications.

Polymers and Polymer Nanocomposites for Cancer Therapy

“…Polymersomes have attracted much attention as versatile carriers due to their tunable membrane properties and ability to encapsulate or integrate a broad range of drugs. A long blood circulation time can be accomplished when PEG is used as a component of the block copolymer membrane, which contributes to good responses to various internal or external stimuli [119].…”

“…Polymersomes are increasingly being used as platforms for simultaneous drug delivery and imaging and are therefore becoming popular theranostic products. Examples of polymersome block copolymers are poly(acrylic acid-co-distearate acrylate), the poly(trimethylene carbonate)-co-poly(Lglutamic acid) copolymer, polybutadiene-b-PEO (PB-b-PEO), poly(ethyl ethylene)-b-PEO (PEE-b-PEO), and PS-b-PEO [119,122].…”

Engineering Polymeric Nanosystems against Oral Diseases

“…In terms of loading of the active payload (e.g., drugs, DNA/RNA or proteins) into the NPs, this can be either dispersed/embedded/encapsulated into the polymer matrix or alternatively it can be adsorbed onto the surface of NPs [ 13 , 35 , 114 , 115 , 116 ]. In this case, though, the interaction between NPs and bioactives might be relatively weak, therefore potentially causing issues with the overall stability of the designed NPs (e.g., upon storage) as well as potential burst-release effects when administered [ 13 , 117 ]. An important advantage of the encapsulation/loading process is related to the potential improvement of undesired properties of the bioactive itself.…”

“…In an effort to treat intracellular bacteria responsible for periodontitis (e.g., P. Gingivalis ), also self-assembled block-copolymer vesicles (a.k.a., polymersomes ) [ 13 , 150 , 151 , 152 , 153 , 154 , 155 ] were used to deliver metronidazole or Dox. Wayakanon et al prepared polymersomes by self-assembly of amphiphilic poly [2-(methacryloy-loxy)ethyl phosphorylcholine] (PMPC) and poly [2-(di-isopropylamino)ethyl methacrylate] (PDPA) block co-polymers [ 156 , 157 , 158 ], reducing the number of intracellular P. gingivalis in patient-derived oral keratinocytes and fibroblasts, as well as organotypic cultures compared to unloaded polymersomes and free drugs used as controls [ 159 ].…”

“…The popularity of NPs originates from the intriguing characteristics deriving precisely from the small scale, which include an extremely high-surface area to volume, but coupled with synthetic versatility which results in adjustable surface charge, tailorable cargo-loading and cargo-release capability, and ultimately versatility for the surface decoration with specific chemical moieties. This latter feature, together with the type of material (e.g., polymers) used for the fabrication, can guarantee extremely high biocompatibility/biodegradability, paramount in the case of healthcare and drug-delivery applications in medicine and dentistry [ 12 , 13 , 14 ].…”