Development of Budesonide Microparticles Using Spray-Drying Technology for Pulmonary Administration: Design, Characterization, In Vitro Evaluation, and In Vivo Efficacy Study

Naikwade, Sonali R.; Bajaj, Amrita; Gurav, Prashant; Gatne, M. M.; Soni, P.S.

doi:10.1208/s12249-009-9290-6

Cited by 48 publications

(26 citation statements)

References 79 publications

(77 reference statements)

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“…The bulk density was determined by pouring a known weight of powder under gravity into a calibrated measuring cylinder and the volume occupied by the powder was recorded. The tapped density of the same samples was subsequently determined using an automatic tapper for $500 times to displace the powder until no further change in the powder volume was observed (Naikwade et al, 2009). Measurements were performed in triplicate.…”

Section: Powder Density and Flowabilitymentioning

confidence: 99%

“…Therefore the development of budesonide for direct delivery to the lung could provide many advantages. Furthermore, inhaled glucocorticosteroids are recommended as the first-line therapy for asthma and as an inhaled drug it acts locally, and a relatively lower dose can be employed resulting in lower systemic side effects (Szefler, 1999;Naikwade et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

“…Several studies have attempted to improve the aerosolization properties of budesonide DPI such as by changing the budesonide particle to nanoporous microparticles (Nolan et al, 2009), agglomerated nanoparticles (El-Gendy et al, 2008), microspheres and porous particles (Naikwade et al, 2009) and ultra-fine particles by antisolvent precipitation (Hu et al, 2008) or mixing with other excipients such as L-leucine (Boraey et al, 2012). All of these studies have reported that the aerosolization properties of the modified dry powders can be improved when compared with untreated budesonide or spray dried budesonide alone.…”

Section: Introductionmentioning

confidence: 99%

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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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Section: Powder Density and Flowabilitymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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

Rattanupatam¹,

Srichana

2014

Drug Delivery

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“…Entrapment efficiency: [15] 10 mg of accurately weighed drugloaded polymeric nanoparticles were added to 100 ml of methanol. The resulting mixture was shaking for 24 hours on an orbital shaker incubator (Remi, RIS-24BL, and India).…”

Section: Evaluation Of Polymeric Nano-particlesmentioning

confidence: 99%

Exploring Polymeric Nano-Particles as Targeted Pulmonary Delivery of Rifampicin, Ethambutol and Ofloxacin against Inh-Resistant Tuberculosis

Patel¹

2017

JLPRR

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Present research focus on novel combination of Rifampicin, Ofloxacin and Ethambutol loaded polymeric nanoparticles for the effective eradication of isoniazid resistant species of Tuberculosis. The nanoparticles containing Rifampicin, Ethambutol and Ofloxacin were prepared by spray drying technique using biodegradable polymer PLGA through critical process as well as polymer attributes which were identified and screened using Plackett-Burman screening design. Partial least square equation generated using Minitab Software for processing parameters as flow rate-5ml/min, inlet temperature-60˚C, aspirator capacity-50, ultrasonication time 40 min, ultrasonic amplitude % 60, and product parameters like drug: polymer ratio 2:1, aerosil concentration 1%, Solvent (DCM: Ethanol) ratio 75:25 on critical responses i.e. particles size, encapsulation efficiency, and product yield. Diffusion study revealed that optimum formulation containing 2:1 drug to polymer ratio was able to sustain the release of drugs up to 12 hrs. Particles Size was found to be less than 100 nm with uniform spherical shape and good agreement using TEM analysis. The three drug combination showed significantly synergism (p 0.007) for isoniazid susceptible species during in-vitro antimicrobial assay prove better efficacy. Overall study explored potential use of polymeric particles as targeted delivery system for drug susceptible and isoniazid resistant tuberculosis treatment.

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“…Therefore, the process parameters in the spray-drying technique should be carefully controlled in order to avoid unwanted consequences such as particle aggregation, low yield, and high moisture content. Previous literatures have focused on the effect of process parameters during spray drying and/or spray congealing process (14)(15)(16)(17). Although NCs around 200 nm have been successfully prepared by spray drying (12,18,19), there is a knowledge gap on the systematic and statistical analysis of the effect of process parameters, specifically during spray drying of oily core NCs.…”

Section: Introductionmentioning

confidence: 99%

Analysis of Process Parameters Affecting Spray-Dried Oily Core Nanocapsules Using Factorial Design

Zhang

Youan

2010

AAPS PharmSciTech

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Abstract. The purpose of this work was to optimize the process parameters required for the production of spray-dried oily core nanocapsules (NCs) with targeted size and drug yield using a two-level fourfactor fractional factorial experimental design (FFED). The coded process parameters chosen were inlet temperature (X 1 ), feed flow rate (X 2 ), atomizing air flow (X 3 ), and aspiration rate (X 4 ). The produced NCs were characterized for size, yield, morphology, and powder flowability by dynamic light scattering, electron microscope, Carr's index, and Hausner ratio measurement, respectively. The mean size of produced NCs ranged from 129.5 to 444.8 nm, with yield varying from 14.1% to 31.1%. The statistical analysis indicated an adequate model fit in predicting the effect of process parameters affecting yield. Predicted condition for maximum yield was: inlet temperature 140°C, atomizing air flow 600 L/h, feed flow rate 0.18 L/h, and aspiration air flow set at 100%, which led to a yield of 30.8%. The morphological analysis showed the existence of oily core and spherical nanostructure. The results from powder flowability analysis indicated average Carr's index and Hausner ratio of 42.77% and 1.76, respectively. Spray-dried oily core NCs with size lower than 200 nm were successfully produced, and the FFED proved to be an effective approach in predicting the production of spray-dried NCs of targeted yield.

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Development of Budesonide Microparticles Using Spray-Drying Technology for Pulmonary Administration: Design, Characterization, In Vitro Evaluation, and In Vivo Efficacy Study

Cited by 48 publications

References 79 publications

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

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

Exploring Polymeric Nano-Particles as Targeted Pulmonary Delivery of Rifampicin, Ethambutol and Ofloxacin against Inh-Resistant Tuberculosis

Analysis of Process Parameters Affecting Spray-Dried Oily Core Nanocapsules Using Factorial Design

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