Polymorph formation in fenofibrate in the absence and presence of polymer stabilizers: a low wavenumber Raman and differential scanning calorimetry study

Ye, Ying; Beck, Christian; Wu, Aide; Davé, Rajesh N.; Iqbal, Zafar

doi:10.1002/jrs.5090

Cited by 4 publications

(4 citation statements)

References 27 publications

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“…Ying et al studied polymorph formation in the anticholesterol drug fenofibrate (FNB) in the absence and presence of polymer stabilizers by low wavenumber Raman and differential scanning calorimetry. Their results were discussed in terms of molecular simulations carried out to determne the nonbonded interaction energies between the polymers and FNB . Zhang, Sha, and Wang used laser perturbation two‐dimensional correlation Raman spectroscopy for assessing quality control of bovine colostrum products.…”

Section: Pharmaceutical Food and Forensic Applicationsmentioning

confidence: 83%

“…Their results were discussed in terms of molecular simulations carried out to determne the nonbonded interaction energies between the polymers and FNB. [199] Zhang, Sha, and Wang used laser perturbation two-dimensional correlation Raman spectroscopy for assessing quality control of bovine colostrum products. Their results showed that the correlation coefficients between each bovine colostrum product with their mean value 0.991 ± 0.003, which indicated that there were high similarities between these products.…”

Section: Liquids Solutions and Liquid Interactionsmentioning

confidence: 99%

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Recent advances in linear and nonlinear Raman spectroscopy. Part XII

Nafie

2018

J Raman Spectroscopy

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This annual review is an overview of advances in the field of Raman spectroscopy as found in papers published in the previous calendar year in the Journal of Raman Spectroscopy (JRS), as well as in trends over the past decade across journals that have published papers important to the field of Raman spectroscopy. This information is gleaned from statistical data on article counts obtained from the Clarivate Analytic's Web of Science Core Collection by year and by subfield of Raman spectroscopy. Additional information is gleaned from presentations at the XXVI International Conference on Raman Spectroscopy (ICORS 2018) in Jeju Island, Korea in August 2018, and contributions on Raman scattering at SCIX 2018, organized by the Federation of Analytical Chemistry and Spectroscopy Societies (FACSS) in Atlanta, Georgia, USA in October 2018. Coverage is also provided for topics from the European Conference on Nonlinear Optical Spetroscopy (ECONOS 2018) held in April in Milan, Italy and GeoRaman 2018 in Catania, Italy in June. Finally, papers published in JRS in 2017 are highlighted and arranged by topics at the frontier of Raman spectroscopy. On the basis of this survey information, it is clear that Raman spectroscopy continues as in recent years as a rapidly expanding field of research across a wide range of novel disciplines and applications that provide sensitive photonic information of matter at the molecular level.

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Section: Pharmaceutical Food and Forensic Applicationsmentioning

confidence: 83%

Section: Liquids Solutions and Liquid Interactionsmentioning

confidence: 99%

Recent advances in linear and nonlinear Raman spectroscopy. Part XII

Nafie

2018

J Raman Spectroscopy

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“…The Raman spectrum also supports that the fenofibrate nanocrystals are form I polymorph (Figure 3c and Figure S11b, Supporting Information). [ 41,42 ] DSC analyses not only suggest the presence of fenofibrate nanocrystals with a single endothermic peak of melting (Figure 3d) but also show a high degree of crystallinity (≈100% in Figure 3e) approximated with the prior knowledge of decreasing fusion enthalpy for lower melting points [ 34,43 ] (Section S11, Supporting Information). The Gibbs–Thomson equation predicts that melting point depression becomes more significant for smaller nanocrystals.…”

Section: Resultsmentioning

confidence: 99%

Design and Use of a Thermogelling Methylcellulose Nanoemulsion to Formulate Nanocrystalline Oral Dosage Forms

Chen

Doyle

2021

Advanced Materials

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However, conventional oral drug formulations typically require costly multistep manufacturing, and poor bioavailability of hydrophobic APIs still remains a persistent challenge in many formulations. It has been reported that 40% of marketed drugs and 90% of drug candidates in the pipeline are hydrophobic. [4] Their poor water-solubility renders the drugs difficult to be absorbed in the gastrointestinal tract, greatly undermining their potency. Over the past decade, many attempts have been made to develop methods for producing API nanocrystals that possess improved solubility and bioavailability because of their significantly larger specific surface area compared to their bulk counterparts. [5][6][7] However, incorporation of the methods into conventional formulation processes is susceptible to many problems. For example, suitable excipients have to be investigated through tedious trial-anderror experiments, [8][9][10] and API inhomogeneity raises a potential risk that causes overdosed or ineffective treatment. [11] Methylcellulose (MC) and hydroxypropyl methylcellulose (HPMC) are two types of natural-based cellulose ester excipients that have been widely formulated into oral solid dosage forms in food and pharmaceutical applications. [12][13][14] Their unique swelling and erosion behaviors are suitable for the design of controlled release systems and for the study of drug delivery models. [15] Upon contact with water, a gel layer can form on the polymer surface due to rapid hydration, which slows down further water penetration into the inner dry polymer core. [16] In addition, fast release can be easily achieved with the use of MC which shows a much faster matrix erosion than HPMC. [14] Despite these ideal properties, formulations of these cellulose esters and hydrophobic APIs into drug products still lack efficient control over API nanocrystal sizes and heavily depend on multiple blending, sieving, and granulation steps. [17,18] Reversible thermal gelation is another "smart" property of MC and HPMC that has gained considerable attention in the field of rheology [19,20] and tissue engineering. [21,22] The polymer gels upon heating and returns back to the sol state upon subsequent cooling. [20] Although researchers have applied this property to develop in situ gelling materials for drug delivery, [23,24] the utility of the thermal gelation property Oral drug products have become indispensable in modern medicine because of their exceptional patient compliance. However, poor bioavailability of ubiquitous low-water-soluble active pharmaceutical ingredients (APIs) and lack of efficient oral drug formulations remain as significant challenges. Nanocrystalline formulations are an attractive route to increase API solubility, but typically require abrasive mechanical milling and several processing steps to create an oral dosage form. Using the dual amphiphilic and thermoresponsive properties of methylcellulose (MC), a new thermogelling nanoemulsion and a facile thermal dripping method are developed for efficient formulatio...

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“…[101,102] Molecular simulations have shown that MC and HPMC have a strongly favorable energetic interaction with surfaces of hydrophobic APIs, including FEN, through hydrogen bonding. [103][104][105][106] Controlling intermolecular interactions during crystallization within hydrogel scaffolds could present an opportunity for polymorphic control, a long-desired goal of drug substance manufacturing. [107]…”

Section: Delayed Pulsatile Drug Release Can Be Programmed From Formul...mentioning

confidence: 99%

Orthogonal Gelations to Synthesize Core–Shell Hydrogels Loaded with Nanoemulsion‐Templated Drug Nanoparticles for Versatile Oral Drug Delivery

Attia

Chen

Doyle

2023

Adv Healthcare Materials

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Hydrophobic active pharmaceutical ingredients are ubiquitous in the drug development pipeline, but their poor bioavailability often prevents their translation into drug products. Industrial processes to formulate hydrophobic APIs are expensive, difficult to optimize, and not flexible enough to incorporate customizable drug release profiles into drug products. Here, a novel, dual‐responsive gelation process that exploits orthogonal thermo‐responsive and ion‐responsive gelations is introduced. This one‐step “dual gelation” synthesizes core‐shell (methylcellulose‐alginate) hydrogel particles and encapsulates drug‐laden nanoemulsions in the hydrogel matrices. In situ crystallization templates drug nanocrystals inside the polymeric core, while a kinetically stable amorphous solid dispersion is templated in the shell. Drug release is explored as a function of particle geometry, and programmable release is demonstrated for various therapeutic applications including delayed pulsatile release and sequential release of a model fixed‐dose combination drug product of ibuprofen and fenofibrate. Independent control over drug loading between the shell and the core is demonstrated. This formulation approach is shown to be a flexible process to develop drug products with biocompatible materials, facile synthesis, and precise drug release performance. This work suggests and applies a novel method to leverage orthogonal gel chemistries to generate functional core‐shell hydrogel particles.This article is protected by copyright. All rights reserved

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Polymorph formation in fenofibrate in the absence and presence of polymer stabilizers: a low wavenumber Raman and differential scanning calorimetry study

Cited by 4 publications

References 27 publications

Recent advances in linear and nonlinear Raman spectroscopy. Part XII

Recent advances in linear and nonlinear Raman spectroscopy. Part XII

Design and Use of a Thermogelling Methylcellulose Nanoemulsion to Formulate Nanocrystalline Oral Dosage Forms

Orthogonal Gelations to Synthesize Core–Shell Hydrogels Loaded with Nanoemulsion‐Templated Drug Nanoparticles for Versatile Oral Drug Delivery

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