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A Novel One-Step Drug-Loading Procedure for Water-Soluble Amphiphilic Nanocarriers
Abstract
Purpose The lack of water-solubility hampers the use of many potent pharmaceuticals. Polymeric micelles are self-assembled nanocarriers with versatile properties that can be engineered to solubilize, target, and release hydrophobic drugs in a controlled-release fashion. Unfortunately, their large-scale use is limited by the incorporation methods available, especially when sterile dosage forms are sought. Methods In this manuscript, we describe a straightforward, economical, and innovative drug-loading procedure that consists in dissolving both the drug and an amphiphilic diblock copolymer in a water/tert-butanol mixture that is subsequently freeze-dried. Results We demonstrate that monodisperse 20-60 nm-sized drug-loaded polymeric micelles are produced directly and spontaneously upon rehydration of the freeze-dried cake. To establish the proof-of-principle, two hydrophobic taxane derivatives were solubilized in the micelles, and their partition coefficient was determined. Conclusions This approach is efficient yet astonishingly simple and may be of great interest for scientists working in nanotechnology and pharmaceutical sciences.
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In one study, a tert-butanol solution of drug added to an aqueous PVP-b-PDLLA polymer solution and then freeze-dried formed stable micelles upon resuspension in aqueous media.
“In one study, a tert-butanol solution of drug was added to an aqueous solution of a polymer (PVP-b-PDLLA), and then the mixture was freeze dried to form stable micelles upon resuspension in aqueous media [280, 281].”
From Polymeric micelles for the delivery of poorly soluble drugs: From nanoformulation to clinical approval. (2020) · cites this paper as [281]
Freeze drying under particular conditions can remove small amounts of residual organic solvents, and freeze drying alone has been used to prepare stable micelle formulations.
“Freeze drying, when done under particular conditions, can be used to remove small amounts of residual organic solvents. Moreover, freeze drying alone has been used to prepare stable micelle formulations.”
From Polymeric micelles for the delivery of poorly soluble drugs: From nanoformulation to clinical approval. (2020) · cites this paper as [281]
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“In one study, a tert-butanol solution of drug was added to an aqueous solution of a polymer (PVP-b-PDLLA), and then the mixture was freeze dried to form stable micelles upon resuspension in aqueous media [280,281].”
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“It is worth noting that all these techniques require sterilization and lyophilization processes; the freeze-dried mixture can be reconstituted to obtain drug-loaded micelles [103].”
Metadata
- Authors
- Fournier, E., Dufresne, M.-H., Smith, D. C., Ranger, M., & Leroux, J.-C.
- Affiliations
- Université de Montréal (CA)
- Labopharm Inc. (Canada) (CA)
- Corresponding author
- Leroux, Jean-Christophe
- Venue
- Pharmaceutical Research
- Published
- 2004-06
- Volume
- 21
- Issue
- 6
- Pages
- 962-968
- ISSN
- 0724-8741 (ISSN-L)
- 1573-904X
- OpenAlex
- W1986186085
- Cited by
- 111
- References
- 37
- Citations by year
- 2025: 5 · 2024: 4 · 2023: 5 · 2022: 7 · 2021: 4 · 2020: 5 · 2019: 6 · 2018: 7 · 2017: 4 · 2016: 4 · 2015: 9 · 2014: 3 · 2013: 3 · 2012: 7
- FWCI
- 3.46
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- Locations
- Pharmaceutical Research (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Canada Research Chairs
- Natural Sciences and Engineering Research Council of Canada
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Physical Sciences › Chemistry › Physical and Theoretical Chemistry › Surfactants and Colloidal Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Keywords
- polymeric micelles, drug loading, amphiphilic diblock copolymers, hydrophobic drug solubilization, freeze-drying, taxane derivatives, partition coefficient, controlled drug release
- MeSH terms
- Butanols, Bridged-Ring Compounds, Chemistry, Physical, Crystallization, Dehydration, Delayed-Action Preparations, Drug Carriers, Drug Compounding, Freeze Drying, Micelles, Particle Size, Polymers, Solubility, Technology, Pharmaceutical, Water, Drug Delivery Systems, Nanotechnology, Taxoids
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