title: Preparation of Two Types of Polymeric Micelles Based on Poly(β-L-Malic Acid) for Antitumor Drug Delivery.
abstract: Polymeric micelles represent an effective delivery system for poorly water-soluble anticancer drugs. In this work, two types of CPT-conjugated polymers were synthesized based on poly(β-L-malic acid) (PMLA) derivatives. Folic acid (FA) was introduced into the polymers as tumor targeting group. The micellization behaviors of these polymers and antitumor activity of different self-assembled micelles were investigated. Results indicate that poly(ethylene glycol)-poly(β-L-malic acid)-campotothecin-I (PEG-PMLA-CPT-I, P1) is a grafted copolymer, and could form star micelles in aqueous solution with a diameter of about 97 nm, also that PEG-PMLA-CPT-II (P2) is an amphiphilic block copolymer, and could form crew cut micelles with a diameter of about 76 nm. Both P1 and P2 micelles could improve the cellular uptake of CPT, especially the FA-modified micelles, while P2 micelles showed higher stability, higher drug loading efficiency, smaller size, and slower drug release rate than that of P1 micelles. These results suggested that the P2 (crew cut) micelles possess better stability than that of the P1 (star) micelles and might be a potential drug delivery system for cancer therapy.
authors.affiliation: Department of Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, China.
authors.forename: Tiehong
authors.initials: T
authors.lastname: Yang
authors.affiliation: Department of Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Li
authors.affiliation: Department of Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Duan
authors.affiliation: Department of Pharmaceutical Sciences, Irma Lerma Rangel College of Pharmacy, Texas A&M University Health Science Center, Kingsville, Texas, 78363, United States.
authors.forename: Lin
authors.initials: L
authors.lastname: Zhu
authors.affiliation: Department of Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, China.
authors.forename: Li
authors.initials: L
authors.lastname: Fan
authors.affiliation: Department of Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, China.
authors.forename: Youbei
authors.initials: Y
authors.lastname: Qiao
authors.affiliation: Department of Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, China.
authors.forename: Hong
authors.initials: H
authors.lastname: Wu
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D002166:Camptothecin / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D004339:Drug Compounding / Q000379:methods*; D016503:Drug Delivery Systems / Q000379:methods*; D065546:Drug Liberation; D005492:Folic Acid / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D008293:Malates / Q000737:chemistry*; D008823:Micelles; D018613:Microscopy, Confocal; D046529:Microscopy, Electron, Transmission; D011092:Polyethylene Glycols / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D008293:Malates; D008823:Micelles; D011108:Polymers; C121060:poly(malic acid); D011092:Polyethylene Glycols; D005492:Folic Acid; D002166:Camptothecin