Development of TPGS/F127/F68 mixed polymeric micelles: Enhanced oral bioavailability and hepatoprotection of syringic acid against carbon tetrachloride-induced hepatotoxicity

The purpose of this study was to develop mixed polymeric micelles with high drug loading capacity to improve the oral bioavailability of icaritin with Soluplus® and Poloxamer 407 using a creative acid-base shift (ABS) method, which exhibits the advantages of exclusion of organic solvents, high drug loading and ease of scaling-up. The feasibility of the ABS method was successfully demonstrated by studies of icaritin-loaded polymeric micelles (IPMs). The prepared IPMs were characterized to have a spherical shape with a size of 72.74 ± 0.51 nm, and 13.18% drug loading content. In vitro release tests confirmed the faster release of icaritin from IPMs compared to an oil suspension. Furthermore, bioavailability of icaritin in IPMs in beagle dogs displayed a 14.9-fold increase when compared with the oil suspension. Transcellular transport studies of IPMs across Caco-2 cell monolayers confirmed that the IPMs were endocytosed in their intact forms through macropinocytosis, clathrin-, and caveolae-mediated pathways. In conclusion, the results suggested that the mixed micelles of Soluplus® and Poloxamer 407 could be a feasible drug delivery system to enhance oral bioavailability of icaritin, and the ABS method might be a promising technology for the preparation of polymeric micelles to encapsulate poorly water-soluble weakly acidic and alkaline drugs.

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Enhanced oral bioavailability of paclitaxel in pluronic/LHR mixed polymeric micelles: Preparation, in vitro and in vivo evaluation

European Journal of Pharmaceutical Sciences ◽

10.1016/j.ejps.2012.05.015 ◽

2012 ◽

Vol 47 (1) ◽

pp. 179-189 ◽

Cited By ~ 78

Author(s):

Fatima Zohra Dahmani ◽

Hui Yang ◽

Jianping Zhou ◽

Jing Yao ◽

Ting Zhang ◽

...

Keyword(s):

Oral Bioavailability ◽

Polymeric Micelles ◽

In Vivo Evaluation ◽

Mixed Polymeric Micelles

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Physical and Pharmacokinetic Characterizations of trans-Resveratrol (t-Rev) Encapsulated with Self-Assembling Lecithin-based Mixed Polymeric Micelles (saLMPMs)

Scientific Reports ◽

10.1038/s41598-017-11320-y ◽

2017 ◽

Vol 7 (1) ◽

Cited By ~ 9

Author(s):

Tzu-Pin Li ◽

Wan-Ping Wong ◽

Ling-Chun Chen ◽

Chia-Yu Su ◽

Lih-Geeng Chen ◽

...

Keyword(s):

Polymeric Micelles ◽

Self Assembling ◽

Mixed Polymeric Micelles

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On the Transition between a Heterogeneous and Homogeneous Corona in Mixed Polymeric Micelles

Langmuir ◽

10.1021/la801816p ◽

2008 ◽

Vol 24 (21) ◽

pp. 12221-12227 ◽

Cited By ~ 18

Author(s):

Ilja K. Voets ◽

Remco Fokkink ◽

Arie de Keizer ◽

Roland P. May ◽

Pieter de Waard ◽

...

Keyword(s):

Polymeric Micelles ◽

Mixed Polymeric Micelles

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Mixed polymeric micelles as a multifunctional visual thermosensor for the rapid analysis of mixed metal ions with Al3+ and Fe3+

New Journal of Chemistry ◽

10.1039/c8nj01917g ◽

2018 ◽

Vol 42 (15) ◽

pp. 12853-12864 ◽

Cited By ~ 3

Author(s):

Juan Han ◽

Yunfeng Cai ◽

Yun Wang ◽

Xiaohui Dai ◽

Lei Wang ◽

...

Keyword(s):

Block Copolymer ◽

Metal Ions ◽

Chain Transfer ◽

Polymeric Micelles ◽

Raft Polymerization ◽

Rapid Analysis ◽

Mixed Metal ◽

Reversible Addition ◽

Mixed Polymeric Micelles

A novel type of responsive mixed double hydrophilic block copolymer (DHBC)-based multifunctional visual thermosensor for the detection of Al3+ and Fe3+ was designed and synthesized based on reversible addition fragmentation chain transfer (RAFT) polymerization.

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