Leucine enhances aerosol performance of Naringin dry powder and its activity on cystic fibrosis airway epithelial cells

Prota, Lucia; Bifulco, Maurizio; Aquino, Rita Patrizia; Mencherini, Teresa; Russo, Paola

doi:10.1016/j.ijpharm.2011.03.055

Cited by 50 publications

(33 citation statements)

References 43 publications

(51 reference statements)

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“…13 B) whereas at 2.0 µM did not. As previously oserved in formulations for inhalation containing leucine [27], this effect seems to be related to leu ability to improve cell proliferation and metabolism of bronchial epithelial CF cells.…”

Section: Effect Of G/leu Powders On Viability Of Cf Airways Epitheliummentioning

confidence: 64%

“…The micronization by means of spray drying process and addition of opportune additives able to improve powder wettability seem to be a valid strategy for the formulation of an efficacious dry powder inhaler. Micronized particles were produced by completely dissolving the active naringin (N) alone (#NET3) or with 5% w/w of leucine (#NET3-leu5) as dispersibility enhancer in 7/3 water/ethanol solutions [27,28]. Spray drying conditions were: inlet temperature 110°C, drying air flow 500L/min, aspirator 100%, feed rate 5ml/min, nozzle 0.5mm.…”

Section: Naringin Dry Powders Production and Characterizationmentioning

confidence: 99%

See 1 more Smart Citation

Development and Investigation of Dry Powder Inhalers for Cystic Fibrosis

Russo¹,

Prota²,

Stigliani³

et al. 2012

Recent Advances in Novel Drug Carrier Systems

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Section: Effect Of G/leu Powders On Viability Of Cf Airways Epitheliummentioning

confidence: 64%

Section: Naringin Dry Powders Production and Characterizationmentioning

confidence: 99%

Development and Investigation of Dry Powder Inhalers for Cystic Fibrosis

Russo¹,

Prota²,

Stigliani³

et al. 2012

Recent Advances in Novel Drug Carrier Systems

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“…They also had been a decreased hygroscopicity, improved surface activity and a change in the density of the particles. L-leucine was especially able to improve drug aerosolization properties (Seville et al, 2007;Pilcer & Amighi, 2010;Prota et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Budesonide dry powder for inhalation: effects of leucine and mannitol on the efficiency of delivery

Rattanupatam¹,

Srichana

2014

Drug Delivery

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Objective: The aim of this study was to develop a budesonide dry powder for inhalation using L-leucine and L-leucine -sieved mannitol as a carrier. Materials and methods: Budesonide and L-leucine were co-spray dried at a mass ratio of 1:50 then blended with various mass ratios of sieved mannitol in the range of 20-80. A 2 3 factorial study was applied to investigate the effects of the spray drying variables; feed rate, aspirator setting and airflow rate on the powder characteristics. The prepared dry powders were characterized using fourier transform-infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and ultracentrifugation. Drug contents and aerosolization properties were evaluated using high performance liquid chromatography (HPLC) and the Andersen cascade impactor (ACI), respectively. Results and discussion: There was no interaction between budesonide and L-leucine after co-spraying. The budesonide dry powders had a mass median aerodynamic diameter (MMAD) in the range of 1.9-2.2 mm at a flow rate of 60 L/min that was suitable for pulmonary delivery. Sieved mannitol as a coarse carrier decreased the interparticulate forces between fine particles of the co-spray dried budesonide-L-leucine and resulted in a high fine particle fraction (FPF) in the range of 64-68% while the co-spray dried powder of budesonide-L-leucine had an FPF of $49%. Conclusions: Blending of the co-spray dried powder with sieved mannitol significantly improved the delivery efficiency of the micronized budesonide better than the co-spray dried with L-leucine alone.

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“…It has been reported that Leu reduces the surface energy of drug particles. 34,35) Yang et al reported that the inhalation performance of spray-dried powders was improved by an increase in Leu up to 20%. 36) In the present study, we added 5% Leu to the powder, which seemed to be sufficient to improve the dispersibility of the powder.…”

Section: Morphologicl Analysis Of Powder Particlesmentioning

confidence: 99%

Development of New Formulation Dry Powder for Pulmonary Delivery Using Amino Acids to Improve Stability

Suzuki

Okuda

Okamoto

2016

Biological & Pharmaceutical Bulletin

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Cationic polymers are being studied as non-viral gene delivery vectors. Poly{N-[N-(2-aminoethyl)-2-aminoethyl]aspartamide} (PAsp(DET)) and their block copolymers with poly(ethylene glycol), PEG-PAsp(DET), have been reported as efficient biodegradable non-viral vectors which form a polyplex with plasmid DNA (pDNA). However, the polyplexes are not stable because PAsp(DET) and PEG-PAsp(DET) are easily subjected to hydrolysis; therefore, they need to be prepared on site. In this study, using the biodegradable polycations as non-viral vectors, PAsp(DET) and PEG-PAsp(DET), we investigated the effects of L-leucine (Leu) on the polyplex. We prepared solutions and dry powders with and without Leu. Both dry powders had large and porous particles and Leu acted as a dispersing agent. The transfection activity of the sample solutions decreased within a month. However, the decrease in the transfection activity was partially suppressed by the dry powder with Leu at 5 and 25°C at 3 months. Furthermore, transfection experiments revealed that Leu exhibited a pDNA-stabilizing effect in the solution and dry powder. Similar results were observed for pDNA integrity, where a polyplex was formed in the dry powder. The results suggest that Leu is a candidate stabilizer to protect pDNA from degradation.

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Leucine enhances aerosol performance of Naringin dry powder and its activity on cystic fibrosis airway epithelial cells

Cited by 50 publications

References 43 publications

Development and Investigation of Dry Powder Inhalers for Cystic Fibrosis

Development and Investigation of Dry Powder Inhalers for Cystic Fibrosis

Budesonide dry powder for inhalation: effects of leucine and mannitol on the efficiency of delivery

Development of New Formulation Dry Powder for Pulmonary Delivery Using Amino Acids to Improve Stability

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