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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 beta-carotene). Poly(epsilon-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 b-carotene was achieved compared with DOX. In addition, both doxorubicin and b-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. (C) 2015 Elsevier B.V. All rights reserved.
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
ISSN: 0378-5173
Year: 2015
Issue: 1-2
Volume: 492
Page: 152-160
3 . 9 9 4
JCR@2015
5 . 3 0 0
JCR@2023
ESI Discipline: PHARMACOLOGY & TOXICOLOGY;
ESI HC Threshold:193
JCR Journal Grade:1
CAS Journal Grade:2
Cited Count:
WoS CC Cited Count: 30
SCOPUS Cited Count: 31
ESI Highly Cited Papers on the List: 0 Unfold All
WanFang Cited Count:
Chinese Cited Count:
30 Days PV: 2
Affiliated Colleges: