Lactose characteristics and the generation of the aerosol

Pilcer, Gabrielle; Wauthoz, Nathalie; Amighi, Karim

doi:10.1016/j.addr.2011.05.003

Cited by 178 publications

(122 citation statements)

References 211 publications

(331 reference statements)

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“…The aerodynamic diameter is the most appropriate measure of aerosol particle size because it relates to particle dynamic behavior and describes the main mechanisms of aerosol deposition in the lung as both gravitational settling and inertial impaction (55). Aerosol particles need to present aerodynamic diameters of between 1 and 5 µm to reach the lower respiratory tract.…”

Section: Preformulation Investigation -Micellar Solubilization Of Tmzmentioning

confidence: 99%

New dry powders for inhalation containing temozolomide-based nanomicelles for improved lung cancer therapy

Rosière

Gelbcke

Mathieu

et al. 2015

International Journal of Oncology

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Abstract. Besides the numerous advantages of a chemotherapy administered by the inhalation route for lung cancer therapy, dry powder for inhalation (DPI) offers many advantages compared to other techniques and seems to be a technique that is well-adapted to an anticancer treatment. DPI formulations were developed using the cytotoxic drug temozolomide and a new folate-grafted self-assembling copolymer, a conjugate of three components, folate-polyethylene glycol-hydrophobically-modified dextran (F-PEG-HMD). F-PEG-HMD was synthesized using carbodiimide-mediated coupling chemistry in three main steps. F-PEG-HMD was characterized by 1 H-NMR, mass spectrometry and thermal analysis. F-PEG-HMD presented a critical micellar concentration in water of 4x10 -7 M. F-PEG-HMD nanomicelles were characterized by a trimodal particle size distribution with Z-average diameter of 83±1 nm in water. Temozolomide-loaded nanomicelles were prepared by solubilization of F-PEG-HMD in the presence of temozolomide. Temozolomide solubility in water was increased in the presence of F-PEG-HMD (2-fold increase in molar solubility) which could potentially lead to increased local concentrations in the tumor site. The temozolomideloaded F-PEG-HMD nanomicelles were characterized by a Z-average diameter of ~50 to ~60 nm, depending on the F-PEG-HMD concentration used. The nanomicelles were then spray-dried to produce dry powders. Temozolomide remained stable during all the formulation steps, confirmed by similar in vitro anticancer properties for the DPI formulations and a raw temozolomide solution. Two of the developed DPI formulations were characterized by good aerodynamic properties (with a fine particle fraction of up to 50%) and were able to release the F-PEG-HMD nanomicelles quickly in aqueous media. Moreover, in vitro, the two DPI formulations showed wide pulmonary deposition in the lower respiratory tract where adenocarcinomas are more often found. The present study, therefore, shows that F-PEG-HMD-based dry powders for inhalation could constitute an interesting drug delivery system able to release nanomicelles that are useful in adenocarcinomas that overexpress folate receptors.

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Section: Preformulation Investigation -Micellar Solubilization Of Tmzmentioning

confidence: 99%

New dry powders for inhalation containing temozolomide-based nanomicelles for improved lung cancer therapy

Rosière

Gelbcke

Mathieu

et al. 2015

International Journal of Oncology

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“…The American and European pharmacopoeias have explained methods based on inertial impaction to assess the in vitro inhalation performance of formulations by determination of the fine particles (Pilcer et al, 2012).…”

Section: Expressions Used To Define Drug Lung Depositionmentioning

confidence: 99%

“…Such particles can theoretically be deposited in the deep lung after inhalation. The fine-particle fraction (FPF), which is the percentage of the FPD usually related to either the nominal dose (total drug mass contained in the device) or the recovered drug (sum of the drug collected in the device and in the different parts of the impingers or impactors after inhalation) (Pilcer et al, 2012).…”

Section: Fine Particle Dose (Fpd) and Fine Particle Fraction (Fpf)mentioning

confidence: 99%

“…In some cases, FPF can be calculated from emitted dose instead of total or recovered dose of drug from impingers or impactors. The ability of the powder to be fluidised by the airflow through an inhaler is usually indicated by the emission dose, whilst the FPD and FPF measure the capability of the formulation to be fluidised and deagglomerated in time to release the drug from the carrier to be deposited in the appropriate level of the impactors and impingers (Pilcer et al, 2012).…”

Section: Emitted Dosementioning

confidence: 99%

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The Role of Carrier in Dry Powder Inhaler

Hamishehkar¹,

Rahimpour²,

Javadzadeh³

2012

Recent Advances in Novel Drug Carrier Systems

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“…Small particles with an aerodynamic diameter of less than 5 μm are deposited deep in the lungs, but in most cases, they have poor flow properties as well as a highly cohesive nature, leading to low stability and poor quality of formulations. 1,2 The addition of a carrier can solve those problems. The fine particle fraction (FPF) represents the mass percentage of drug particles with an aerodynamic diameter below 5 μm, and is used for in vitro assessment of the aerodynamic properties of aerosols.…”

Section: Introductionmentioning

confidence: 99%

Empirical modeling of the fine particle fraction for carrier-based pulmonary delivery formulations

Pacławski

Szlęk

Lau

et al. 2015

IJN

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In vitro study of the deposition of drug particles is commonly used during development of formulations for pulmonary delivery. The assay is demanding, complex, and depends on: properties of the drug and carrier particles, including size, surface characteristics, and shape; interactions between the drug and carrier particles and assay conditions, including flow rate, type of inhaler, and impactor. The aerodynamic properties of an aerosol are measured in vitro using impactors and in most cases are presented as the fine particle fraction, which is a mass percentage of drug particles with an aerodynamic diameter below 5 μm. In the present study, a model in the form of a mathematical equation was developed for prediction of the fine particle fraction. The feature selection was performed using the R-environment package “fscaret”. The input vector was reduced from a total of 135 independent variables to 28. During the modeling stage, techniques like artificial neural networks, genetic programming, rule-based systems, and fuzzy logic systems were used. The 10-fold cross-validation technique was used to assess the generalization ability of the models created. The model obtained had good predictive ability, which was confirmed by a root-mean-square error and normalized root-mean-square error of 4.9 and 11%, respectively. Moreover, validation of the model using external experimental data was performed, and resulted in a root-mean-square error and normalized root-mean-square error of 3.8 and 8.6%, respectively.

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Lactose characteristics and the generation of the aerosol

Cited by 178 publications

References 211 publications

New dry powders for inhalation containing temozolomide-based nanomicelles for improved lung cancer therapy

New dry powders for inhalation containing temozolomide-based nanomicelles for improved lung cancer therapy

The Role of Carrier in Dry Powder Inhaler

Empirical modeling of the fine particle fraction for carrier-based pulmonary delivery formulations

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Lactose characteristics and the generation of the aerosol

Cited by 178 publications

References 211 publications

New dry powders for inhalation containing temozolomide-based nanomicelles for improved lung cancer therapy

New dry powders for inhalation containing temozolomide-based nanomicelles for improved lung cancer therapy

The Role of Carrier in Dry Powder Inhaler

Empirical modeling of the fine particle fraction for&nbsp;carrier-based pulmonary delivery formulations

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Product

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Empirical modeling of the fine particle fraction for carrier-based pulmonary delivery formulations