Effect of Hydrophobicity of Core on the Anticancer Efficiency of Micelles as Drug Delivery Carriers

Abstract

Recently, micelles, which are self-assembled by amphiphilic copolymers, have attracted tremendous attention as promising drug delivery systems for cancer treatment. Thus, the hydrophobic core of the micelles, which could efficiently encapsulate small molecular drug, will play a significant role for the anticancer efficiency. Unfortunately, the effect of hydrophobicity of micellar core on its anticancer efficiency was rarely reported. Herein, the amphiphilic diblock polymers of poly(ethylene glycol) and polyphosphoester with different side groups (butyl, hexyl, octyl) were synthesized to tune the hydrophobicity of the micellar core. We found that the in vitro cytotoxicity of the DOX-loaded micelles decreased with the increasing hydrophobicity of micellar core due to the drug release rate. However, following systemic delivery, the DOX-loaded micelles with the most hydrophobic core exhibited the most significant inhibition of tumor growth in a MDA-MB-231 tumor model, indicating the importance of hydrophobicity of core on the antitumor efficacy of drug delivery systems.

Chlorin e6-Encapsulated Polyphosphoester Based Nanocarriers with Viscous Flow Core for Effective Treatment of Pancreatic Cancer

“…Similar released profile of the encapsulated drug was also observed previously. 28 To demonstrate the reason, the CMC of mPEG 45 -b-PHEP 60 at pH 7.4 and pH 5.5 was detected. From the sigmoidal shape curve in Figure S3, the CMC values were calculated as 1.3×10 -3 mg/mL at pH 7.4 and which was resulted from the chemical hydrolysis of DCFH-DA at basic pH.…”

“…28 Herein, we developed photosensitizers loaded polyphosphoester based nanocarriers for near-infrared light (NIR) photodynamic therapy (Scheme 1). Chlorin e6 (Ce6) was selected as the photosensitizers since its high sensitizing efficacy and high fluorescent emission at long wavelengths of 660-670 nm, which can offer a clear window and ideal penetration for optical image and PDT in vivo.…”

“…The critical micelle concentration (CMC) of the obtained amphiphilic copolymers mPEG-b-PHEP was detected using the fluorescence probe pyrene as previously described. 28 Preparation and characterization of Ce6-loaded polyphosphoester based nanocarriers (NP-PPE/Ce6). Firstly, photosensitizer Ce6 (10.0 mg/mL in DMSO, 0.1 mL) and polymer mPEG 45 -b-PHEP 60 (10.0 mg/mL in DMSO, 1.0 mL) were mixed and stirred for 20 minutes.…”

Polyphosphoesters: New Trends in Synthesis and Drug Delivery Applications

“…By this reaction, a range of cyclic phosphotriester having R′ = H and various R groups that include alkyl chains of various size (methyl to octyl) and unsaturated chains (allyl, butenyl, butynyl, acrylate) has been obtained in good purity enough to be polymerized by the ROP process. However, the purification of these monomers that are highly sensitive toward traces of water or other protic species that easily open the ring, remains a tedious step.…”

HDAC inhibitor conjugated polymeric prodrug micelles for doxorubicin delivery

“…4 Amphiphilic diblock copolymers of PEG and polyphosphoester with different side groups (butyl, hexyl, octyl) have been reported to tune the hydrophobicity of the micellar core. 5 Widely used core-forming hydrophobic polymers for drug delivery can be classified into the following groups: poly(propylene oxide) (PPO), 6 poly(esters) such as poly(lactic acid) 7 and poly(ε-caprolactone) (PCL), 8, 9 poly(L-amino acids) such as poly(L-lysine), 10 and polystyrene. 11 The encapsulation of drug within hydrophobic cores constructed from these polymers mainly occurs via hydrophobic interactions that are thermodynamically driven.…”