The impact of electrostatic charge in pharmaceutical powders with specific focus on inhalation-powders

Karner, Stefan; Urbanetz, Nora Anne

doi:10.1016/j.jaerosci.2011.02.010

Cited by 98 publications

(46 citation statements)

References 113 publications

(144 reference statements)

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“…It is known that electrostatic charge is one of five mechanisms that govern the deposition of inhaled particles in the lungs (Karner and Urbanetz, 2011;Wong et al, 2015). Furthermore, the electrostatic charge of the plastic constituting the dry powder inhaler devices can have a strong impact on material loss during manufacturing of the product and upon actuation of the inhaler (Karner and Urbanetz, 2011).…”

Section: Spray Dried Sodium Hyaluronate Powders With Respirable Attrimentioning

confidence: 99%

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Engineered sodium hyaluronate respirable dry powders for pulmonary drug delivery

Martinelli

Balducci

Kumar

et al. 2017

International Journal of Pharmaceutics

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Engineered sodium hyaluronate respirable dry powders for pulmonary drug delivery.International Journal of Pharmaceutics http://dx.doi.org/10. 1016/j.ijpharm.2016.12.002 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. Abstract:Sodium hyaluronate (HYA) warrants attention as a material for inhalation due to its (i) therapeutic potential, (ii) utility as a formulation excipient or drug carrier, and (iii) ability to target lung inflammation and cancer. This study aimed to overcome formulation and manufacturing impediments to engineer biocompatible spray-dried HYA powders for inhalation. Novel methodology was developed to produce HYA microparticles by spray drying. Different types of surfactant were included in the formulation to improve powder respirability, which was evaluated in vitro using cascade impactors. The individual formulation components and formulated products were evaluated for their biocompatibility with A549 respiratory epithelial cells. The inclusion of stearyl surfactants, 5% w/v, produced the most respirable HYA-powders; FPF 59.0-66.3%. A trend to marginally higher respirability was observed for powders containing stearylamine > stearyl alcohol > cetostearyl alcohol. Pure HYA was biocompatible with A549 cells at all concentrations measured, but the biocompatibility of the stearyl surfactants (based on lethal concentration 50%; LC50) in the MTT assay ranked stearyl alcohol > cetostearyl alcohol > stearylamine with LC50 of 24.7, 13.2 and 1.8 µg/mL, respectively. We report the first respirable HYA powders produced by spray-drying. A lead formulation containing 5% stearyl alcohol was identified for further studies aimed at translating the proposed benefits of inhaled HYA into safe and clinically effective HYA products.

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Section: Spray Dried Sodium Hyaluronate Powders With Respirable Attrimentioning

confidence: 99%

“…Charged particles tend to adhere on the walls of the mixing vessel In the mixing process as well as to the inhaler material during loading and discharging and thus influence the released dose (Karner and Urbanetz, 2011;Wong et al, 2015).…”

Section: Spray Dried Sodium Hyaluronate Powders With Respirable Attrimentioning

confidence: 99%

Engineered sodium hyaluronate respirable dry powders for pulmonary drug delivery

Martinelli

Balducci

Kumar

et al. 2017

International Journal of Pharmaceutics

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“…In addition, particle charging can cause problems in the manufacture of formulations by affecting powder flow, reducing fill and dose uniformity [18,19]; for example particle charging may cause adhesion and deposition of particles to walls especially in case of fine particles such as in dry powder inhalers [20,21]. Triboelectrification has been used to study the impact of the counter ion on flurbiprofen salts as a consideration during the preformulation process [22], reduce the charging of flurbiprofen (a drug with a high propensity for charging) in binary mixtures of cellulose ethers [23], ordered mixing [24] and recently as a way of manipulating the charge of their final product of solid dispersions using single solvents and binary mixtures of solvents [25].…”

Section: Accepted M Manuscriptmentioning

confidence: 99%

An assessment of triboelectrification effects on co-ground solid dispersions of carbamazepine

et al. 2016

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An assessment of triboelectrification effects on co-ground solid dispersions of carbamazepine, Powder Technology (2016Technology ( ), doi: 10.1016Technology ( /j.powtec.2016 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.A C C E P T E D M A N U S C R I P T AbstractOne of strategies adopted to improve the dissolution rates of poorly soluble drugs is by co-grinding the drug with a hydrophilic carrier. However, the introduction of mechanical forces during th e grinding process can lead to changes in the physicochemical characteristics as well as an increase in the surface free energy of the ground particles, which causes an alteration in the electrostatic properties of these particles. The solid state characteristics of glucosamine hydrochloride (GLU) and carbamazepine (CBZ) and their co-ground mixtures were studied using DSC, XRPD and SEM.These revealed that polymorphic transformations occurred due to the grinding process. The influence of grinding time on the triboelectrification properties of the formulations was also studied.Both pure CBZ and GLU powders were predominantly electro-positively charged and their charging properties increased with increasing grinding time. CBZ:GLU physical mixtures exhibited complicated bipolar charging behaviour, however, when subjected to grinding, these mixtures demonstrated mainly electronegative charge properties. The influence of both grinding time and CBZ content within CBZ:GLU mixtures were examined. The value of net-electronegative-charge density of CBZ:GLU mixtures was shown to increase with grinding time and /or when increasing the percentage proportion of CBZ up to 30 % w:w. This study helps to provide information about the handling of these formulation and gives a formulator tools to ascertain appropriate ratios for handling and possible simultaneous dissolution improvements.

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“…To evaluate electrostatic forces and triboelectric charging, Faraday pails or wells are commonly used (Byron et al, 1997;Elajnaf et al, 2006;Karner and Urbanetz, 2011). Such a device basically consists of two conductive balls or wells of different sizes.…”

Section: Electrical Force Measurementsmentioning

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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The impact of electrostatic charge in pharmaceutical powders with specific focus on inhalation-powders

Cited by 98 publications

References 113 publications

Engineered sodium hyaluronate respirable dry powders for pulmonary drug delivery

Engineered sodium hyaluronate respirable dry powders for pulmonary drug delivery

An assessment of triboelectrification effects on co-ground solid dispersions of carbamazepine

Characterisation of dry powder inhaler formulations using atomic force microscopy

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