Pharmacokinetics and in vivo delivery of curcumin by copolymeric mPEG-PCL micelles
Abstract
Curcumin (CUR) has been associated with anti-inflammatory, antimicrobial, antioxidant, anti-amyloid, and antitumor effects, but its application is limited because of its low aqueous solubility and poor oral bioavailability. To progress the bioavailability and water solubility of CUR, we synthesized five series of mono methoxy poly (ethylene glycol)-poly (ε-caprolactone) (mPEG-PCL) diblock copolymers. The structure of the copolymers was characterized by H NMR, FTIR, DSC and GPC techniques. In this study, CUR was encapsulated within micelles through a single-step nano-precipitation method, leading to formation of CUR-loaded mPEG-PCL (CUR/mPEG-PCL) micelles. The resulting micelles were characterized further by various techniques such as dynamic light scattering (DLS) and atomic force microscopy (AFM). The cytotoxicity of void CUR, mPEG-PCL and CUR/mPEG-PCL micelles was compared to each other by performing MTT assay of the treated MCF-7 and 4T1 cell line. Study of the in vivo pharmacokinetics of the CUR-loaded micelles was also carried out on selected copolymers in comparison with CUR solution formulations. The results showed that the zeta potential of CUR-loaded micelles was about -11.5mV and the average size was 81.0nm. CUR was encapsulated into mPEG-PCL micelles with loading capacity of 20.65±0.015% and entrapment efficiency of 89.32±0.34%. The plasma AUC (0-t), t 1/2 and C max of CUR micelles were increased by 52.8, 4.63 and 7.51-fold compared to the CUR solution, respectively. In vivo results showed that multiple injections of CUR-loaded micelles could prolong the circulation time and increase the therapeutic efficacy of CUR. These results suggested that mPEG-PCL micelles would be a potential carrier for CUR.
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AFM has been indicated as a proper tool for micelles size determination due to its ability to distinguish particles with different dimensions in a mixture as well as to operate at room temperature, thus allowing the analysis of biological samples close to native and physiological conditions.
“AFM has been indicated as a proper tool for micelles size determination due to its ability to distinguish particles with different dimensions in a mixture as well as to operate at room temperature, thus allowing the analysis of biological samples close to native and physiological conditions [133,[154][155][156].”
From Polymeric micelles in drug delivery: An insight of the techniques for their characterization and assessment in biorelevant conditions (2021) · cites this paper as [156]
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- Authors
- Kheiri Manjili, H., Ghasemi, P., Malvandi, H., Mousavi, M. S., Attari, E., & Danafar, H.
- Affiliations
- Zanjan University of Medical Sciences (IR)
- Corresponding author
- Danafar, Hossein
- Venue
- European Journal of Pharmaceutics and Biopharmaceutics
- Publisher
- Elsevier BV
- Published
- 2017-07
- Volume
- 116
- Pages
- 17-30
- ISSN
- 0939-6411 (ISSN-L)
- OpenAlex
- W2532582651
- Cited by
- 108
- References
- 40
- Citations by year
- 2026: 6 · 2025: 11 · 2024: 6 · 2023: 10 · 2022: 10 · 2021: 11 · 2020: 13 · 2019: 13 · 2018: 12 · 2017: 15 · 2016: 1
- FWCI
- 6.67
- Type
- journal article
- Language
- en
- Update notices
- erratum (2019-09-01)
- Open access
- closed
- Locations
- European Journal of Pharmaceutics and Biopharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Faculty of Pharmacy, Zanjan University of Medical Sciences
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Medicine › Curcumin's Biomedical Applications
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Keywords
- curcumin, polymeric micelles, pharmacokinetics, nanoprecipitation, drug delivery, oral bioavailability, water solubility, encapsulation efficiency, MCF-7 cells, 4T1 cells, cytotoxicity, circulation time
- MeSH terms
- Animals, Chemistry, Pharmaceutical, Curcumin, Drug Carriers, Female, Humans, Mice, Inbred BALB C, Micelles, Particle Size, Polyesters, Polyethylene Glycols, Polymers, Solubility, Drug Delivery Systems, Cell Line, Tumor, Mice, MCF-7 Cells
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