Recent advances in the characterization of amorphous pharmaceuticals by X-ray diffractometry

Thakral, Seema; Terban, Maxwell W.; Thakral, Naveen K.; Suryanarayanan, Raj

doi:10.1016/j.addr.2015.12.013

Cited by 68 publications

(39 citation statements)

References 75 publications

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“…The physical form of the components and their compatibility can be determined using XRD, DSC, Raman and infrared spectroscopies, all of which will be familiar to researchers in this field. The interested reader is directed to some excellent reviews which have documented recent progress in these techniques [258,259]. Other important characterisation includes a determination of the drug encapsulation efficiency of the fibers (which is often almost 100% and can be determined using UV-vis spectroscopy, high performance liquid chromatography (HPLC) or other quantitative analysis methods) and the stability of the API after electrospinning (which is often explored using HPLC or nuclear magnetic resonance spectroscopy) [260,261].…”

Section: Characterisation Of Electrospun Nanofiber-based Asdsmentioning

confidence: 99%

Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review

Williams

et al. 2018

Journal of Controlled Release

231

147

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The development of oral dosage forms for poorly water-soluble active pharmaceutical ingredients (APIs) is a persistent challenge. A range of methods has been explored to address this issue, and amorphous solid dispersions (ASDs) have received increasing attention. ASDs are typically prepared by starting with a liquid precursor (a solution or melt) and applying energy for solidification. Many techniques can be used, with the emergence of electrospinning as a potent option in recent years. This method uses electrical energy to induce changes from liquid to solid. Through the direct applications of electrical energy, electrospinning can generate nanofiber-based ASDs from drug-loaded solutions, melts and melt-solutions. The technique can also be combined with other approaches using the application of mechanical, thermal or other energy sources. Electrospinning has numerous advantages over other approaches to produce ASDs. These advantages include extremely rapid drying speeds, ease of implentation, compatibility with a wide range of active ingredients (including those which are thermally labile), and the generation of products with large surface areas and high porosity. Furthermore, this technique exhibits the potential to create so-called 'fifth-generation' ASDs with nanostructured architectures, such as core/shell or Janus systems and their combinations. These advanced systems can improve dissolution behaviour and provide programmable drug release profiles. Additionally, the fiber components and their spatial distributions can be precisely controlled. Electrospun fiber-based ASDs can maintain an incorporated active ingredient in the amorphous physical form for prolonged periods of time because of their homogeneous drug distribution within the polymer matrix (typically they comprise solid solutions), and ability to inhibit molecular motion. These ASDs can be utilised to generate oral dosage forms for poorly water-soluble drugs, resulting in linear or multiple-phase release of one or more APIs. Electrospun ASDs can also be exploited as templates for manipulating molecular self-assembly, offering a bridge between ASDs and other types of dosage forms. This review addresses the development, advantages and pharmaceutical applications of electrospinning for producing polymeric ASDs. Material preparation and analysis procedures are considered. The mechanisms through which performance has been improved are also discussed.

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Section: Characterisation Of Electrospun Nanofiber-based Asdsmentioning

confidence: 99%

Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review

Williams

et al. 2018

Journal of Controlled Release

231

147

View full text Add to dashboard Cite

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“…In order to overcome poor solubility and improve bioavailability the use of amorphous and nanocrystalline systems are growing, as is the necessity of improved methods to characterize them6. In amorphous systems the atoms are ordered primarily at short (2–5 Å) and medium-range (5–20 Å.…”

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confidence: 99%

Local Structure of Ion Pair Interaction in Lapatinib Amorphous Dispersions characterized by Synchrotron X-Ray diffraction and Pair Distribution Function Analysis

Araujo

Benmore

Byrn³

2017

Sci Rep

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For many years, the idea of analyzing atom-atom contacts in amorphous drug-polymer systems has been of major interest, because this method has always had the potential to differentiate between amorphous systems with domains and amorphous systems which are molecular mixtures. In this study, local structure of ionic and noninonic interactions were studied by High-Energy X-ray Diffraction and Pair Distribution Function (PDF) analysis in amorphous solid dispersions of lapatinib in hypromellose phthalate (HPMCP) and hypromellose (HPMC-E3). The strategy of extracting lapatinib intermolecular drug interactions from the total PDF x-ray pattern was successfully applied allowing the detection of distinct nearest neighbor contacts for the HPMC-E3 rich preparations showing that lapatinib molecules do not cluster in the same way as observed in HPMC-P, where ionic interactions are present. Orientational correlations up to nearest neighbor molecules at about 4.3 Å were observed for polymer rich samples; both observations showed strong correlation to the stability of the systems. Finally, the superior physical stability of 1:3 LP:HPMCP was consistent with the absence of significant intermolecular interactions in (∆) in the range of 3.0 to 6.0 Å, which are attributed to C-C, C-N and C-O nearest neighbor contacts present in drug-drug interactions.

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“…11B). Our study confirms the literature findings [81][82][83] that XRPD is a proper method for the detection of water sorption in polymer systems.…”

Section: X-ray Powder Diffractionsupporting

confidence: 82%

“…Similar changes were found in the amorphous HPC's XRPD patterns, as Teng at al. described in case of PVP [81]. The shape and the high angle halo displayed a shoulder resembling the halo for bound water.…”

Section: X-ray Powder Diffractionmentioning

confidence: 99%

Design and characterization of mucoadhesive hydroxypropyl cellulose oral films

Gottnek

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Recent advances in the characterization of amorphous pharmaceuticals by X-ray diffractometry

Cited by 68 publications

References 75 publications

Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review

Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review

Local Structure of Ion Pair Interaction in Lapatinib Amorphous Dispersions characterized by Synchrotron X-Ray diffraction and Pair Distribution Function Analysis

Design and characterization of mucoadhesive hydroxypropyl cellulose oral films

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