%0 Journal Article
%T pH-Responsive Triblock Copolymeric Micelles Decorated with a Cell-Penetrating Peptide Provide Efficient Doxorubicin Delivery
%A Adeel Masood Butt
%A Arun K. Iyer
%A Haliza Katas
%A Khen Eng Ng
%A Mohd Cairul Iqbal Mohd Amin
%A Muhammad Wahab Amjad
%A Prashant Kesharwani
%J Archive of "Nanoscale Research Letters".
%D 2016
%R 10.1186/s11671-016-1755-4
%X This study developed novel triblock pH-responsive polymeric micelles (PMs) using cholic acid-polyethyleneimine-poly-l-arginine (CA-PEI-pArg) copolymers. PEI provided pH sensitivity, while the hydrophilic cell-penetrating pArg peptide promoted cellular PM internalization. The copolymers self-assembled into PMs in aqueous solution at above the critical micelle concentration (2.98£¿¡Á£¿10£¿7 M) and encapsulated doxorubicin in the core region, with a 34.2% (w/w) entrapment efficiency. PMs showed pH-dependent swelling, increasing in size by almost sevenfold from pH 7.4 to 5.0. Doxorubicin release was pH-dependent, with about 65% released at pH 5.0, and 32% at pH 7.4. Cellular uptake, assessed by confocal microscopy and flow cytometry, was enhanced by using doxorubicin-loaded CA-PEI-pArg PMs, as compared to free doxorubicin and DOX-loaded CA-PEI PMs. Moreover, 24-h incubation of these PMs with a human breast cancer cell line produced greater cytotoxicity than free doxorubicin. These results indicate that pH-responsive CA-PEI-pArg micelles could provide a versatile delivery system for targeted cancer therapy using hydrophobic drugs
%K Polymeric micelle
%K pH responsive
%K Triblock copolymer
%K Drug delivery
%K Doxorubicin
%K Polyarginine
%U https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5138181/