Characterization and Aerosolization Performance of HydroxyPropyl-Beta-Cyclodextrin Particles Produced Using Supercritical Assisted Atomization

Wu, Hsien-Tsung; Chuang, Yao-Hsiang; Lin, Han-Cyuan; Chien, Liang-Jung

doi:10.3390/polym13142260

Cited by 5 publications

(9 citation statements)

References 47 publications

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“…In addition, increased LEU content altered the morphology of the spherical γ-CD carrier particles by depositing needle-like fibrous crystals on the surface, thus producing pronounced wrinkles and roughened surfaces. The same phenomenon was observed in previous studies on BDP-mannitol composites [15], HP-β-CD particles [28], as well as the complex particles derived from sulfobutylether-β-cyclodextrin [9]. In vitro aerodynamic evaluation indicated an extremely high ED fraction (ED, %) which was higher than 97% for all prepared samples.…”

Section: In Vitro Aerosolization Performance Of γ-Cd Carrier Particle...supporting

confidence: 87%

“…Based on the results, γ-CD particles which were prepared in the presence of LEU exhibited better flowability (runs #L2-L6) in comparison to that of the sample in run #L1 (performed under high H R condition). In particular, γ-CD-LEU particles with an optimum LEU content of 10% exhibited excellent aerosol performance (run #L4), which is comparable to the results of previous studies [17,28,42]. Correspondingly, the FPF of the same γ-CD particles was significantly increased to 23.5 ± 1.5% (approximately double that of γ-CD particles, which had no LEU; run #L1), along with the lowest recorded MMAD of 3.44 ± 0.2 µm.…”

Section: In Vitro Aerosolization Performance Of γ-Cd Carrier Particle...supporting

confidence: 87%

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Instant Formulation of Inhalable Beclomethasone Dipropionate—Gamma-Cyclodextrin Composite Particles Produced Using Supercritical Assisted Atomization

Lin

et al. 2023

Pharmaceutics

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Medical composites derived from Gamma-cyclodextrin (γ-CD) and beclomethasone dipropionate−gamma-cyclodextrin (BDP−γ-CD) are synthesized over supercritical-assisted atomization (SAA) herein. Carbon dioxide, which serves the dual function of spraying medium and co-solute, is incorporated in this process along with the ethanolic solvent. Results indicate that, for fine spherical particles, optimized aerosol performance could be obtained with 50.0% (w/w) ethanolic solvent, precipitator, and saturator at 373.2 K and 353.2 K, respectively, and carbon dioxide-to-γ-CD flow ratio of 1.8 in the presence of 10 wt% leucine (LEU) as dispersion enhancer. It is also noted that γ-CD solution at low concentration typically renders better aerosol performance of the particles. During drug particle-derivation, the solubility of drug BDP elevated considerably due to the formation of inclusion complexes, further assisted by the ethanolic solvent which increases the lipophilicity of BDP. Meanwhile, the in vitro aerosolization and dissolution performance of drug composites derived from varied γ-CD-to-BDP mass ratio (Z) were also evaluated. It was found that high Z promises higher fine particle fraction in the obtained drug composite while the dissolution rate of active ingredient (BDP) exhibits positive correlation to the content of water-soluble excipient (γ-CD) in the formulation. This study offers a new avenue for instant drug formulation with promising pulmonary delivery over the SAA technique.

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Section: In Vitro Aerosolization Performance Of γ-Cd Carrier Particle...supporting

confidence: 87%

Section: In Vitro Aerosolization Performance Of γ-Cd Carrier Particle...supporting

confidence: 87%

Instant Formulation of Inhalable Beclomethasone Dipropionate—Gamma-Cyclodextrin Composite Particles Produced Using Supercritical Assisted Atomization

Lin

et al. 2023

Pharmaceutics

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“…The solvent concentration and optimal conditions for the production of drug–HP-β-CD composites via SAA were adopted from the phase solubility study and a previous study on the formation of fine spherical HP-β-CD particles with excellent aerosolization performance [ 36 ]. These conditions include 54.2% ( w / w ) aqueous ethanol as the solvent, mass flow ratio ( R ) of 1.95 between CO 2 and the ethanol solution, precipitator temperature and saturator temperature of 373.15 K and 353.15 K, respectively, and addition of the dispersion enhancer (LEU) with an optimal concentration of 13.0 mass% (100 × LEU/(LEU+HP-β-CD)).…”

Section: Resultsmentioning

confidence: 99%

Immediate Release Formulation of Inhaled Beclomethasone Dipropionate-Hydroxypropyl-Beta-Cyclodextrin Composite Particles Produced Using Supercritical Assisted Atomization

Chuang

Lin

et al. 2022

Polymers

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In this study, the enhanced solubilization performance of a poorly soluble drug, beclomethasone dipropionate (BDP), was investigated using hydroxypropyl-β-cyclodextrin (HP-β-CD) and ethanol. The enhanced solubility of the drug was determined using the phase solubility method and correlated as a function of both HP-β-CD and ethanol concentrations. The effective progress of drug solubility originated from the formation of cyclodextrin and BDP inclusion complexes and increase in the lipophilicity of the medium, by aqueous ethanol, for hydrophobic BDP. BDP and HP-β-CD composite particles were produced using supercritical assisted atomization (SAA) with carbon dioxide as the spraying medium, 54.2% (w/w) aqueous ethanol as the solvent, and an optimal amount of the dispersion enhancer leucine. The effect of the mass ratio of HP-β-CD to BDP (Z) on the in vitro aerosolization and in vitro dissolution performance of BDP–HP-β-CD composite particles was evaluated. The aerosolization performance showed that the fine particles fraction (FPF) of the composite particles increased with increasing mass ratio. The water-soluble excipient (HP-β-CD) effectively enhance the dissolution rate of BDP from composite particles. This study suggests that BDP–HP-β-CD composite particles produced using SAA can be employed in immediate-release drug formulations for pulmonary delivery.

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“…Following set optimal parameters of SAA process T P : 373.2 K, T s : 353.2 K, flow ratio of CO 2 /HPβCD: 1.8, and fixed concentration of the HPβCD solution 10 mg/mL, Leu was added to investigate formulations' aerosol performance. The mass concentration of 13% achieved a FPF value of 27.8 ± 0.4. whereas the augmented concentration of Leu to 16.7% resulted in agglomerations and reduced FPF value (Wu et al 2021 ).…”

Section: Drying Techniquesmentioning

confidence: 99%

Recent progress in drying technologies for improving the stability and delivery efficiency of biopharmaceuticals

Emami

Shokooh

Yazdi

2022

J. Pharm. Investig.

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Background Most biopharmaceuticals are developed in liquid dosage forms that are less stable than solid forms. To ensure the stability of biopharmaceuticals, it is critical to use an effective drying technique in the presence of an appropriate stabilizing excipient. Various drying techniques are available for this purpose, such as freeze drying or lyophilization, spray drying, spray freeze-drying, supercritical fluid drying, particle replication in nonwetting templates, and fluidized bed drying. Area covered In this review, we discuss drying technologies and their applications in the production of stable solid-state biopharmaceuticals, providing examples of commercially available products or clinical trial formulations. Alongside this, we also review how different analytical methods may be utilized in the evaluation of aerosol performance and powder characteristics of dried protein powders. Finally, we assess the protein integrity in terms of conformational and physicochemical stability and biological activity. Expert opinion With the aim of treating either infectious respiratory diseases or systemic disorders, inhaled biopharmaceuticals reduce both therapeutic dose and cost of therapy. Drying methods in the presence of optimized protein/stabilizer combinations, produce solid dosage forms of proteins with greater stability. A suitable drying method was chosen, and the process parameters were optimized based on the route of protein administration. With the ongoing trend of addressing deficiencies in biopharmaceutical production, developing new methods to replace conventional drying methods, and investigating novel excipients for more efficient stabilizing effects, these products have the potential to dominate the pharmaceutical industry in the future.

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Characterization and Aerosolization Performance of HydroxyPropyl-Beta-Cyclodextrin Particles Produced Using Supercritical Assisted Atomization

Cited by 5 publications

References 47 publications

Instant Formulation of Inhalable Beclomethasone Dipropionate—Gamma-Cyclodextrin Composite Particles Produced Using Supercritical Assisted Atomization

Instant Formulation of Inhalable Beclomethasone Dipropionate—Gamma-Cyclodextrin Composite Particles Produced Using Supercritical Assisted Atomization

Immediate Release Formulation of Inhaled Beclomethasone Dipropionate-Hydroxypropyl-Beta-Cyclodextrin Composite Particles Produced Using Supercritical Assisted Atomization

Recent progress in drying technologies for improving the stability and delivery efficiency of biopharmaceuticals

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