Powder Production and Particle Engineering for Dry Powder Inhaler Formulations

Lin, Yu-Chieh; Wong, John; Qu, Li; Chan, Hak‐Kim; Zhou, Qi Tony

doi:10.2174/1381612821666150820111134

Cited by 77 publications

(51 citation statements)

References 167 publications

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“…However, such carrier-based DPI formulations may not be suitable for high dose antibiotics because the drug load of a single dose is substantially limited by the inclusion of carriers (24). Particle engineering is of growing interest as an effective approach to improve the flow and aerosolization of the drug particles by reducing intrinsic powder cohesion (25–27). Spray drying is one of the most popular approaches to engineer the inhalable powder formulation to improve aerosol performance (28,29).…”

Section: Introductionmentioning

confidence: 99%

Physico-Chemical Properties, Aerosolization and Dissolution of Co-Spray Dried Azithromycin Particles with L-Leucine for Inhalation

Mangal

Nie

et al. 2018

Pharm Res

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Purpose Inhalation therapy is popular to treat lower respiratory tract infections. Azithromycin is effective against some bacteria that cause respiratory tract infections; but it has poor water solubility that may limit its efficacy when administrated as inhalation therapy. In this study, dry powder inhaler formulations were developed by co-spray drying azithromycin with L-leucine with a purpose to improve dissolution. Methods The produced powder formulations were characterized regarding particle size, morphology, surface composition and in-vitro aerosolization performance. Effects of L-leucine on the solubility and in-vitro dissolution of azithromycin were also evaluated. Results The spray dried azithromycin alone formulation exhibited a satisfactory aerosol performance with a fine particle fraction (FPF) of 62.5 ± 4.1%. Addition of L-leucine in the formulation resulted in no significant change in particle morphology and FPF, which can be attributed to enrichment of azithromycin on the surfaces of composite particles. Importantly, compared with the spray-dried amorphous azithromycin alone powder, the co-spray dried powder formulations of azithromycin and L-leucine demonstrated a substantially enhanced in-vitro dissolution rate. Such enhanced dissolution of azithromycin could be attributed to the formation of composite system and the acidic microenvironment around azithromycin molecules created by the dissolution of acidic L-leucine in the co-spray dried powder. Fourier transform infrared spectroscopic data showed intermolecular interactions between azithromycin and L-leucine in the co-spray dried formulations. Conclusions We developed the dry powder formulations with satisfactory aerosol performance and enhanced dissolution for a poorly water soluble weak base, azithromycin, by co-spray drying with an amino acid, L-leucine.

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Section: Introductionmentioning

confidence: 99%

Physico-Chemical Properties, Aerosolization and Dissolution of Co-Spray Dried Azithromycin Particles with L-Leucine for Inhalation

Mangal

Nie

et al. 2018

Pharm Res

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“…12 However, jet-milled powders are often highly cohesive due to the high surface energy generated during the milling process. 13 The jet-milled powder thus often possesses poor flowability, fluidization and aerosolization properties.…”

Section: Introductionmentioning

confidence: 99%

Investigation of the Changes in Aerosolization Behavior Between the Jet-Milled and Spray-Dried Colistin Powders Through Surface Energy Characterization

Jong

Morton

et al. 2016

Journal of Pharmaceutical Sciences

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This study aimed to investigate the surface energy factors behind improved aerosolization performance of spray-dried colistin powder formulations compared to those produced by jet-milling. Inhalable colistin powder formulations were produced by jet-milling or spray-drying (with or without L-leucine). Scanning electron micrographs showed the jet-milled particles had irregularly angular shapes, while the spray-dried particles were more spherical. Significantly higher fine particle fractions (FPFs) were measured for the spray-dried (43.8-49.6%) vs. the jet-milled formulation (28.4 %) from a Rotahaler at 60L/min; albeit the size distribution of the jet-milled powder was smaller. Surprisingly, addition of L-leucine in the spray drying feed-solution gave no significant improvement in FPF. As measured by inverse gas chromatography, spray-dried formulations had significantly (p<0.001) lower dispersive, specific and total surface energy values and more uniform surface energy distributions than the jet-milled powder. Interestingly, no significant difference was measured in the specific and total surface energy values between the spray-dried formulation with or without L-leucine. Based upon our previous findings in the self-assembling behavior of colistin in aqueous solution and the surface energy data obtained here, we propose the self-assembly of colistin molecules during spray-drying, contributed significantly to the reduction of surface free energy and the superior aerosolization performance.

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“…In addition, the charge carried by the particles is also very high, which may result in cohesiveness aggregation and agglomeration of the particles. This will cause a hindrance when the medicament is to be delivered via the inhaler (Malcolmson and Embleton, 1998;Lin, 2015). Although there is an advancement in the design of inhalers, this method is not widely preferred for manufacturing of DPI.…”

Section: Millingmentioning

confidence: 99%

Recent updates on dry powder for inhalation for pulmonary drug delivery systems

Deshkar

Vas

2019

ijrps

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Pulmonary drug delivery system is an attractive and most promising approach which is gaining great impetus for the delivery of various therapeutic agents which includes administration of proteins and peptides, agents for the treatment of tuberculosis, asthma, diabetes chronic obstructive pulmonary diseases (COPD), various fungal infections, cancer, etc. This route has gained great importance due to its large surface and the absorptive area, which can potentially bypass the hepatic first-pass metabolism. The dawn of nanotechnology has brought a lot of advancement in the pre-existing formulation aspect with respect to reducing the systemic toxicity and dosing, specific targeting and enhanced efficiency of the treatment. This review reflects on the basics of pulmonary drug delivery, various formulations options available for administration via dry powder inhalers and advances in the same.

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Powder Production and Particle Engineering for Dry Powder Inhaler Formulations

Cited by 77 publications

References 167 publications

Physico-Chemical Properties, Aerosolization and Dissolution of Co-Spray Dried Azithromycin Particles with L-Leucine for Inhalation

Physico-Chemical Properties, Aerosolization and Dissolution of Co-Spray Dried Azithromycin Particles with L-Leucine for Inhalation

Investigation of the Changes in Aerosolization Behavior Between the Jet-Milled and Spray-Dried Colistin Powders Through Surface Energy Characterization

Recent updates on dry powder for inhalation for pulmonary drug delivery systems

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