Preparation of camptothecin-loaded polymeric micelles and evaluation of their incorporation and circulation stability
Abstract
To improve its aqueous solubility and stability in biological fluid, CPT was physically loaded in polymeric micelles. Polymeric micelles were composed of various poly(ethylene glycol)-poly(aspartate ester) block copolymers (PEG-P(Asp(R))). The incorporation and circulation stability of CPT micelles were evaluated by measuring the CPT in micelle using gel-permeation chromatography and by CPT concentration measurement after intravenous injection using HPLC, respectively, in terms of chemical structure of block copolymers. The stability of CPT-loaded micelles in vivo depended on the amount of benzyl esters, and length of PEG in the polymers to a greater degree than it did in vitro. A stable formulation of CPT-loaded micelles was obtained using PEG-P(Asp) with PEG of 5,000 (MW), 27 Asp units, and 57-75% benzyl esterification of Asp residue. This CPT-loaded micelles showed about a 17-fold lower blood clearance value than unstable micelles. The CPT-loaded micelles are potentially delivered to tumor sites owing to an extended circulation in the blood stream.
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Zhang et al. reported that approximately 60% of PEG-PCL micelles in mouse plasma were intact 72 h after intravenous injection, i.e., most micelles remain intact during blood circulation.
“Zhang et al. [237] which reported that approximately 60% of PEG-PCL micelles in mouse plasma were intact 72 h after i.v.injection, i.e. most of micelles remain intact during blood circulation.”
From Polymeric micelles in drug delivery: An insight of the techniques for their characterization and assessment in biorelevant conditions (2021) · cites this paper as [237]
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- Authors
- Watanabe, M., Kawano, K., Yokoyama, M., Opanasopit, P., Okano, T., & Maitani, Y.
- Affiliations
- Hoshi University (JP)
- Kanagawa Academy of Science and Technology (JP)
- Tokyo Women's Medical University (JP)
- Corresponding author
- Maitani, Yoshie
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2006-02
- Volume
- 308
- Issue
- 1-2
- Pages
- 183-189
- ISSN
- 0378-5173 (ISSN-L)
- OpenAlex
- W1995415878
- Cited by
- 128
- References
- 32
- Citations by year
- 2026: 2 · 2025: 1 · 2023: 6 · 2022: 8 · 2021: 4 · 2020: 8 · 2019: 2 · 2018: 5 · 2017: 4 · 2016: 5 · 2015: 4 · 2014: 8 · 2013: 9 · 2012: 7
- FWCI
- 4.08
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- International Journal of Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Keywords
- camptothecin, polymeric micelles, drug loading, blood clearance, tumor targeting, anticancer drug delivery, water solubility
- MeSH terms
- Animals, Antineoplastic Agents, Phytogenic, Aspartic Acid, Biopolymers, Camptothecin, Drug Carriers, Drug Stability, Injections, Intravenous, Male, Micelles, Particle Size, Polyethylene Glycols, Polymers, Solubility, Area Under Curve, Mice
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