Preparation of Doxorubicin-Loaded Amphiphilic Poly(D,L-Lactide-Co-Glycolide)-b-Poly(N-Acryloylmorpholine) AB2 Miktoarm Star Block Copolymers for Anticancer Drug Delivery

Abstract

Owing to their unique topology and physical properties, micelles based on miktoarm amphiphilic star block copolymers play an important role in the biomedical field for drug delivery. Herein, we developed a series of AB2-type poly(D,L-lactide-co-glycolide)-b-poly(N-acryloyl morpholine) (PLGA-b-PNAM2) miktoarm star block copolymers by reversible addition–fragmentation chain–transfer polymerization and ring-opening copolymerization. The resulting miktoarm star polymers were investigated by 1H NMR spectroscopy and gel permeation chromatography. The critical micellar concentration value of the micelles increases with an increase in PNAM block length. As revealed by transmission electron microscopy and dynamic light scattering, the amphiphilic miktoarm star block copolymers can self-assemble to form spherical micellar aggregates in water. The anticancer drug doxorubicin (DOX) was encapsulated by polymeric micelles; the drug-loading efficiency and drug-loading content of the DOX-loaded micelles were 81.7% and 9.1%, respectively. Acidic environments triggered the dissociation of the polymeric micelles, which led to the more release of DOX in pH 6.4 than pH 7.4. The amphiphilic PLGA-b-PNAM2 miktoarm star block copolymers may have broad application as nanocarriers for controlled drug delivery.

Poly(N-acryloylmorpholine) Nanogels as Promising Materials for Biomedical Applications: Low Protein Adhesion and High Colloidal Stability

“…In the area of drug delivery, the utilization of P­(NAM) is still in its infancy. Up to now, only a few reports have focused on its utilization as the hydrophilic backbone in polymer drug conjugates or as the hydrophilic component in amphiphilic block copolymer micelles. − In addition, P­(NAM) was used to modify the surface of the synthetic liposomes with a hydrophilic shell. Here, it was shown that its protein-repellent properties were able to increase circulation time and prevent accelerated blood clearance in rats …”

Fully Automated Multi-Step Synthesis of Block Copolymers

“…Furthermore, copolymers containing, e.g., poly(ethylene oxide) as hydrophilic block and poly(L-amino acid) as hydrophobic block, can aggregate in water to micelles [6]. The core of the micelles can be loaded with a drug for the use as long-circulating drug carriers [7,8].…”

Improvement of High-Throughput Experimentation Using Synthesis Robots by the Implementation of Tailor-Made Sensors

“…An additional procedure for postpolymerization modification is the degradation of the end group by irradiation with UV light [ 29 ]. After such an end-group modification, these polymers can be applied, e.g., for optoelectronic applications [ 30 ] or pharmaceutical purposes such as drug [ 31 ] or gene delivery [ 32 ].…”