Investigations on the Mechanism of Magnesium Stearate to Modify Aerosol Performance in Dry Powder Inhaled Formulations

Jetzer, Martin W.; Schneider, Marcel; Morrical, Bradley D.; Imanidis, Georgios

doi:10.1016/j.xphs.2017.12.006

Cited by 31 publications

(11 citation statements)

References 64 publications

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“…To further investigate the effects of the dispersibility enhancers on FPF, leucine and Mg-St were added in formulation F2 and F3. The high FPF of the formulations F2 and F3 (containing leucine and Mg-St); 40.9% and 41.9%, respectively are the evidence of the greater dispersion and aerosolization of puerarin as compared to drug only formulation devoid of the excipients [ 40 ]. The recovered dose ranged between 98% to 100% for all the formulation mixtures [ 41 ].…”

Section: Resultsmentioning

confidence: 99%

Puerarin dry powder inhaler formulations for pulmonary delivery: Development and characterization

et al. 2021

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This study aims at developing and characterizing the puerarin dry powder inhaler (DPI) formulations for pulmonary delivery. The inhalable particles size (<2 μm) was accomplished by micronization and its morphology was examined by scanning electron microscopy (SEM). The puerarin-excipient interaction in powder mixtures was analyzed by using Fourier transform infrared spectroscopy (FTIR), Raman confocal microscopy, X-Ray powder Diffraction (XRD), and differential scanning calorimetry (DSC) methods. Using a Twin stage impinger (TSI), the in-vitro aerosolization of the powder formulations was carried out at a flow rate of 60 L/min and the drug was quantified by employing a validated HPLC method. No significant interactions between the drug and the excipients were observed in the powder formulations. The fine particle fraction (FPF) of the drug alone was 4.2% which has increased five to six-fold for the formulations with aerosolization enhancers. Formulation containing lactose as large carriers produced 32.7% FPF, which further increased with the addition of dispersibility enhancers, leucine and magnesium stearate (40.8% and 41.2%, respectively). The Raman and FTIR techniques are very useful tool for understanding structural integrity and stability of the puerarin in the powder formulations. The puerarin was found to be compatible with the excipients used and the developed DPI formulation may be considered as an efficient formulation for pulmonary delivery for the management of various diseases at a very low dose.

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Section: Resultsmentioning

confidence: 99%

Puerarin dry powder inhaler formulations for pulmonary delivery: Development and characterization

et al. 2021

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“…The samples were eluted with an isocratic method described by Jetzer et al, where simultaneous determination of both active compounds takes place. [79]. Specifically, the column was a type of CNW Technologies Athena C18, 120 A, 5 µm, 250 mm × 4.6 mm set at room temperature.…”

Section: Swelling Capacitymentioning

confidence: 99%

Microencapsulation of Fluticasone Propionate and Salmeterol Xinafoate in Modified Chitosan Microparticles for Release Optimization

et al. 2020

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Chitosan (CS) is a natural polysaccharide, widely studied in the past due to its unique properties such as biocompatibility, biodegradability and non-toxicity. Chemical modification of CS is an effective pathway to prepare new matrices with additional functional groups and improved properties, such as increment of hydrophilicity and swelling rate, for drug delivery purposes. In the present study, four derivatives of CS with trans-aconitic acid (t-Acon), succinic anhydride (Succ), 2-hydroxyethyl acrylate (2-HEA) and acrylic acid (AA) were prepared, and their successful grafting was confirmed by FTIR and 1H-NMR spectroscopies. Neat chitosan and its grafted derivatives were fabricated for the encapsulation of fluticasone propionate (FLU) and salmeterol xinafoate (SX) drugs, used for chronic obstructive pulmonary disease (COPD), via the ionotropic gelation technique. Scanning electron microscopy (SEM) micrographs demonstrated that round-shaped microparticles (MPs) were effectively prepared with average sizes ranging between 0.4 and 2.2 μm, as were measured by dynamic light scattering (DLS), while zeta potential verified in all cases their positive charged surface. FTIR spectroscopy showed that some interactions take place between the drugs and the polymeric matrices, while X-ray diffraction (XRD) patterns exhibited that both drugs were encapsulated in MPs’ interior with a lower degree of crystallinity than the neat drugs. In vitro release studies of FLU and SX exposed a great amelioration in the drugs’ dissolution profile from all modified CS’s MPs, in comparison to those of neat drugs. The latter fact is attributed to the reduction in crystallinity of the active substances in the MPs’ interior.

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“…Given that inhalation products have markedly different aerosol performance metrics, we prefer to use the total lung dose ( ) as the defining metric. Adhesive mixtures comprising a force control agent such as magnesium stearate can achieve a of about 50% of the nominal dose [21,22]. Hence, the breakpoint between low and high doses would equate to a of 1 mg.…”

Section: High Dose Delivery With Portable Dry Powder Inhalersmentioning

confidence: 99%

Optimizing Spray-Dried Porous Particles for High Dose Delivery with a Portable Dry Powder Inhaler

Son¹,

Miller²,

Weers³

2021

Preprint

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This manuscript critically reviews the design and delivery of spray-dried particles for the achievement of high total lung doses (TLD) with a portable dry powder inhaler. We introduce a new metric termed the product density, which is simply the TLD of a drug divided by the volume of the receptacle it is contained within. The product density is given by the product of three terms: the packing density (the mass of powder divided by the volume of the receptacle), the drug loading (the mass of drug divided by the mass of powder), and the aerosol performance (the TLD divided by the mass of drug). This manuscript discusses strategies for maximizing each of these terms. Spray drying at low drying rates with small amounts of a shell-forming excipient (low Peclet Number) leads to formation of higher density particles with high packing densities. This enables ultrahigh TLD (>100 mg of drug) to be achieved from a single receptacle. Emptying of powder from capsules is directly proportional to the mass of powder in the receptacle, requiring an inhaled volume of about 1 L for fill masses between 40 and 50 mg and up to 3.2 L for a fill mass of 150 mg.

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Investigations on the Mechanism of Magnesium Stearate to Modify Aerosol Performance in Dry Powder Inhaled Formulations

Cited by 31 publications

References 64 publications

Puerarin dry powder inhaler formulations for pulmonary delivery: Development and characterization

Puerarin dry powder inhaler formulations for pulmonary delivery: Development and characterization

Microencapsulation of Fluticasone Propionate and Salmeterol Xinafoate in Modified Chitosan Microparticles for Release Optimization

Optimizing Spray-Dried Porous Particles for High Dose Delivery with a Portable Dry Powder Inhaler

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