Next Article in Journal
Drug Delivery Technology to the CNS in the Treatment of Brain Tumors: The Sherbrooke Experience
Next Article in Special Issue
Hyaluronic Acid-Coated Nanomedicine for Targeted Cancer Therapy
Previous Article in Journal / Special Issue
Hyaluronic Acid Nanocapsules as a Platform for Needle-Free Vaccination
Open AccessArticle

pH-Responsive i-motif Conjugated Hyaluronic Acid/Polyethylenimine Complexes for Drug Delivery Systems

by Gyeong Jin Lee 1 and Tae-il Kim 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.
Pharmaceutics 2019, 11(5), 247; https://doi.org/10.3390/pharmaceutics11050247
Received: 1 May 2019 / Revised: 21 May 2019 / Accepted: 24 May 2019 / Published: 27 May 2019
(This article belongs to the Special Issue Hyaluronic Acid for Biomedical Applications)
i-motif is cytosine (C)-rich oligonucleotide (ODN) which shows pH-responsive structure change in acidic condition. Therefore, it has been utilized for the trigger of intercalated drug release, responding to environmental pH change. In this study, 2.76 molecules of i-motif binding ODNs (IBOs) were conjugated to each hyaluronic acid (HA) via amide bond linkages. Synthesis of HA-IBO conjugate (HB) was confirmed by FT-IR and agarose gel electrophoresis with Stains-All staining. After hybridization of HB with i-motif ODN (IMO), it was confirmed that doxorubicin (DOX) could be loaded in HB-IMO hybrid structure (HBIM) with 65.6% of drug loading efficiency (DLE) and 25.0% of drug loading content (DLC). At pH 5.5, prompt and significant DOX release from HBIM was observed due to the disruption of HBIM hybrid structure via i-motif formation of IMO, contrary to pH 7.4 condition. Then, HBIM was complexed with low molecular weight polyethylenimine (PEI1.8k), forming positively charged nanostructures (Z-average size: 126.0 ± 0.4 nm, zeta-potential: 16.1 ± 0.3 mV). DOX-loaded HBIM/PEI complexes displayed higher anticancer efficacy than free DOX in A549 cells, showing the potential for pH-responsive anticancer drug delivery systems. View Full-Text
Keywords: hyaluronic acid; i-motif; pH-responsive; polyethylenimine; nanostructure; drug delivery systems hyaluronic acid; i-motif; pH-responsive; polyethylenimine; nanostructure; drug delivery systems
Show Figures

Graphical abstract

MDPI and ACS Style

Lee, G.J.; Kim, T.-I. pH-Responsive i-motif Conjugated Hyaluronic Acid/Polyethylenimine Complexes for Drug Delivery Systems. Pharmaceutics 2019, 11, 247.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop