title: In vitro evaluation of polymeric micelles based on hydrophobically-modified sulfated chitosan as a carrier of doxorubicin.
abstract: Four types of doxorubicin (DOX)-loaded polymeric micelles based on hydrophobically-modified sulfated chitosan (SCTS) were prepared. The hydrophobic group was composed of glycyrrhetinic acid (GA), cholic acid, stearic acid (SA) or lauric aldehyde. DOX encapsulation depended on several parameters, including the degree of substitution of the sulfate group and the hydrophobic group, and the type of hydrophobic group. Of these micelles, GA-SCTS micelles had the best capability to solubilize DOX. In addition, GA-SCTS micelles had the ability to target HepG(2) cells, and the IC50 for DOX-loaded GA-SCTS micelles was 54.7 ng/mL, which was much lower than that of the other micelles. Further studies on the DOX-loaded GA-SCTS micelles showed that they were stable in salt and protein solutions, in cell culture media, and during long-term storage (6 months). Based on these results, these micelles may be a promising DOX-encapsulated formulation, particularly, GA-SCTS as a potential vehicle for liver-targeted delivery.
authors.affiliation: Key Laboratory of Functional Polymer Materials, Ministry of Education, Institute of Polymer Chemistry, Nankai University, Tianjin, 300071, People's Republic of China.
authors.forename: Xiu-Hua
authors.initials: XH
authors.lastname: Wang
authors.forename: Qin
authors.initials: Q
authors.lastname: Tian
authors.forename: Wei
authors.initials: W
authors.lastname: Wang
authors.forename: Chuang-Nian
authors.initials: CN
authors.lastname: Zhang
authors.forename: Ping
authors.initials: P
authors.lastname: Wang
authors.forename: Zhi
authors.initials: Z
authors.lastname: Yuan
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage*; D002460:Cell Line; D048271:Chitosan / Q000737:chemistry*; D004317:Doxorubicin / Q000008:administration & dosage*; D004337:Drug Carriers; D006801:Humans; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008823:Micelles; D010316:Particle Size; D011108:Polymers; D013431:Sulfates / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; D011108:Polymers; D013431:Sulfates; D004317:Doxorubicin; D048271:Chitosan