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Nanomaterials 2019, 9(3), 459; https://doi.org/10.3390/nano9030459

Cholic Acid-Conjugated Methylcellulose-Polyethylenimine Nano-Aggregates for Drug Delivery Systems

1,†, 1,† and 1,2,*
1
Department of Biosystems & Biomaterials Science and Engineering, College of Agriculture and Life Sciences, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 08826, Korea
2
Research Institute of Agriculture and Life Sciences, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 08826, Korea
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Received: 25 February 2019 / Revised: 12 March 2019 / Accepted: 18 March 2019 / Published: 19 March 2019
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Abstract

Cholic acid-conjugated methylcellulose-polyethylenimines (MCPEI-CAs) were synthesized and characterized for drug delivery systems. Their synthesis was confirmed by 1H NMR and FT-IR analysis. Induced circular dichroism result with Congo red showed that methylcellulose (MC) and polyethylenimine-grafted cationic derivative (MC-PEI) would have helical conformation and random coil structure, respectively. It was found that MCPEI-CAs could form positively charged (>30 mV Zeta-potential) and spherical nano-aggregates (~250 nm Z-average size) by hydrophobic interaction of CA moieties. Critical aggregation concentration of MCPEI-CA10 was measured as 7.2 × 10−3 mg/mL. MCPEI-CA10 could encapsulate the anticancer drug doxorubicin (Dox) with 58.0% of drug loading content and 23.2% of drug loading efficiency and its release was facilitated in acidic condition. Cytotoxicity of MCPEI-CAs was increased with the increase of cholic acid (CA) graft degrees, probably due to the cellular membrane disruption by interaction with specific molecular structure of amphiphilic MCPEI-CA nano-aggregates. MCPEI-CA10/Dox nano-aggregates showed concentration-dependent anticancer activity, which could overcome the multidrug resistance of cancer cells. In this work, molecular conformation change of MC derivatives by chemical modification and a potential of MCPEI-CA10/Dox nano-aggregates for drug delivery systems were revealed. View Full-Text
Keywords: cholic acid; methylcellulose; polyethylenimine; molecular conformation; nano-aggregates; drug delivery systems cholic acid; methylcellulose; polyethylenimine; molecular conformation; nano-aggregates; drug delivery systems
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Kim, T.; Park, J.; Kim, T.-I. Cholic Acid-Conjugated Methylcellulose-Polyethylenimine Nano-Aggregates for Drug Delivery Systems. Nanomaterials 2019, 9, 459.

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