Hydroxypropyl-β-cyclodextrin as anti-hygroscopicity agent inamorphous lactose carriers for dry powder inhalers

Zhao, Ziyu; Zhang, Xuejuan; Cui, Yingtong; Huang, Ying; Huang, Zhengwei; Wang, Guanlin; Liang, Ruifeng; Pan, Xin; Liang, Tao; Wu, Chuanbin

doi:10.1016/j.powtec.2018.09.098

Cited by 14 publications

(6 citation statements)

References 48 publications

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“…The efficacy of this route relies on the adequate aerosolization properties of the dosage form, as well as the drug permeability through the lung, its solubility in small aqueous volumes, and its suitable organoleptic properties. Both solid and dissolved CD/drug ICs have been formulated as dry powders and nebulizers, improving the aerosolization properties of formulations and enhancing the drug dissolution in the lung fluids [ 116 ] and recent research continues showing the promising potential of using CDs for pulmonary medications [ [117] , [118] , [119] ].…”

Section: Resultsmentioning

confidence: 99%

Technological evolution of cyclodextrins in the pharmaceutical field

Rincón-López

Almanza-Arjona

Riascos

et al. 2021

Journal of Drug Delivery Science and Technology

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We herein disclose how global cyclodextrin-based pharmaceutical technologies have evolved since the early 80s through a 1998 patents dataset retrieved from Derwent Innovation Index. We used text-mining techniques based on the patents semantic content to extract the knowledge contained therein, to analyze technologies related to the principal attributes of CDs: solubility, stability, and taste-masking enhancement. The majority of CDs pharmaceutical technologies are directed toward parenteral aqueous solutions. The development of oral and ocular formulations is rapidly growing, while technologies for nasal and pulmonary routes are emerging and seem to be promising. Formulations for topical, transdermal, vaginal, and rectal routes do not account for a high number of patents, but they may be hiding a great potential, representing opportunity research areas. Certainly, the progress in materials sciences, supramolecular chemistry, and nanotechnology, will influence the trend of that, apparently neglected, research. The bottom line, CDs pharmaceutical technologies are still increasing, and this trend is expected to continue in the coming years. Patent monitoring allows the identification of relevant technologies and trends to prioritize research, development, and investment in both, academia and industry. We expect the scope of this approach to be applied in the pharmaceutical field beyond CDs technological applications.

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Section: Resultsmentioning

confidence: 99%

Technological evolution of cyclodextrins in the pharmaceutical field

Rincón-López

Almanza-Arjona

Riascos

et al. 2021

Journal of Drug Delivery Science and Technology

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“…In the present study, the surface roughness of HP-β-CD/MAN microcapsules was higher that of other microcapsules. This was likely due to the increase in MAN and HP-β-CD concentrations as the moisture evaporated, with the high- and low-solubility-component HP-β-CD and MAN, respectively, tending to migrate to the inner and outer layer of the droplet, with the MAN forming crystals as its concentration becomes saturated [ 8 , 21 , 22 ]. This finding is consistent with the microcapsule crystallinity shown in Figure 2 , explaining the rough morphology observed.…”

Section: Resultsmentioning

confidence: 99%

Mannitol Is a Good Anticaking Agent for Spray-Dried Hydroxypropyl-Beta-Cyclodextrin Microcapsules

Kou

Cheng

et al. 2023

Molecules

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Agglomeration is an undesirable phenomenon that often occurs in spray-dried microcapsules powder. The objective of this work is to determine the best solution for spray-dried hydroxypropyl-β-cyclodextrin (HP-β-CD) microcapsules from four anticaking agents, namely calcium stearate (CaSt), magnesium stearate (MgSt), silicon dioxide (SiO2), and mannitol (MAN), and to explore their anticaking mechanisms. Our results showed that MAN was found to be the superior anticaking agent among those tested. When the MAN ratio is 12%, the microcapsules with a special Xanthium-type shape had higher powder flowability and lower hygroscopicity and exhibited good anticaking properties. Mechanism research revealed that CaSt, MgSt, and SiO2 reduce hygroscopicity and caking by increasing the glass transition temperature of the microcapsules, while MAN prevents the hydroxyl group of HP-β-CD from combining with water molecules in the air by a crystal outer-layer on the microcapsule surface.

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“…Specifically, it realized real-time monitoring of PDPs of DPIs in the inhaler device, throat and bronchi separately, which was the indispensable prerequisite for efficient optimization of DPIs. Except for the air flow rate, there were some other key factors that influenced the PDPs such as the physicochemical properties of carriers 16 , 17 , 18 and parameters of inhaler devices 19 . It was noteworthy that carriers served as the fundamental component of carrier-based DPIs due to their high proportions in the formulations 20 .…”

Section: Introductionmentioning

confidence: 99%

A real-time and modular approach for quick detection and mechanism exploration of DPIs with different carrier particle sizes

Cui

Huang

Zhang

et al. 2022

Acta Pharmaceutica Sinica B

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Dry powder inhalers (DPIs) had been widely used in lung diseases on account of direct pulmonary delivery, good drug stability and satisfactory patient compliance. However, an indistinct understanding of pulmonary delivery processes (PDPs) hindered the development of DPIs. Most current evaluation methods explored the PDPs with over-simplified models, leading to uncompleted investigations of the whole or partial PDPs. In the present research, an innovative modular process analysis platform (MPAP) was applied to investigate the detailed mechanisms of each PDP of DPIs with different carrier particle sizes (CPS). The MPAP was composed of a laser particle size analyzer, an inhaler device, an artificial throat and a pre-separator, to investigate the fluidization and dispersion, transportation, detachment and deposition process of DPIs. The release profiles of drug, drug aggregation and carrier were monitored in real-time. The influence of CPS on PDPs and corresponding mechanisms were explored. The powder properties of the carriers were investigated by the optical profiler and Freeman Technology four powder rheometer. The next generation impactor was employed to explore the aerosolization performance of DPIs. The novel MPAP was successfully applied in exploring the comprehensive mechanism of PDPs, which had enormous potential to be used to investigate and develop DPIs.

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Hydroxypropyl-β-cyclodextrin as anti-hygroscopicity agent inamorphous lactose carriers for dry powder inhalers

Cited by 14 publications

References 48 publications

Technological evolution of cyclodextrins in the pharmaceutical field

Technological evolution of cyclodextrins in the pharmaceutical field

Mannitol Is a Good Anticaking Agent for Spray-Dried Hydroxypropyl-Beta-Cyclodextrin Microcapsules

A real-time and modular approach for quick detection and mechanism exploration of DPIs with different carrier particle sizes

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