Reverse aqueous emulsions and microemulsions in HFA227 propellant stabilized by non-ionic ethoxylated amphiphiles

Chokshi, Udayan; Selvam, Parthiban; Porcar, Lionel; Rocha, Sandro R. P. da

doi:10.1016/j.ijpharm.2008.10.025

Cited by 17 publications

(9 citation statements)

References 53 publications

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“…Although pluronics are not currently used in marketed pMDI products, several recent patents and publications have detailed the use of these surfactants in this manner [16–19]. The main motivation for this work was to determine if the in vitro aerosol performance of these model systems could be adequately modulated using the two components mentioned previously.…”

Section: Discussionmentioning

confidence: 99%

Tuning Aerosol Particle Size Distribution of Metered Dose Inhalers Using Cosolvents and Surfactants

Saleem

2013

BioMed Research International

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Objectives. The purpose of these studies was to understand the influence of cosolvent and surfactant contributions to particle size distributions emitted from solution metered dose inhalers (pMDIs) based on the propellant HFA 227. Methods. Two sets of formulations were prepared: (a) pMDIs-HFA 227 containing cosolvent (5–15% w/w ethanol) with constant surfactant (pluronic) concentration and (b) pMDIs-HFA 227 containing surfactant (0–5.45% w/w pluronic) with constant cosolvent concentration. Particle size distributions emitted from these pMDIs were analyzed using aerodynamic characterization (inertial impaction) and laser diffraction methods. Results. Both cosolvent and surfactant concentrations were positively correlated with median particle sizes; that is, drug particle size increased with increasing ethanol and pluronic concentrations. However, evaluation of particle size distributions showed that cosolvent caused reduction in the fine particle mode magnitude while the surfactant caused a shift in the mode position. These findings highlight the different mechanisms by which these components influence droplet formation and demonstrate the ability to utilize the different effects in formulations of pMDI-HFA 227 for independently modulating particle sizes in the respirable region. Conclusion. Potentially, the formulation design window generated using these excipients in combination could be used to match the particle size output of reformulated products to preexisting pMDI products.

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Section: Discussionmentioning

confidence: 99%

Tuning Aerosol Particle Size Distribution of Metered Dose Inhalers Using Cosolvents and Surfactants

Saleem

2013

BioMed Research International

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“…A similar approach is to formulate drugs in water-in-oil (reverse) microemulsions, where the emulsions create an aqueous microenvironment within the propellant system that enables the delivery of water-soluble compounds. For instance, Selvam et al and Chokshi et al utilized various ethylene oxide-propylene oxideethylene oxide (EO n −PO~3 0 −EO n ) polymers to form reverse aqueous microemulsions in HFAs 134a and 227 (139,140). It was found that PO-based amphiphiles can reduce the tension of the propellant-water interface, thus permitting the formation of reverse aggregates, which can be utilized to deliver polar solutes via MDIs.…”

Section: Stabilizing and Suspending Agentsmentioning

confidence: 99%

Advances in Metered Dose Inhaler Technology: Formulation Development

2014

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Pressurized metered dose inhalers (MDIs) are a long-standing method to treat diseases of the lung, such as asthma and chronic obstructive pulmonary disease. MDIs rely on the driving force of the propellant, which comprises the bulk of the MDI formulation, to atomize droplets containing drug and excipients, which ideally should deposit in the lungs. During the phase out of chlorofluorocarbon propellants and the introduction of more environmentally friendly hydrofluoroalkane propellants, many improvements were made to the methods of formulating for MDI drug delivery along with a greater understanding of formulation variables on product performance. This review presents a survey of challenges associated with formulating MDIs as solution or suspension products with one or more drugs, while considering the physicochemical properties of various excipients and how the addition of these excipients may impact overall product performance of the MDI. Propellants, volatile and nonvolatile cosolvents, surfactants, polymers, suspension stabilizers, and bulking agents are among the variety of excipients discussed in this review article. Furthermore, other formulation approaches, such as engineered excipient and drug-excipient particles, to deliver multiple drugs from a single MDI are also evaluated.

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“…Aqueous-based dispersions can be stabilized in the form of emulsions (micron size and kinetically stable) 22) or microemulsions (nanometer in size -transparent, and thermodynamically stable) 36,37) provided a suitable amphiphile is identified. Poly(lactide)- 38) , poly(propylene oxide)- 39) and fluorine-based 40) nonionic amphiphiles have been shown to be effective in stabilizing reverse water-in-HFA (W/HFA) emulsions. The emulsion-based formulations can be potentially used for the local or systemic delivery of therapeutics to and through the lungs.…”

Section: Novel Hfa-based Pmdi Formulationsmentioning

confidence: 99%

Applications of the Atomic Force Microscope in the Development of Propellant-based Inhalation Formulations

Rocha

2008

KONA

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Reverse aqueous emulsions and microemulsions in HFA227 propellant stabilized by non-ionic ethoxylated amphiphiles

Cited by 17 publications

References 53 publications

Tuning Aerosol Particle Size Distribution of Metered Dose Inhalers Using Cosolvents and Surfactants

Tuning Aerosol Particle Size Distribution of Metered Dose Inhalers Using Cosolvents and Surfactants

Advances in Metered Dose Inhaler Technology: Formulation Development

Applications of the Atomic Force Microscope in the Development of Propellant-based Inhalation Formulations

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