Poly(2-(diethylamino)ethyl methacrylate)-based, pH-responsive, copolymeric mixed micelles for targeting anticancer drug control release

Abstract

We have demonstrated a novel drug delivery system to improve the selectivity of the current chemotherapy by pH-responsive, polymeric micelle carriers. The micelle carriers were prepared by the self-assembly of copolymers containing the polybasic poly(2-(diethylamino) ethyl methacrylate) (PDEAEMA) block. The mixed copolymers exhibited a comparatively low critical micelle concentration (CMC; 1.95–5.25 mg/L). The resultant mixed micelles were found to be <100 nm and were used to encapsulate the anticancer drug doxorubicin (DOX) with pretty good drug-loading content (24%) and entrapment efficiency (55%). Most importantly, the micelle carrier exhibited a pH-dependent conformational conversion and promoted the DOX release at the tumorous pH. Our in vitro studies demonstrated the comparable level of DOX-loaded mixed micelle delivery into tumor cells with the free DOX (80% of the tumor cells were killed after 48 h incubation). The DOX-loaded mixed micelles were effective to inhibit the proliferation of tumor cells after prolonged incubation. Overall, the pH-responsive mixed micelle system provided desirable potential in the controlled release of anticancer therapeutics.

Development of Smart Polymer Microparticles through Suspension Polymerization for Treatment of Schistosomiasis

“…Besides, it becomes clear that acidic media promoted the increase of the rates of PZQ release, confirming once more the formation of pH‐sensitive copolymers. As explained early, the protonation of the amine groups at acidic media lead to hydrophilic structures, promoting the swelling of the particles and therefore the more efficient release of the drug . On the other hand, in basic media it becomes possible to observe the slower release kinetics, ratifying the pH‐sensitive response of the produced copolymers.…”

“…Another approach used to confirm the incorporation of the comonomers into the polymer chains was the evaluation of contact angle analyses in acidic media. It is believed that the diethylaminoethyl and dimethylaminoethyl groups present in PDEAEMA and PDMAEMA, respectively, can be protonated, resulting in more hydrophilic structures . It is known that the increase of the hydrophilicity of the material leads to reduction of the contact angle between the material and the aqueous phase .…”

Antibacterial Amphiphilic Copolymers of Dimethylamino Ethyl Methacrylate and Methyl Methacrylate to Control Biofilm Adhesion for Antifouling Applications

“…Traces of symmetric GPC distribution showed the uniformity of the copolymers via free radical polymerization. [ 30 ]. These unimodal curves showed that the polymerization was completed successfully and that there was no unreacted monomers in the reaction product.…”

“…Samples were washed carefully with phosphate buffer solution (PBS) (1/100 mL) to remove unattached cells and subjected them to SEM fixation. 100–200 µL of 4% para formaldehyde (PFA) was placed on washed samples and allowed to dry for 30–40 min [ 30 , 31 ]. Samples were washed with 25%, 50%, 70% and 100% concentrations of ethanol.…”

In Situ Incorporation of Praziquantel in Polymer Microparticles through Suspension Polymerization for Treatment of Schistosomiasis

“…SEM micrographs shown in Figure 17 show that the copolymer microparticles were spherical but exhibited rough and irregular surfaces, with the formation of some agglomerates. This is certainly due to the higher hydrophilicity of the cationic copolymers, which are partially soluble in water and tend to accumulate on the particle surfaces.…”