title: Multi-functional envelope-type nanoparticles assembled from amphiphilic peptidic prodrug with improved anti-tumor activity.
abstract: A novel multifunctional amphiphilic peptidic prodrug was reported here by conjugating the antitumor drug of doxorubicin (DOX) to the hydrophobic tail of a designed peptide-amphiphile (PA), in which the hydrophilic peptide headgroup comprises a glycine-arginine-glycine-aspartic acid-serine (GRGDS) sequence and octaarginine (R8) sequence. Because of the amphiphilic nature, this peptidic prodrug can spontaneously self-assemble into spherical multifunctional envelop-type nanoparticles (MENPs) with the functional peptide sequences gathered on surface. By means of the multifunctions of RGD-mediated tumor targeting, R8-mediated membrane penetration and intracellular protease-mediated hydrolyzing peptide bonds, the MENPs could targeted deliver doxorubicin (DOX) to tumor cells, showing improved antitumor activity both in vitro and in vivo with much reduced side effects.
authors.affiliation: Key Laboratory of Biomedical Polymers of Ministry of Education, Department of Chemistry, Wuhan University , Wuhan 430072, P. R. China.
authors.forename: Jing-Xiao
authors.initials: JX
authors.lastname: Chen
authors.forename: Xiao-Ding
authors.initials: XD
authors.lastname: Xu
authors.forename: Wei-Hai
authors.initials: WH
authors.lastname: Chen
authors.forename: Xian-Zheng
authors.initials: XZ
authors.lastname: Zhang
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D053758:Nanoparticles; D010455:Peptides / Q000737:chemistry* / Q000494:pharmacology; D011355:Prodrugs / Q000737:chemistry* / Q000494:pharmacology; D013499:Surface Properties
chemical_list: D000970:Antineoplastic Agents; D010455:Peptides; D011355:Prodrugs