Studies on the spray dried lactose as carrier for dry powder inhalation

Wu, Lifu; Xu, Miao; Shan, Ziyun; Huang, Ying; Li, L u; Pan, Xin; Yao, Qinghe; Li, G e; Wu, Chuanbin

doi:10.1016/j.ajps.2014.07.006

Cited by 79 publications

(36 citation statements)

References 23 publications

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“…Pulmonary delivery systems offer several advantages including increased local drug concentration in the lungs, reduced systemic side effects, rapid onset of action due to the enormous surface area and plentiful capillary vessels in the lung, and avoidance of the first-pass metabolism associated with the liver (20–25). While dry powder aerosolized nanoparticles (less than 500 nm) will be exhaled owing to their small size and mass, aerosolized particles with aerodynamic diameters of 1–5 µm (or larger) can effectively deposit into the lungs.…”

Section: Introductionmentioning

confidence: 99%

Nanocomposite microparticles (nCmP) for the delivery of tacrolimus in the treatment of pulmonary arterial hypertension

Wang

Cuddigan

Gupta

et al. 2016

International Journal of Pharmaceutics

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Tacrolimus (TAC) has exhibited promising therapeutic potential in the treatment of pulmonary arterial hypertension (PAH); however, its application is prevented by its poor solubility, instability, poor bioavailability, and negative systemic side effects. To overcome the obstacles of using TAC for the treatment of PAH, we developed nanocomposite microparticles (nCmP) for the pulmonary delivery of tacrolimus in the form of dry powder aerosols. These particles can provide targeted pulmonary delivery, improved solubility of tacrolimus, the potential of penetration through mucus barrier, and controlled drug release. In this system, tacrolimus-loaded polymeric nanoparticles (NP) were prepared via emulsion solvent evaporation and nCmP were prepared by spray drying these NP with mannitol. The NP were approximately 200 nm in diameter with narrow size distribution both before loading into and after redispersion from nCmP. The NP exhibited smooth, spherical morphology and the nCmP were raisin-like spheres. High encapsulation efficacy was achieved both in the encapsulation of tacrolimus in NP and that of NP in nCmP. nCmP exhibited desirable aerosol dispersion properties, allowing them to deposit into the deep lung regions for effective drug delivery. A549 cells were used as in vitro models to demonstrate the non-cytotoxicity of TAC nCmP. Overall, the designed nCmP have the potential to aid in the delivery of tacrolimus for the treatment of PAH.

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Section: Introductionmentioning

confidence: 99%

Nanocomposite microparticles (nCmP) for the delivery of tacrolimus in the treatment of pulmonary arterial hypertension

Wang

Cuddigan

Gupta

et al. 2016

International Journal of Pharmaceutics

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“…Researchers have proved that insulin aerosols with large geometric diameter and porous morphology with 10 μm of MMAD t got aerosolized quickly from a dry powder inhaler (DPI) and settled in the alveoli of the lungs (Ungaro et al, 2009). To produce aerosols with desired properties, many techniques such as spray drying (Wu et al, 2014), spray-freeze drying (Ali & Lamprecht, 2014), solvent evaporation (Ungaro, De Rosa, Miro, Quaglia, & La Rotonda, 2006), and electrospraying (Morozov, 2011) have been experimented.…”

Section: Introductionmentioning

confidence: 99%

Development of β‐carotene aerosol formulations using a modified spray dryer

Lavanya

Dutta

Moses

et al. 2019

J Food Process Engineering

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The objective of this study was to develop β‐carotene inhalable powders through a modified spray drying process. The conventional spray dryer nozzle was replaced with a nebulizer. The core (β‐carotene) to wall (HPβCD) ratio was varied (1:10, 1:25, and 1:50) to determine its effect on physical properties, aerosolization, and morphology of the powders. Scanning electron microscopy images of particles confirmed the formation of spherical particles with porous surface, with geometric diameters ranging from 2.9 to 3.8 μm. The particles exhibited low density and excellent flowability. Core to wall ratios showed a narrow range of mass median aerodynamic diameters of 3.02, 2.82, and 2.85 μm for 1:10, 1:25, and 1:50, respectively. Around 73–81% of powder was emitted from the dry powder inhaler for all core to wall ratios. The in vitro release of β‐carotene inhalable powder was studied with TRIS buffer for 12 h; it was found that in 1:50 formulation powders, the release was slow and sustained as compared to other formulations, and the release was found to be via diffusion. This approach can be used for developing a range of bioactive inhalable powders for dry powder inhalation applications. Practical Applications Development of β‐carotene inhalable powder by modified spray dryer is helpful in achieving the required aerodynamic properties. By using this method nutrients can be supplemented through lungs in the form of aerosol for effective absorption of the same in blood. This approach can be used for developing a range of bioactive inhalable powders for dry powder inhalation applications.

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“…The deep lung (alveolar) region can be utilized as a route for systematic drug delivery due to the enormous surface area available and nearby plentiful capillary vessels that facilitate drug absorption, the very thin (approximately 0.1 µm) liquid layer over the alveoli that ensures rapid and unhindered drug absorption, and low enzymatic activity, which enhances drug availability (Collier et al, 2016; Cui et al, 2011; Hoang et al, 2014). As a result, various therapeutics such as antibiotics, proteins, peptides, anti-cancer drugs (Wu et al, 2014), plasmid DNA (Takashima et al, 2007), siRNA (Jensen et al, 2010), and anti-tuberculosis (TB) drugs have been employed in inhalation formulations for the treatment of pulmonary diseases such as asthma, chronic obstructive pulmonary disease (COPD), cystic fibrosis (CF)-related pulmonary infections, and lung cancer (Meenach et al, 2013a; Wu et al, 2014). …”

Section: Introductionmentioning

confidence: 99%

“…Dry powders are a dosage formulation that delivers therapeutics to the lung, in the form of particles, using a dry powder inhaler (Wu et al, 2014). Compared with liquid aerosols, these formulations offer additional benefits such as enhanced stability of the formulation, controllable particle size for targeting different regions of the lung, and increased drug loading of hydrophobic payloads (Cohen et al, 2010; Meenach et al, 2013a).…”

Section: Introductionmentioning

confidence: 99%

“…Spray drying has proven to be a suitable technology in the preparation of dry powder therapeutics (Meenach et al, 2013a), as it is capable of producing respirable microparticles for deep lung delivery with acceptable aerosol dispersion properties (Belotti et al, 2015). Properties of dry powder particles such as particle size, particle shape, and surface morphology can be modified by controlling the spray drying production process, thus providing desirable particle characteristics (Belotti et al, 2015; Wu et al, 2014). …”

Section: Introductionmentioning

confidence: 99%

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Development and physicochemical characterization of acetalated dextran aerosol particle systems for deep lung delivery

Wang

Gupta

Meenach

2017

International Journal of Pharmaceutics

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Biocompatible, biodegradable polymers are commonly used as excipients to improve the drug delivery properties of aerosol formulations, in which acetalated dextran (Ac-Dex) exhibits promising potential as a polymer in various therapeutic applications. Despite this promise, there is no comprehensive study on the use of Ac-Dex as an excipient for dry powder aerosol formulations. In this study, we developed and characterized pulmonary drug delivery aerosol microparticle systems based on spray-dried Ac-Dex with capabilities of (1) delivering therapeutics to the deep lung, (2) targeting the particles to a desired location within the lungs, and (3) releasing the therapeutics in a controlled fashion. Two types of Ac-Dex, with either rapid or slow degradation rates, were synthesized. Nanocomposite microparticle (nCmP) and microparticle (MP) systems were successfully formulated using both kinds of Ac-Dex as excipients and curcumin as a model drug. The resulting MP were collapsed spheres approximately 1 µm in diameter, while the nCmP were similar in size with wrinkled surfaces, and these systems dissociated into 200 nm nanoparticles upon reconstitution in water. The drug release rates of the Ac-Dex particles were tuned by modifying the particle size and ratio of fast to slow degrading Ac-Dex. The pH of the environment was also a significant factor that influenced the drug release rate. All nCmP and MP systems exhibited desirable aerodynamic diameters that are suitable for deep lung delivery (e.g. below 5 µm). Overall, the engineered Ac-Dex aerosol particle systems have the potential to provide targeted and effective delivery of therapeutics into the deep lung.

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Studies on the spray dried lactose as carrier for dry powder inhalation

Cited by 79 publications

References 23 publications

Nanocomposite microparticles (nCmP) for the delivery of tacrolimus in the treatment of pulmonary arterial hypertension

Nanocomposite microparticles (nCmP) for the delivery of tacrolimus in the treatment of pulmonary arterial hypertension

Development of β‐carotene aerosol formulations using a modified spray dryer

Development and physicochemical characterization of acetalated dextran aerosol particle systems for deep lung delivery

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