Characterization of Drug Particle Surface Energetics and Young’s Modulus by Atomic Force Microscopy and Inverse Gas Chromatography

Davies, Michael J.; Brindley, Anne; Chen, Xinyong; Marlow, Maria; Doughty, Stephen W.; Shrubb, Ian; Roberts, Clive J.

doi:10.1007/s11095-005-5647-z

Cited by 67 publications

(34 citation statements)

References 55 publications

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“…Knowledge of surface energetics of excipients can therefore be of similar importance to that of the APIs in the formulation design of multi-component systems and the prediction of processing performance such as binder-drug adhesion, powder flow, compaction and granulation performances (2)(3)(4)(5). Common methods of characterizing the surface energetics of particulate pharmaceuticals rely on indirect approaches involving the use of characterized or known vapours, liquids or solids as probes as in inverse gas chromatography (IGC) (6), sessile drop contact angle (7) and atomic force microscopy (AFM) (8) respectively.…”

Section: Introductionmentioning

confidence: 99%

Determination of surface heterogeneity of d-mannitol by sessile drop contact angle and finite concentration inverse gas chromatography

Hinder

Watts

et al. 2010

International Journal of Pharmaceutics

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Section: Introductionmentioning

confidence: 99%

Determination of surface heterogeneity of d-mannitol by sessile drop contact angle and finite concentration inverse gas chromatography

Hinder

Watts

et al. 2010

International Journal of Pharmaceutics

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“…28) On the other hand, mechanofusion enhanced the surface energy of the lactose carrier. As the surface energy enhancement could be reflected in an increase of the surface adhesiveness, 30,31) there seemed to be discrepancy between the ACI study profile and the measured surface adhesiveness.…”

mentioning

confidence: 97%

Application and Mechanism of Inhalation Profile Improvement of DPI Formulations by Mechanofusion with Magnesium Stearate

et al. 2008

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Dry powder inhaler (DPI) formulations have been utilized in the treatment of respiratory disease [1][2][3] and for systemic administration.4 -7) They have become common in the inhalation therapy field because of various advantages, such as being free from anti-environmental propellants 8) and ease of use with portable small devices.DPI formulations with fine drug particles and coarse carrier particles have been widely used for a long time. Usually their components are simple and they can be manufactured with conventional equipment. Therefore, they appear to be a valuable option as the formulation for clinical trials, especially in the early stages of development. The carrier particles play the critical role in preventing the agglomeration of fine drug particles which possesses high surface energy due to their large specific surface area. On the other hand, it is necessary to achieve the high deposition in the deep lungs to satisfy the required bioavailability. Because only small particles (aerodynamic diameter below 5 mm) can reach the lungs, fine drug particles should be detached from the coarse carrier particles through the inhalation process. The percentage of small particles to the entire dose is defined as fine particle fraction (FPF). Therefore, FPF is an index of the extent of deposition in the lungs.Studies have been conducted to clarify the factors that control the inhalation properties of the carrier-based DPI formulations. [9][10][11][12][13][14] Many studies focused on the carrier surface properties especially rugosity and/or coverage of high energy binding sites. 10,[15][16][17][18][19][20][21] Surface energy of particles would be one of the major factors influencing the inhalation profile of DPI including FPF. 22,23) However the mechanism of FPF increase has not been fully clarified so far. This seems to be because the inhalation profile of DPI is affected by various factors including particle size, morphology electrostatic charge and inhalation condition. 10,12,[24][25][26] Therefore, there is a need for preparation and characterization of series of powder samples that are different in surface properties but similar in other properties and compare them under the same inhalation condition.Mechanofusion can modify the surface energy of lactose carrier particles without drastic change of the particle size and can make the particle shape round to lessen the differences.Inverse gas chromatography (IGC) has been utilized to examine the effect of surface energy on the inhalation behavior of DPI. We reported that mechanofusion on a lactose carrier changed the carrier's surface condition and the inhalation properties of DPI formulations containing the lactose carrier and Compound A.27) The Andersen cascade impactor (ACI) profile suggested that the increase of FPF was accompanied by the decrease of the interaction between Compound A and carrier particles. Begat et al. also reported that mechanofusion of lactose with Mg-St reduced the interaction between drug and lactose particles.28) Mg-St is known as lubri...

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“…Elasticity (Davies et al, 2005;Perkins et al, 2009Perkins et al, , 2007 Deformation (local) Hardness (Masterson and Cao, 2008;Perkins et al, 2009) Degradation during storage or processing (Perkins et al, 2009) Force distance measurements Elastic modulus Elasticity (Davies et al, 2005;Perkins et al, 2009, 2007 Hardness (Masterson and Cao, 2008;Perkins et al, 2009) Adhesion Degradation during storage or processing (Perkins et al, 2009) Crystallinity (Perkins et al, 2007) Particle surface energetics (Davies et al, 2005;Perkins et al, 2009) Chemical surface properties (Hooton et al, 2004) Correlation of surface specific properties (Perkins et al, 2007;Ward et al, 2005) Colloidal probe AFM Adhesion Physical interaction between materials (Beach et al, 2002;Hooton et al, 2004;Rogueda et al, 2011) Chemical interaction between materials (Hooton et al, 2004;Islam et al, 2014;Rogueda et al, 2011) Cohesive adhesive balance (Begat et al, 2004a;Jones et al, 2008a,b) Particle surface energetics (Hooton et al, 2006a) Electrostatic surface properties (Götzinger and Peukert, 2003;Kwek et al, 2011) Triboelectric charging (Kwek et al, 2011) Surface polarity (Kwek et al, 2011) Fig. 1.…”

Section: Phase Imagingmentioning

confidence: 99%

“…Similarly, Davies et al (2005) investigated the local elastic modulus of budesonide. Masterson and Cao (2008) and James et al (2008) demonstrated the success of the technique by assessing the elastic moduli of a range of materials: formoterol fumarate, salmeterol xinafoate, salbutamol sulphate, mometasone furoate and salmon calcitonin (Masterson and Cao, 2008) and by evaluating the hardness of drug, lactose and sucrose particles (James et al, 2008).…”

Section: Mechanical Propertiesmentioning

confidence: 99%

Characterisation of dry powder inhaler formulations using atomic force microscopy

Weiss

McLoughlin

Cathcart

2015

International Journal of Pharmaceutics

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A B S T R A C TInhalation formulations are a popular way of treating the symptoms of respiratory diseases. The active pharmaceutical ingredient (API) is delivered directly to the site of action within the deep lung using an inhalation device such as the dry powder inhaler (DPI).The performance of the formulation and the efficiency of the treatment depend on a number of factors including the forces acting between the components. In DPI formulations these forces are dominated by interparticulate interactions. Research has shown that adhesive and cohesive forces depend on a number of particulate properties such as size, surface roughness, crystallinity, surface energetics and combinations of these. With traditional methods the impact of particulate properties on interparticulate forces could be evaluated by examining the bulk properties. Atomic force microscopy (AFM), however, enables the determination of local surface characteristics and the direct measurement of interparticulate forces using the colloidal probe technique. AFM is considered extremely useful for evaluating the surface topography of a substrate (an API or carrier particle) and even allows the identification of crystal faces, defects and polymorphs from high-resolution images. Additionally, information is given about local mechanical properties of the particles and changes in surface composition and energetics. The assessment of attractive forces between two bodies is possible by using colloidal probe AFM.This review article summarises the application of AFM in DPI formulations while specifically focussing on the colloidal probe technique and the evaluation of interparticulate forces.2015 Elsevier B.V. All rights reserved.

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Characterization of Drug Particle Surface Energetics and Young’s Modulus by Atomic Force Microscopy and Inverse Gas Chromatography

Cited by 67 publications

References 55 publications

Determination of surface heterogeneity of d-mannitol by sessile drop contact angle and finite concentration inverse gas chromatography

Determination of surface heterogeneity of d-mannitol by sessile drop contact angle and finite concentration inverse gas chromatography

Application and Mechanism of Inhalation Profile Improvement of DPI Formulations by Mechanofusion with Magnesium Stearate

Characterisation of dry powder inhaler formulations using atomic force microscopy

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