Low density, good flowability cyclodextrin-raffinose binary carrier for dry powder inhaler: anti-hygroscopicity and aerosolization performance enhancement

Zhao, Ziyu; Huang, Zhengwei; Zhang, Xuejuan; Huang, Ying; Cui, Yingtong; Ma, Cheng; Wang, Guanlin; Freeman, Tim; Lu, Xiang-Yun; Pan, Xin; Wu, Chuanbin

doi:10.1080/17425247.2018.1450865

Cited by 30 publications

(10 citation statements)

References 70 publications

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“…Indeed, Zhao et al proved that a spherical formulation composed only of raffinose displays physical properties which are completely different to corrugated particles made of HPβCD and raffinose (ratio 60/40). While diameters were similar among experimental groups (d0.5 = 4 µm), bulk density, aeration and permeability results were highly different, indicating a higher sensitivity to the airflow for corrugated particles [26].…”

Section: Aerosolization Performance Parametersmentioning

confidence: 81%

“…Another important point to take into consideration is the tendency that HPβCD has to form a shell layer around raffinose-core particles [26]. To demonstrate this claim, an experimental protocol was set up where HPβCD and raffinose were mixed in different proportions (0/100, 20/80, 30/70, 40/60, 60/40, 70/30, 80/20, and 100/0) and combined with budesonide (30/1 w/w); microparticles were produced by spray drying and physicochemical attributes were explored.…”

Section: Interest Of Cyclodextrins In Dpi Engineeringmentioning

confidence: 99%

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Influence of Composition and Spray-Drying Process Parameters on Carrier-Free DPI Properties and Behaviors in the Lung: A review

Lechanteur

Évrard

2020

Pharmaceutics

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Although dry powder inhalers (DPIs) have attracted great interest compared to nebulizers and metered-dose inhalers (MDIs), drug deposition in the deep lung is still insufficient to enhance therapeutic activity. Indeed, it is estimated that only 10–15% of the drug reaches the deep lung while 20% of the drug is lost in the oropharyngeal sphere and 65% is not released from the carrier. The potentiality of the powders to disperse in the air during the patient’s inhalation, the aerosolization, should be optimized. To do so, new strategies, in addition to classical lactose-carrier, have emerged. The lung deposition of carrier-free particles, mainly produced by spray drying, is higher due to non-interparticulate forces between the carrier and drug, as well as better powder uniformity and aerosolization. Moreover, the association of two or three active ingredients within the same powder seems easier. This review is focused on a new type of carrier-free particles which are characterized by a sugar-based core encompassed by a corrugated shell layer produced by spray drying. All excipients used to produce such particles are dissected and their physico-chemical properties (Péclet number, glass transition temperature) are put in relation with the lung deposition ability of powders. The importance of spray-drying parameters on powders’ properties and behaviors is also evaluated. Special attention is given to the relation between the morphology (characterized by a corrugated surface) and lung deposition performance. The understanding of the closed relation between particle material composition and spray-drying process parameters, impacting the final powder properties, could help in the development of promising DPI systems suitable for local or systemic drug delivery.

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Section: Aerosolization Performance Parametersmentioning

confidence: 81%

Section: Interest Of Cyclodextrins In Dpi Engineeringmentioning

confidence: 99%

Influence of Composition and Spray-Drying Process Parameters on Carrier-Free DPI Properties and Behaviors in the Lung: A review

Lechanteur

Évrard

2020

Pharmaceutics

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“…A new substance from oranges was isolated in 1930. It was thought that at that moment it was a member of a new vitamin class and was designated as vitamin P. Later on it became clear that this substance was a flavonoid (rutin) and till now more than 4000 varieties of flavonoids have been identified [6][7][8][9]. Chemically flavonoids are based on a 15-carbon skeleton composed of two benzene rings connected through a heterocyclic pyrane ring (C).…”

Section: Oralmentioning

confidence: 99%

“…Most of the drug molecule fail to reach at target site. To overcome these problems, various nanoparticles (NPs) based drug delivery systems have been designed by different researchers NPs are defined as particles sized below 1000 nm [7][8][9] and can be formulated from different biodegradable materials including natural or synthetic polymers, lipids or phospholipids, even metals. However, some other scientists regard the nanoscale range from 1 to 100 nm and 1 to 200 nm [10][11][12][13][14].…”

Section: Oralmentioning

confidence: 99%

Formulation and development of hesperidin loaded solid lipid nanoparticles for diabetes

2019

Biointerface Res Appl Chem

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Most of the research on Diabetes has been focused on synthetic compound however the disease burden of Diabetes has not been reduced, natural chemistry has provided various safer options in different disease areas. Hesperidin (bioflavonoid) has shown good promise in anti-diabetes efficacy however its bioavailability is low. In this work, SLN of Hesperidin wasprepared, physiochemically evaluated and tested for anti-diabetic potential. Various drug- lipid ratio were tested along with other formulation parameter for fabrication of formulation and optimization. The optimized formulation has been shownuniform particle size with negative surface charge with more than 90% entrapment efficiency and 91.45% drug release. The formulation exhibited Korsmeyer-Peppas release kinetic. The optimize formulation showed 21 % increase in anti-diabetes activity of hesperidin.

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“…It was commonly held that pulmonary drug delivery efficiency was mainly influenced by the transportation and detachment processes 12 , 15 . These two key processes were closely related to various factors, including the powder properties of the carrier 13 , 16 , 17 , the interaction of API‒carrier 18 , and the content of fine particles 19 , 20 . In addition, the air flow pattern 21 , 22 , 23 produced by the inhaler device and the inhalation mode of patients, such as the air flow rate 24 , 25 and duration of inhalation 26 , also exerted a significant influence on the PDPs.…”

Section: Introductionmentioning

confidence: 99%

Novel approach for real-time monitoring of carrier-based DPIs delivery process via pulmonary route based on modular modified Sympatec HELOS

Zhang

Cui

Liang

et al. 2020

Acta Pharmaceutica Sinica B

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An explicit illustration of pulmonary delivery processes (PDPs) was a prerequisite for the formulation design and optimization of carrier-based DPIs. However, the current evaluation approaches for DPIs could not provide precise investigation of each PDP separately, or the approaches merely used a simplified and idealized model. In the present study, a novel modular modified Sympatec HELOS (MMSH) was developed to fully investigate the mechanism of each PDP separately in real-time. An inhaler device, artificial throat and pre-separator were separately integrated with a Sympatec HELOS. The dispersion and fluidization, transportation, detachment and deposition processes of pulmonary delivery for model DPIs were explored under different flow rates. Moreover, time-sliced measurements were used to monitor the PDPs in real-time. The Next Generation Impactor (NGI) was applied to determine the aerosolization performance of the model DPIs. The release profiles of the drug particles, drug aggregations and carriers were obtained by MMSH in real-time. Each PDP of the DPIs was analyzed in detail. Moreover, a positive correlation was established between the total release amount of drug particles and the fine particle fraction (FPF) values ( R 2 = 0.9898). The innovative MMSH was successfully developed and was capable of illustrating the PDPs and the mechanism of carrier-based DPIs, providing a theoretical basis for the design and optimization of carrier-based DPIs.

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Low density, good flowability cyclodextrin-raffinose binary carrier for dry powder inhaler: anti-hygroscopicity and aerosolization performance enhancement

Abstract: CRBC with anti-hygroscopicity and aerosolization performance enhancement properties was a promising approach for pulmonary drug delivery, which could provide new possibilities to the application of hygroscopic carriers for DPI.

Cited by 30 publications

References 70 publications

Influence of Composition and Spray-Drying Process Parameters on Carrier-Free DPI Properties and Behaviors in the Lung: A review

Influence of Composition and Spray-Drying Process Parameters on Carrier-Free DPI Properties and Behaviors in the Lung: A review

Formulation and development of hesperidin loaded solid lipid nanoparticles for diabetes

Novel approach for real-time monitoring of carrier-based DPIs delivery process via pulmonary route based on modular modified Sympatec HELOS

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