title: Characteristic of core materials in polymeric micelles effect on their micellar properties studied by experimental and dpd simulation methods.
abstract: Polymeric micelles are one important class of nanoparticles for anticancer drug delivery, but the impact of hydrophobic segments on drug encapsulation and release is unclear, which deters the rationalization of drug encapsulation into polymeric micelles. This paper focused on studying the correlation between the characteristics of hydrophobic segments and encapsulation of structurally different drugs (DOX and β-carotene). Poly(ϵ-caprolactone) (PCL) or poly(l-lactide) (PLLA) were used as hydrophobic segments to synthesize micelle-forming amphiphilic block copolymers with the hydrophilic methoxy-poly(ethylene glycol) (mPEG). Both blank and drug loaded micelles were spherical in shape with sizes lower than 50 nm. PCL-based micelles exhibited higher drug loading capacity than their PLLA-based counterparts. Higher encapsulation efficiency of β-carotene was achieved compared with DOX. In addition, both doxorubicin and β-carotene were released much faster from PCL-based polymeric micelles. Dissipative particle dynamics (DPD) simulation revealed that the two drugs tended to aggregate in the core of the PCL-based micelles but disperse in the core of PLLA based micelles. In vitro cytotoxicity investigation of DOX loaded micelles demonstrated that a faster drug release warranted a more efficient cancer-killing effect. This research could serve as a guideline for the rational design of polymeric micelles for drug delivery.
authors.affiliation: College of Polymer Science and Engineering, Sichuan University, Chengdu 610065, China; National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China.
authors.forename: Furong
authors.initials: F
authors.lastname: Cheng
authors.affiliation: West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
authors.forename: Xuewa
authors.initials: X
authors.lastname: Guan
authors.affiliation: Institute of Biomedical and Pharmaceutical Technology, Fuzhou University, Fuzhou 350116, China.
authors.forename: Huan
authors.initials: H
authors.lastname: Cao
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China.
authors.forename: Ting
authors.initials: T
authors.lastname: Su
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China. Electronic address: caojun@scu.edu.cn.
authors.forename: Jun
authors.initials: J
authors.lastname: Cao
authors.affiliation: College of Polymer Science and Engineering, Sichuan University, Chengdu 610065, China.
authors.forename: Yuanwei
authors.initials: Y
authors.lastname: Chen
authors.affiliation: College of Polymer Science and Engineering, Sichuan University, Chengdu 610065, China.
authors.forename: Mengtan
authors.initials: M
authors.lastname: Cai
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China.
authors.forename: Bin
authors.initials: B
authors.lastname: He
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China.
authors.forename: Zhongwei
authors.initials: Z
authors.lastname: Gu
authors.affiliation: College of Polymer Science and Engineering, Sichuan University, Chengdu 610065, China. Electronic address: luoxl@scu.edu.cn.
authors.forename: Xianglin
authors.initials: X
authors.lastname: Luo
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004317:Doxorubicin / Q000008:administration & dosage / Q000737:chemistry*; D065546:Drug Liberation; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D051379:Mice; D008823:Micelles; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D019207:beta Carotene / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D008823:Micelles; D011091:Polyesters; D019207:beta Carotene; C016240:polycaprolactone; D011092:Polyethylene Glycols; C033616:poly(lactide); D004317:Doxorubicin; C028210:monomethoxypolyethylene glycol
keywords: Chain characteristic; Dissipative particle dynamics simulation; Drug delivery; Encapsulation; Polymeric micelles