Characteristics, cellular uptake and transepithelial transport of coumarin-6 loaded PEO-(hb-PG)-g-PCL miktoarm copolymer micelles

doi:10.5246/jcps.2013.03.036

Abstract

Abstract:

Recently, advances in synthetic methodologies have provided efficient routes to generate nonlinear amphiphilic polymers. However, the uptake and transport of model-drug loaded novel miktoarm copolymer micelles have not been extensively studied. In this study, a comparison of the characteristics of two types of PEO-(hb-PG)-g-PCL micelles and the uptake of these two micelles loaded with coumarin-6 (C6) on Caco-2 cellular monolayers was carried out for the first time. PEO₁₁₃-(hb-PG)₁₅-g-PCL₂₂micelles (PMs) were then chosen as the vehicle to study the uptake and transport of PMs-C6 across Caco-2 cellular monolayers. In the cellular uptake and transport study, PMs were found to significantly enhance the uptake and transepithelial transport for C6. Mechanism studies further revealed that caveolin-mediated endocytosis pathway, rather than clathrin-mediated pathway, may play an important role in the uptake of PMs-C6. Thus, the novel PEO-(hb-PG)-g-PCL micelles prepared here might have the potential to be used for oral drug delivery due to its advantages in low critical micelle concentration, low cytotoxicity and significant facilitation of the uptake and transport of C6 on Caco-2 cellular monolayers.

Key words: Miktoarm copolymer micelles, Caco-2, Uptake, Endocytosis

CLC Number:

R943

Supporting:

Xiaofei Zhang, Zheng Cui, Xiaojin Zhang, Bing He, Xueqing Wang, Hua Zhang, Zhenlin Zhong, Qiang Zhang^*. Characteristics, cellular uptake and transepithelial transport of coumarin-6 loaded PEO-(hb-PG)-g-PCL miktoarm copolymer micelles[J]. , DOI: 10.5246/jcps.2013.03.036.

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