Hydrophobic Drug-Loaded PEGylated Magnetic Liposomes for Drug-Controlled Release

Abstract

Less targeted and limited solubility of hydrophobic-based drug are one of the serious obstacles in drug delivery system. Thus, new strategies to enhance the solubility of hydrophobic drug and controlled release behaviors would be developed. Herein, curcumin, a model of hydrophobic drug, has been loaded into PEGylated magnetic liposomes as a drug carrier platform for drug controlled release system. Inductive magnetic heating (hyperthermia)-stimulated drug release, in vitro cellular cytotoxicity assay of curcumin-loaded PEGylated magnetic liposomes and cellular internalization-induced by magnetic guidance would be investigated. The resultant of drug carriers could disperse homogeneously in aqueous solution, showing a superparamagnetic characteristic and could inductive magnetic heating with external high-frequency magnetic field (HFMF). In vitro curcumin release studies confirmed that the drug carriers exhibited no significant release at 37 °C, whereas exhibited rapid releasing at 45 °C. However, it would display enormous (three times higher) curcumin releasing under the HFMF exposure, compared with that without HFMF exposure at 45 °C. In vitro cytotoxicity test shows that curcumin-loaded PEGylated magnetic liposomes could efficiently kill MCF-7 cells in parallel with increasing curcumin concentration. Fluorescence microscopy observed that these drug carriers could internalize efficiently into the cellular compartment of MCF-7 cells. Thus, it would be anticipated that the novel hydrophobic drug-loaded PEGylated magnetic liposomes in combination with inductive magnetic heating are promising to apply in the combination of chemotherapy and thermotherapy for cancer therapy.

Tailoring Iron Oxide Nanoparticles for Efficient Cellular Internalization and Endosomal Escape

“…This is mainly because the formed lipoplexes increase the distribution of nanoconjugates in the cytosol of cells in the tissues of interest [ 273 , 275 ]. Hardiansyah and colleagues synthesized anionic magnetoliposomes with 19 mol% cholesterol and 4.8 mol% PEGylation that efficiently escaped endosomes and, combined with a magnetic field, successfully enabled the time-controlled release of cargoes [ 278 ]. In the same way, Amstad and colleagues demonstrated that palmityl-nitroDOPA coated IONs encapsulated in 5 mol% PEGylated zwitterionic liposomes internalized effectively and escaped endosomes.…”

pH-Responsive Charge-Conversional and Hemolytic Activities of Magnetic Nanocomposite Particles for Cell-Targeted Hyperthermia

“…In another approach, PEGylated magnetic liposomes 39 were fabricated by conjugating poly(ethylene glycol) (PEG) to the liposome surface, reported to enhance the accumulation of liposomes in tumor cells through the enhanced permeation and retention effect facilitated by their long circulation time. 13 , 47 However, the excessively hydrated shell of PEGylated liposomes causes a severe problem associated with their limited cellular uptake in targeted areas, resulting in nonselective cell heating. 14 , 16 Strategies to improve targeting ability have introduced stimuli-responsive (temperature, light, sound, pH, etc.)…”

Recent advances in the bioanalytical methods of polyethylene glycols and PEGylated pharmaceuticals

“…Hardiansyah et al. reported a PEGylated magnetic liposome system as a drug carrier for hydrophobic drugs [122]. With the help of passive targeting mechanism of liposomes and magnetic targeting under the exposure to external magnetic fields, the magnetic liposomes are assumed to be accumulated in targeted tumor site.…”