Affiliation of Author(s):[1]Sichuan Univ, West China Hosp, Collaborat Innovat Ctr Biotherapy, State Key Lab Biotherapy, Chengdu 610041, Peoples R China;[2]Hosp Univ Elect Sci & Technol China, Dept Pharm, Chengdu 610072, Peoples R China;[3]Sichuan Prov Peoples Hosp, Chengdu 610072, Peoples R China
Journal:JOURNAL OF DRUG TARGETING
Key Words:(Asp)7-CHOL-modified liposome; hydroxyapatite; (Asp)7-CHOL; bone targeting; drug delivery system
Abstract:Specific delivery of drugs to bone tissue is very challenging due to the architecture and structure of bone tissue. A seven-repeat sequence of aspartate, a representative bone-targeting oligopeptide, is preferentially used for targeted therapy for bone diseases. In this study, Asp7-cholesterol((Asp)7-CHOL) was synthesized and (Asp)7-CHOL-modified liposome loaded with doxorubicin (DOX) was successfully prepared using both pre-insertion (pre-L) and post-insertion (post-L) methods. The formulation was optimized according to particle size, zeta potential and the drug-loading efficiency of the liposome. In addition, the bone affinity of the (Asp)7-CHOL-modified liposome was evaluated using a hydroxyapatite (HA) absorption method. The results suggested that (Asp)7-CHOL-modified liposome show excellent HA absorption; pre-L showed slightly higher HA binding than post-L. However, post-L had a higher DOX entrapment efficiency than pre-L. In vivo imaging further demonstrated that pre-L showed a higher bone-targeting efficiency than post-L, which was consistent with in vitro results. In all, (Asp)7-CHOL-modified liposome showed excellent bone-targeting activity, suggesting their potential for use as a drug delivery system for bone disease-targeted therapies.
Document Type:Article
Volume:25
Issue:2
Page Number:149-155
ISSN No.:1061-186X
Translation or Not:no