Using X-ray Diffraction Techniques for Biomimetic Drug Development, Formulation, and Polymorphic Characterization

Rodríguez, Israel; Gautam, Ritika; Tinoco, Arthur D.

doi:10.3390/biomimetics6010001

Cited by 26 publications

(11 citation statements)

References 126 publications

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“…It can also incorporate some methods like standard addition, internal standard, and reference internal ratio (RIR), combined with peak and background fitting, integral and Rietveld refinement calculations, to determine the amorphous content in the sample relative to the total crystalline phase content. However, recent uses of synchrotron have allowed wider investigations in the field of amorphous or poorly-crystalline solids [44].…”

Section: Phase Identification and Quantificationmentioning

confidence: 99%

X-ray Diffraction Techniques for Mineral Characterization: A Review for Engineers of the Fundamentals, Applications, and Research Directions

2022

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X-ray diffraction (XRD) is an important and widely used material characterization technique. With the recent development in material science technology and understanding, various new materials are being developed, which requires upgrading the existing analytical techniques such that emerging intricate problems can be solved. Although XRD is a well-established non-destructive technique, it still requires further improvements in its characterization capabilities, especially when dealing with complex mineral structures. The present review conducts comprehensive discussions on atomic crystal structure, XRD principle, its applications, uncertainty during XRD analysis, and required safety precautions. The future research directions, especially the use of artificial intelligence and machine learning tools, for improving the effectiveness and accuracy of the XRD technique, are discussed for mineral characterization. The topics covered include how XRD patterns can be utilized for a thorough understanding of the crystalline structure, size, and orientation, dislocation density, phase identification, quantification, and transformation, information about lattice parameters, residual stress, and strain, and thermal expansion coefficient of materials. All these important discussions on XRD analysis for mineral characterization are compiled in this comprehensive review, so that it can benefit specialists and engineers in the chemical, mining, iron, metallurgy, and steel industries.

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Section: Phase Identification and Quantificationmentioning

confidence: 99%

X-ray Diffraction Techniques for Mineral Characterization: A Review for Engineers of the Fundamentals, Applications, and Research Directions

2022

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“…XRD has been used for the identification of the crystalline state of 5-FU and the possible interaction of the drug with four lipids [49,50]. XRD peak depends on crystal size because the crystalline nature of the drug was detected at a certain value at the 2θ range [51].…”

Section: Pre-formulation Studies With Excipientsmentioning

confidence: 99%

Pre-Formulation Study on 5-Fluorouracil and Certain Lipids for Solid Lipid Nanoparticles Preparation

et al. 2022

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Objective: The study's objective involved compatibility studies to investigate the possible interactions between 5-fluorouracil (5-FU) and four different lipids, and the most appropriate lipid was chosen. Differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier Transform Infrared spectroscopy (FT-IR) are used for the compatibility study between 5-FU and several excipients as cholesterol, compritol®, stearic acid, and glycerol monostearate (GMS). Methods: The physical mixture between 5-FU and each lipid was made by mixing of a certain amount of drug with the same amount of lipid. Drug lipid blended mixtures were made by solvent evaporation casting method. 5-FU alone, physical mixture and blended mixture were measured using Differential scanning calorimetry (DSC) to investigate melting peak of drug and effect of each lipid on this melting point, X-ray diffraction (XRD) to observe the crystalline or amorphous state of drug and Fourier Transform Infrared (FT-IR) to determine any chemical interaction between drug and these lipids by observing any shift happened to characteristic peaks related to the drug. Results: 5-FU Tm (280.04 °C) peak appeared in drug-lipid physical mixtures with minor changes in position while this peak disappeared in 5-FU-compritol® and 5-FU-cholesterol blended mixture, indicating that the drug is molecular dispersed. XRD result showed that the crystalline structure of 5-FU was present in physical mixtures with four lipids, while in the 5-FU-compritol® blended mixture, the crystalline state of the drug was disappeared, confirming the DSC result. The FT-IR spectrum of the 5-FU-physical mixtures with four lipids showed that all characteristic peaks of the drug appeared with minor changes. In the case of 5-FU-blended mixtures with mentioned lipids, no chemical interaction occurred between the drug and mentioned lipids except in the drug-stearic acid blended mixture, the N-H peak at 3136.25 cm-1 was disappeared due to amide ester formation. Conclusion: The most appropriate lipids suitable for the preparation of 5-FU solid lipid nanoparticles were GMS and cholesterol.

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“…On the other hand, the non-destructive nature of XRD and FTIR spectroscopic methods makes them ideal tools for systematic drug-excipient compatibility assessment in the pre-formulation studies. It is well known that the percent of crystallinity can influence a drug's processing behaviour as well as its pharmacological performance [13,28], being related to its solubility and dissolution [2,36]. Additionally, the vibrational changes detected by FTIR method serve as direct evidence for potential intermolecular interactions among the dosage components.…”

Section: Ft-ir Spectroscopymentioning

confidence: 99%

Compatibility Study Between Magnesium Orotate and Various Excipients in Their Physical Mixtures

MOISA¹

2022

FARMACIA

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The assessment of magnesium orotate compatibility with various excipients is an important step in the development of drug formulation and development. A good physicochemical compatibility between magnesium orotate and different excipients allows obtaining novel combinations with a complex composition that enhances the therapeutic effect of magnesium orotate. The purpose of this research was to assess the compatibility of magnesium orotate with various excipients presently used in pharmaceutical formulations in a 1:1 mass ratio, which was higher than what was currently used in drug formulation, with the possibility of influencing the expected therapeutic benefit by delaying magnesium orotate release. The compatibility of the most used excipients (croscarmellose, corn starch, lactate, magnesium stearate, microcrystalline cellulose, polyvinylpyrrolidone and talcum) with magnesium orotate was assessed by investigating the TG-DTA-DTG curves, FTIR spectra and XRD pattern of the excipients and their physical mixture with magnesium orotate. A partial compatibility of magnesium orotate with corn starch, cellulose and croscarmellose was noticed based on thermal analysis. The FTIR spectra and TG-DTG results indicated the best stability of magnesium orotate in combination with polyvinyl-pyrrolidone, while a possible incompatibility between magnesium orotate and talcum was evidenced based upon FTIR spectra. No modifications in XRD pattern of magnesium orotate was noticed in the spectra corresponding to binary combinations. By corroborating the results, one can conclude that polyvinyl-pyrrolidone is the best choice as excipient for magnesium orotate. RezumatEvaluarea compatibilității orotatului de magneziu cu diverși excipienți este un pas important în dezvoltarea formulării și dezvoltării medicamentelor. O bună compatibilitate fizico-chimică între orotatul de magneziu și diferiți excipienți permite obținerea unor combinații noi, cu o compoziție complexă, care sporește efectul terapeutic al orotatului de magneziu. Scopul acestui studiu a fost de a evalua compatibilitatea orotatului de magneziu cu diferiți excipienți utilizați în prezent în formulările farmaceutice, într-un raport masic 1:1, mai mare decât cel utilizat în prezent în formularea medicamentelor, cu o posibilă influență asupra efectului terapeutic așteptat, prin încetinirea eliberării orotatului de magneziu. Compatibilitatea celor mai utilizați excipienți (croscarmeloză, amidon de porumb, lactat, stearat de magneziu, celuloză microcristalină, polivinilpirolidonă și talc) cu orotatul de magneziu a fost evaluată prin investigarea curbelor TG-DTA-DTG, a spectrelor FTIR și a modelului XRD a excipienților și a amestecului lor fizic cu orotatul de magneziu. Pe baza analizei termice, s-a observat o compatibilitate parțială a orotatului de magneziu cu amidonul de porumb, celuloza și croscarmeloza. Spectrele FTIR și rezultatele TG-DTG au indicat cea mai bună stabilitate a orotatului de magneziu în combinație cu polivinilpirolidona, în timp ce o posibilă incompatibilitate în...

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Using X-ray Diffraction Techniques for Biomimetic Drug Development, Formulation, and Polymorphic Characterization

Cited by 26 publications

References 126 publications

X-ray Diffraction Techniques for Mineral Characterization: A Review for Engineers of the Fundamentals, Applications, and Research Directions

X-ray Diffraction Techniques for Mineral Characterization: A Review for Engineers of the Fundamentals, Applications, and Research Directions

Pre-Formulation Study on 5-Fluorouracil and Certain Lipids for Solid Lipid Nanoparticles Preparation

Compatibility Study Between Magnesium Orotate and Various Excipients in Their Physical Mixtures

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