Cited by 36Photodynamic Therapy Research StudiesNanoplatforms for cancer theranosticsNanoparticle-Based Drug Delivery

A pH-sensitive micelle composed of heparin, phospholipids, and histidine as the carrier of photosensitizers: Application to enhance photodynamic therapy of cancer

Debele, Tilahun Ayane, Mekuria, Shewaye Lakew, Tsai, Hsieh-Chih·2017·International Journal of Biological Macromolecules

Abstract

In this study, we describe the synthesis of a stable, pH-sensitive micelle composed of heparin, 1, 2-distearoyl-sn-glycerol-3-phosphoethanolamine, and l-histidine (HDH) through 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC)/N-hydroxysuccinimide (NHS) chemistry. 1 H-Nuclear magnetic resonance (NMR) and Fourier transform infrared spectroscopy (FTIR) analyses confirmed the formation of HDH copolymers and dynamic light scattering (DLS) measurements indicated a particle size of 111.57±12.36nm and zeta potential of -59.8±5.2mV for the nanoparticles. The drug-loading and encapsulation efficiency of the micelles were 14.52±1.2% and 65.47±1.87%, respectively. Drug release studies showed approximately 91% zinc phthalocyanine (ZnPc) release from micelles in acidic conditions (pH 5.0) in comparison with 63% in physiological conditions (pH 7.4) after 96h of incubation. Singlet oxygen (1 O 2) detection revealed that the micelles prevented ZnPc aggregation and enhanced 1 O 2 generation. Cellular uptake of ZnPc-loaded micelles (ZnPc-HDH) was observed using confocal microscopy. Phototoxicity experiments in HeLa cells showed that ZnPc-loaded micelles had higher toxicity than that shown by the same concentration of free ZnPc. Hence, pH-sensitive HDH micelles are a promising carrier for hydrophobic ZnPc and improving PDT efficacy.

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Crossref · 10.1016/j.ijbiomac.2017.01.103

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  • At pH 5.0 and pH 6.0 about 91% and 63% of zinc phthalocyanine drugs were released after 96 h from HDH-based micelles.

    “Remarkably, at pH 5.0 and pH 6.0 about 91% and 63% of zinc phthalocyanine drugs were released after 96 h.”

    From Recent Advances in Nanomicelles Delivery Systems. (2020) · cites this paper as [164]

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Authors
Debele, T. A., Mekuria, S. L., & Tsai, H.-C.
Affiliations
National Taiwan University of Science and Technology (TW)
Corresponding author
Tsai, Hsieh-Chih
Venue
International Journal of Biological Macromolecules
Publisher
Elsevier BV
Published
2017-05
Volume
98
Pages
125-138
ISSN
0141-8130 (ISSN-L)
OpenAlex
W2582247865
Cited by
36
References
73
Citations by year
2025: 3 · 2024: 1 · 2023: 1 · 2022: 8 · 2021: 1 · 2020: 4 · 2019: 6 · 2018: 8 · 2017: 4
FWCI
4.98
Type
journal article
Language
en
Open access
closed
Locations
  • International Journal of Biological Macromolecules (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • Ministry of Science and Technology (103-2221-E-011-035)
  • National Taiwan University of Science and Technology (102H451201)
Topics
  • Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Photodynamic Therapy Research Studies
  • Physical Sciences › Engineering › Biomedical Engineering › Nanoplatforms for cancer theranostics
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Keywords
pH-responsive micelles, heparin, phospholipids, histidine, photosensitizers, zinc phthalocyanine, photodynamic therapy, drug carriers, singlet oxygen generation, drug release, HeLa cells, cancer therapy
MeSH terms
Animals, Biological Transport, Drug Carriers, HeLa Cells, Heparin, Histidine, Humans, Hydrogen-Ion Concentration, Indoles, Micelles, Organometallic Compounds, Phospholipids, Photochemotherapy, Swine, Photosensitizing Agents, Zinc Compounds, Singlet Oxygen, Isoindoles, Drug Liberation

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