Synthesis and in vitro evaluation of pH-sensitive PEG-I-dC16 block polymer micelles for anticancer drug delivery
Abstract
OBJECTIVES: To develop an acid trigger release of antitumour drug delivery carriers, pH-sensitive amphiphilic poly (ethyleneglycol)-imine-benzoic-dipalmitate (PEG-I-dC16 ) polymers were designed and synthesized and the drug-loaded micelles were evaluated in vitro. METHODS: PEG-I-dC16 synthesized by Schiff base synthetic method and characterized by (1) H-NMR. To determine the drug-loading capacity, doxorubicin (DOX) was encapsulated in the micelles using membrane dialysis method. Zeta potential, particle size, drug-loading capacity, in vitro drug release in different pH conditions and cytotoxicity evaluation of micelles were carried out comparing with non-acid liable PEG-amide-benzoic-dipalmitate (PEG-A-dC16) polymers micelles. The cellular uptake and intracellular distribution of DOX were detected by flow cytometry and confocal laser scanning microscope. KEY FINDINGS: Drug-loading capacity and encapsulation efficiency of micelle (PEG molecular weight 2k) were 12.7 ± 1.1% and 49.8 ± 2.2%, respectively. The average particle size was 72.3 ± 2.5 nm. The DOX release rate of PEG-I-dC16 micelles is much higher at pH 6.5 than at pH 7.4. DOX cellular uptake and nuclear accumulation of PEG-I-dC16 micelles were more efficiency than that of PEG-A-dC16 micelles. CONCLUSION: The pH-sensitive PEG-I-dC16 micelles could be a promising drug delivery system for anticancer drugs.
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By comparison with the PEG-A-dC16 micelles bonded by nonacid sensitive amide bonds, the rapid release of DOX from the PEG-I-dC16 micelles was accelerated by changing the pH from 7.4 to 6.5.
“Acid-sensitive Schiff base groups have been utilized to link PEG and double-stranded C16 chains to prepare the PEG-I-dC16 micelles, by comparison with the PEG-A-dC16 micelles bonded by nonacid sensitive amide bonds, the rapid release of DOX from the PEG-I-dC16 micelles was accelerated by changing the pH from 7.4 to 6.5.”
From Recent Advances in Nanomicelles Delivery Systems. (2020) · cites this paper as [141]
Confocal microscopy displayed that the acid-labile micelles had more accumulation in cellular than nonacid-labile micelles and free DOX, and the cytotoxicity of DOX-loaded acid-labile micelles was greater than that of DOX-loaded nonacid-labile micelles against A549 and HepG2 cancer cells.
“Confocal microscopy technique displayed that the acid-labile micelles had more accumulation in cellular than nonacid-labile micelles and free DOX, and the cytotoxicity of DOX-loaded acid-labile micelles was greater than that of DOX-loaded nonacid-labile micelles against A549 and HepG2 cancer cells.”
From Recent Advances in Nanomicelles Delivery Systems. (2020) · cites this paper as [141]
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Recent Advances in Nanomicelles Delivery Systems.
Tawfik, S. M., Azizov, S., Elmasry, M. R., Sharipov, M., & Lee, Y.-I. (2020) · Nanomaterials · doi:10.3390/nano11010070 · Cited by 156 · see citing works
- Authors
- Rongbin, H., Lei, X., Ying, L., Xiangping, D., Xuan, C., Lanfang, L., Cuiyun, Y., Yanming, C., & Guotao, T.
- Affiliations
- The First People's Hospital of Xiangtan City , Xiangtan,
- University of South China (CN)
- Institute of Pharmacy and Pharmacology, Learning Key Laboratory for Pharmacoproteomics University of South China , Hengyang,
- Mu Dan Jiang You Bo Pharmacertical Co.Ltd , Mudanjiang,
- Corresponding author
- Guotao, Tang
- Venue
- Journal of Pharmacy and Pharmacology
- Publisher
- Oxford University Press (OUP)
- Published
- 2016-06-01
- Volume
- 68
- Issue
- 6
- Pages
- 751-761
- ISSN
- 0022-3573 (ISSN-L)
- 2042-7158
- OpenAlex
- W2327382463
- Cited by
- 11
- References
- 43
- Citations by year
- 2025: 2 · 2021: 1 · 2020: 2 · 2019: 1 · 2018: 1 · 2017: 2 · 2016: 2
- FWCI
- 0.82
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- academic.oup.com/journals/pages/open_access/funder_policies/chorus/standard_publication_model (vor)
- Locations
- Journal of Pharmacy and Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Cooperative Innovation Center for Molecular Target New Drug Study and research foundation of education (13C833)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Physical Sciences › Materials Science › Polymers and Plastics › Dendrimers and Hyperbranched Polymers
- Keywords
- pH-responsive micelles, block copolymer micelles, doxorubicin, acid-triggered drug release, anticancer drug delivery, encapsulation efficiency, cellular uptake, subcellular localization
- MeSH terms
- Antibiotics, Antineoplastic, Benzamides, Cell Survival, Delayed-Action Preparations, Dose-Response Relationship, Drug, Doxorubicin, Drug Carriers, Drug Compounding, Humans, Hydrogen-Ion Concentration, Liver Neoplasms, Lung Neoplasms, Micelles, Particle Size, Polyethylene Glycols, Technology, Pharmaceutical, Hep G2 Cells
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