On the Polymorphism of Griseofulvin: Identification of Two Additional Polymorphs

Mahieu, Aurélien; willart, Jean-François; Dudognon, Emeline; Eddleston, Mark D.; Jones, William; Danède, Florence; Descamps, Marc

doi:10.1002/jps.23349

Cited by 53 publications

(57 citation statements)

References 23 publications

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“…But the patterns were different to that of the raw-GF. The XRD pattern of the prepared nano-sized samples matched well with the polymorphic form I of GF as reported in the literature (Mahieu et al 2013). GF is reported to have at least three polymorphic forms, namely form I, form II, and form III (Mahieu et al 2013).…”

Section: In Vitro Dissolution Studiessupporting

confidence: 83%

“…The XRD pattern of the prepared nano-sized samples matched well with the polymorphic form I of GF as reported in the literature (Mahieu et al 2013). GF is reported to have at least three polymorphic forms, namely form I, form II, and form III (Mahieu et al 2013). It appears that raw-GF contained a mixture of different polymorphs (Beck et al 2013;Mahieu et al 2013).…”

Section: In Vitro Dissolution Studiessupporting

confidence: 83%

“…GF is reported to have at least three polymorphic forms, namely form I, form II, and form III (Mahieu et al 2013). It appears that raw-GF contained a mixture of different polymorphs (Beck et al 2013;Mahieu et al 2013). As the polymorphic form of the raw-GF was different from that of the nano-sized particles, a direct comparison of crystallinity of the nanoparticles with raw-GF was not attempted.…”

Section: In Vitro Dissolution Studiesmentioning

confidence: 99%

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Controlling the size and morphology of griseofulvin nanoparticles using polymeric stabilizers by evaporation-assisted solvent–antisolvent interaction method

Kumar

Siril

2015

J Nanopart Res

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Griseofulvin (GF) is a potential drug for cancer therapy. However, its application is limited by its poor water solubility. Ultrafine GF nanoparticles were prepared through evaporation-assisted solventantisolvent interaction method for improving its solubility. Acetone was used as the solvent and water was used as the antisolvent. It was observed that particle size could be controlled by varying the concentration of GF in acetone. Average particle size was very low, 16 ± 4 and 28 ± 8 nm, when the concentration of GF was 5 and 25 mM, respectively, in acetone. However, the particle size increased drastically to more than 3 lm, when the concentration was increased to 50 mM. Interestingly, the presence of optimized concentration of polyvinylpyrrolidone (PVP) and hydroxypropyl methylcellulose (HPMC) as stabilizers in the antisolvent resulted in significant reduction of particle size. Particle size decreased to less than 40 nm in the presence of the polymeric stabilizers, even when the concentration was 50 mM.Field emission scanning electron microscopy, transmission electron microscopy, and atomic force microscopy imaging revealed that the polymeric stabilizers encapsulated very small GF particles and thus stabilized them. The solubility of GF-HPMC, GF-PVP, and the bare GF particles that were prepared from 50 mM solution (micro-GF) was nearly 24, 19, and 11 times, respectively, higher than that of raw-GF. In vitro dissolution studies revealed that almost 100 % of the drug was released in 60 min from GF-PVP and GF-HPMC. Fourier transform infrared spectroscopy did not detect any strong interaction between GF and the stabilizers. X-ray diffraction showed that the prepared GF nanoparticles and the micro-GF were in polymorphic form I. Differential scanning calorimetric studies showed that the crystallinity of the nanoformulated GF was only slightly lower than that of raw-GF. Thus, particle size reduction and the presence of stabilizers led to significant enhancement in solubility and dissolution rate.

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Section: In Vitro Dissolution Studiessupporting

confidence: 83%

Section: In Vitro Dissolution Studiessupporting

confidence: 83%

Section: In Vitro Dissolution Studiesmentioning

confidence: 99%

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Controlling the size and morphology of griseofulvin nanoparticles using polymeric stabilizers by evaporation-assisted solvent–antisolvent interaction method

Kumar

Siril

2015

J Nanopart Res

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“…1a) corresponds to the XRPD pattern of crystalline form I reported by Mahieu et al [32]. Quench cooling of griseofulvin resulted in an X-ray amorphous sample as indicated by the XRPD pattern (Fig.…”

Section: Characterisation Of Griseofulvin Tabletsmentioning

confidence: 52%

“…There are three reported crystalline polymorphic forms of griseofulvin: the stable form I and the metastable forms II and III [32]. The amorphous form of griseofulvin can be prepared either by quench cooling or cryomilling [33,34].…”

Section: Introductionmentioning

confidence: 99%

Use of low-frequency Raman spectroscopy and chemometrics for the quantification of crystallinity in amorphous griseofulvin tablets

Mah

Fraser

Reish

et al. 2015

Vibrational Spectroscopy

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Phase Identification and Discovery of an Elusive Polymorph of Drug‐Polymer Inclusion Complex Using Automated 3D Electron Diffraction

Lightowler,

Li,

et al. 2024

Angewandte Chemie

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3D electron diffraction (3D ED) has shown great potential in crystal structure determination in materials, small organic molecules, and macromolecules. In this work, an automated, low‐dose and low‐bias 3D ED protocol has been implemented to identify six phases from a multiple‐phase melt‐crystallisation product of an active pharmaceutical ingredient, griseofulvin (GSF). Batch data collection under low‐dose conditions using a widely available commercial software was combined with automated data analysis to collect and process over 230 datasets in three days. Accurate unit cell paramters obtained from 3D ED data allowed direct phase identification of GSF Forms III, I and the known GSF inclusion complex (IC) with polyethylene glycol (PEG) (GSF‐PEG IC‐I), as well as three minor phases, namely GSF Forms II, V and an elusive new phase, GSF‐PEG IC‐II. Their structures were then directly determined by 3D ED. Furthermore, we reveal how the stabilities of the two GSF‐PEG IC polymorphs are closely related to their crystal structures. These results demonstrate the power of automated 3D ED for accurate phase identification and direct structure determination of complex, beam‐sensitive crystallisation products, which is significant for drug development where solid form screening is crucial for the overall efficacy of the drug product.

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On the Polymorphism of Griseofulvin: Identification of Two Additional Polymorphs

Cited by 53 publications

References 23 publications

Controlling the size and morphology of griseofulvin nanoparticles using polymeric stabilizers by evaporation-assisted solvent–antisolvent interaction method

Controlling the size and morphology of griseofulvin nanoparticles using polymeric stabilizers by evaporation-assisted solvent–antisolvent interaction method

Use of low-frequency Raman spectroscopy and chemometrics for the quantification of crystallinity in amorphous griseofulvin tablets

Phase Identification and Discovery of an Elusive Polymorph of Drug‐Polymer Inclusion Complex Using Automated 3D Electron Diffraction

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