Particle formation of budesonide from alcohol-modified subcritical water solutions

Carr, Adam G.; Mammucari, Raffaella; Foster, Neil R.

doi:10.1016/j.ijpharm.2010.11.042

Cited by 25 publications

(6 citation statements)

References 21 publications

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“…Powder particles had an appropriate median mass aerodynamic diameter (MMAD) of 3.8 µm and the FPF reached 66%. Another study has demonstrated that the atomization of budesonide in ethanol alone produced a very cohesive powder which was therefore not compatible with an efficient lung deposition, confirming the importance of amino acids to enhance drug aerosolization performance [51]. The relation between the solid content and the particle size is explained in Section 3.…”

Section: Amino Acidsmentioning

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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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: Amino Acidsmentioning

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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“…In terms of the extraction process, subcritical water has the added advantage of not requiring the drying of samples prior to processing . Among others, subcritical water technologies have been applied to the removal and decomposition of pollutants, for the extraction of compounds such as polycyclic aromatic hydrocarbons (PAHs) and polychlorinated biphenyls from soils, and recently to the micronization of hydrophobic drugs. ,,,− The onward desire for sustainability through the reduction in the costs and usage of toxic organic solvents, the search for alternatives that are nonexhaustible, and the need for versatility in extraction techniques became the motivation for the development of subcritical water technologies. , …”

Section: Introductionmentioning

confidence: 99%

Solubility and Solubility Modeling of Polycyclic Aromatic Hydrocarbons in Subcritical Water

Teoh

Mammucari

Melo

et al. 2013

Ind. Eng. Chem. Res.

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A static analytical equilibrium method was used to measure the binary and ternary solubilities of anthracene and p-terphenyl in subcritical water between 393 and 473 K and at 50 and 150 bar. Temperature was found to have the most significant effect on the solubility of polycyclic aromatic hydrocarbons (PAHs) in subcritical water. The effect of pressure, and the combined effect of temperature and pressure on solubility were found to be insignificant, particularly when the range of pressure considered is relatively small. The solubilities of PAHs were found to be governed primarily by sublimation pressure, and only secondarily by the dielectric constant of water. The Peng−Robinson equation of state was used to correlate the aqueous solubilities of PAHs under subcritical conditions, with good agreement between experimental and calculated values obtained for binary systems.

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“…Figure 3 depicts the SEM images of pure budesonide as regular geometric crystal form [45] and loss of geometry were clearly observed in the formulated polymeric films. All the film formulations showed smooth and homogenous surfaces may be due to interpenetration and considerable solubility of budesonide into the matrix system.…”

Section: Sem Analysismentioning

confidence: 99%

Budesonide-Cyclodextrin in Hydrogel System: Impact of Quaternary Surfactant on in vitro-in vivo Assessment of Mucosal Drug Delivery

Pattanaik¹,

Nandi²,

Sahoo³

et al. 2020

Rev. Chim.

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Budesonide, a glucocorticosteroid is generally used to treat chronic inflammation and asthma. Hepatic first-pass metabolism and poor solubility are the major causes of its limited oral bioavailability. Present work was undertaken for the preparation of hydrogel film formulation with cyclodextrin complexation of budesonide containing quaternary surfactant for possible enhancement of mucosal permeation. FTIR study confirmed drug-polymer hydrogen bonding. Almost complete amorphization of the drug was pronounced by SEM, DSC and XRD studies. The film containing benzalkonium and hydroxypropyl beta-cyclodextrin exhibited in vitro dissolution and mucosal permeation to the highest extent of 87.2 and 95.8 % respectively in contrast to the others. Film formed hydrogel in aqueous mucin and enhanced the mucosal tissue residence time due to the mucoadhesive nature of the polymer. Acute inflammation in the rabbit eye was controlled within 3 h by applying the film in the cul-de-sac. The presence of cyclodextrin and quaternary surfactant brought about significantly improved drug release and mucosal permeation compared to their absence in the HPMC film. Hydrogel formed in aqueous mucin enhanced the mucosal residence time and controlled acute inflammation in the rabbit eye within 3 h after topical application.

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Particle formation of budesonide from alcohol-modified subcritical water solutions

Cited by 25 publications

References 21 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

Solubility and Solubility Modeling of Polycyclic Aromatic Hydrocarbons in Subcritical Water

Budesonide-Cyclodextrin in Hydrogel System: Impact of Quaternary Surfactant on in vitro-in vivo Assessment of Mucosal Drug Delivery

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