Co-delivery of doxorubicin and AS1411 aptamer by poly(ethylene glycol)-poly(β-amino esters) polymeric micelles for targeted cancer therapy

pH-Control in Aptamer-Based Diagnostics, Therapeutics, and Analytical Applications

“…Many systems incorporating both aptamers and pH responsive elements have been developed for the targeted delivery of anti-cancer drugs [ 7 , 13 , 14 ]. Often, chemotherapeutics cause off-target toxicity; directed delivery can increase the effectiveness of the drugs and reduce adverse effects [ 14 ]. Biomarkers that are only found, or are overexpressed, on cancerous cells are key targets for drug carriers [ 15 ].…”

“…In many cases, superior targeting is achieved by conjugating aptamers to a separate pH-responsive drug carrier mechanism [ 16 ]. One popular method of drug delivery is the encapsulation of a hydrophobic drug within the core of a polymeric micelle; the hydrophilic exterior of the micelle can then be conjugated with targeting ligands or other coatings to increase longevity in the system [ 14 ]. In 2015, Zhang et al designed artificial micelles composed of two polymers: one pH-responsive, and one decorated with aptamers targeting nucleolin, a membrane protein overexpressed on cancer cells that allows internalization when bound by an aptamer [ 10 ].…”

“…The aptamer was encapsulated inside the pH responsive artificial micelles, which were used to improve uptake and release of the therapeutic aptamer intracellularly [ 23 ]. In 2017, Zhang et al designed a polymeric, pH-sensitive micelle for the delivery of both doxorubicin and a therapeutic aptamer for nucleolin [ 14 ]. The aptamer, AS1411, had previously been shown to inhibit tumour growth; additionally, it can bind to and trigger internalization into a tumour cell [ 14 ].…”

“…In 2017, Zhang et al designed a polymeric, pH-sensitive micelle for the delivery of both doxorubicin and a therapeutic aptamer for nucleolin [ 14 ]. The aptamer, AS1411, had previously been shown to inhibit tumour growth; additionally, it can bind to and trigger internalization into a tumour cell [ 14 ]. The micelle carried doxorubicin within its hydrophobic core, while the aptamer was attached electrostatically to the hydrophilic exterior [ 14 ].…”

“…The aptamer, AS1411, had previously been shown to inhibit tumour growth; additionally, it can bind to and trigger internalization into a tumour cell [ 14 ]. The micelle carried doxorubicin within its hydrophobic core, while the aptamer was attached electrostatically to the hydrophilic exterior [ 14 ]. After the nanoparticle was internalized, the pH-responsive polymer dissociated within the endosome and the drug and aptamer were released [ 14 ].…”