An overview of automated systems relevant in pharmaceutical salt screening

Kumar, Lokesh; Amin, Aeshna; Bansal, Arvind K.

doi:10.1016/j.drudis.2007.08.002

Cited by 51 publications

(30 citation statements)

References 40 publications

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“…The search for new drugs of potential clinical interest directed to specific pathologically relevant targets is usually conducted through the analysis of the effect of hundreds to thousands of potential compounds, under many different possible conditions, in tests carried out under automated or semi-automated regimes (43)(44)(45). Our fluorescent plate reader assay has demonstrated its utility to evaluate surfactant inhibition effects such as those produced by serum proteins like albumin (8,46).…”

Section: Discussionmentioning

confidence: 99%

High-throughput evaluation of pulmonary surfactant adsorption and surface film formation

Ravasio

Cruz

Pérez‐Gil

et al. 2008

Journal of Lipid Research

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The assessment of new therapeutic strategies to cure surfactant-associated lung disorders would greatly benefit from assay systems allowing routine evaluations of surfactant functions. We present a method to measure surfactant adsorption kinetics into interfacial air-liquid interfaces based on fluorescence microplate readers. The principle of measurement is simple, robust, and reproducible: Wells of a microtiter plate contain an aqueous solution of a light-absorbing agent. Fluorescence is excited and collected from the top of the wells so that fluorescently labeled surfactant injected into the bulk can be detected only once adsorbed into the air-liquid interface. Mass transfer from the bulk to the interface is achieved by orbital shaking implemented in the plate reader instrument. The method has been tested and validated by using phospholipids or surfactants of different origins, by using albumin as surfactant inhibitor, and by comparison of results with Wilhelmy balance measurements. The method is suited for implementation in high-throughput screening routines for conditions affecting, or improving, surfactant film formation. In contrast to surface tension measurements, our method gives a direct readout of the amount of surfactant adsorbing into the interface, including the functionally important amount of material firmly associating with the interfacial film.-Ravasio, A., A. Cruz, J. Pérez-Gil, and T. Haller. High-throughput evaluation of pulmonary surfactant adsorption and surface film formation. J. Lipid Res. 2008Res. . 49: 2479Res. -2488

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Section: Discussionmentioning

confidence: 99%

High-throughput evaluation of pulmonary surfactant adsorption and surface film formation

Ravasio

Cruz

Pérez‐Gil

et al. 2008

Journal of Lipid Research

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“…Also, as has already been discussed, for inhalation candidates the amount of material readily available for such work can often be limited by synthetic complexity and by the small quantities produced for early clinical studies, hence any methodology needs to be bulk sparing. Comprehensive reviews on the subject of solid-form screening have been published [65][66][67][68][69][70][71][72], therefore, only a brief overview will be provided herein.…”

Section: Screening Capabilitymentioning

confidence: 99%

A Perspective on Synthetic and Solid-Form Enablement of Inhalation Candidates

Selby¹,

Koning

Roberts

2011

Future Med. Chem.

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The administration of compounds by a dry-powder inhaler presents significant challenges to the development and discovery chemist, owing to the stringent requirements placed upon the physical characteristics of the active pharmaceutical ingredient and the high complexity of the molecules concerned. The current state of synthetic chemistry technology is such that commercial syntheses of these compounds are demanding but achievable. While synthetic chemistry will remain a major component of the development of inhaled therapies, the main challenge facing practitioners in this area is the early identification of a suitable solid form. Further advances in the prediction of solid-form properties would significantly enable this field and may allow triage of molecules to be carried out at the design stage of projects.

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“…Therefore, and not surprisingly, several high‐throughput screening (HTS) approaches and automated systems have been developed in the last decade [6–10]. HTS tend to explore both salt formation and polymorphism in one experimental set‐up.…”

Section: Introductionmentioning

confidence: 99%

“…Therefore, and not surprisingly, several high-throughput screening (HTS) approaches and automated systems have been developed in the last decade. [6][7][8][9][10] HTS tend to explore both salt formation and polymorphism in one experimental set-up. The use of many different acids combined with a large selection of diverse solvents often results in different crystalline forms of various salts.…”

Section: Introductionmentioning

confidence: 99%