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Anti‐solvent crystallization for the preparation of drug nanocrystals via amphiphilic copolymer (AcMH‐b‐PEG) micelles as soft templates.

Title: Anti‐solvent crystallization for the preparation of drug nanocrystals via amphiphilic copolymer (AcMH‐b‐PEG) micelles as soft templates.
Authors: Wang, Yini; Lou, Boxuan; Xu, Yue; Yuan, Haikuan; Lu, Jie
Source: Canadian Journal of Chemical Engineering; Jul2026, Vol. 104 Issue 7, p3840-3857, 18p
Subject Terms: Copolymer micelles; Crystallization; Block copolymers; Medical polymers; Nanomedicine; Nanocrystals; Controlled release drugs; Isoflavonoids
Abstract: Nanometerization of drug particles as a well‐regarded approach can enhance the solubility and bioavailability of water‐insoluble drugs. (R)‐Equol is frequently employed in research for its ability to inhibit the replication of cancer cells, but the application of (R)‐equol is still limited by its water‐insoluble nature. Novel biocompatible polymeric micelles were prepared through the self‐assembly of amphiphilic block copolymers composed of acetylated maltoheptose‐b‐polyethylene glycol (AcMH‐b‐PEG) in water. Using AcMH‐b‐PEG micelles as templates, (R)‐equol nanocrystals with good crystallinity and regular morphology were prepared by a micelle‐mediated anti‐solvent crystallization method. These nanocrystals were identified as an isolated‐site hydrate form of (R)‐equol, stabilized by a robust three‐dimensional hydrogen‐bonding network and distinct from those obtained via conventional methods. In vitro release experiment showed that AcMH‐b‐PEG micelle exhibited a sustained‐release effect on (R)‐equol, with the drug being released slowly and continuously. In mouse plasma, the cumulative release reached 65.70% over 24 h. In particular, it was found that (R)‐equol was more readily released under acidic milieus. This study demonstrated that using amphiphilic micelles as templates for anti‐solvent crystallization represented a potent and robust approach to prepare crystalline nanodrugs. [ABSTRACT FROM AUTHOR]
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Database: Complementary Index