Preparation of microsized spherical aggregates of ultrafine ciprofloxacin particles for dry powder inhalation (DPI)

Zhao, Hong; Le, Yuan; Liu, Haoying; Hu, Tingting; Shen, Zhigang; Yun, Jimmy; Chen, Jianfeng

doi:10.1016/j.powtec.2009.03.031

Cited by 25 publications

(13 citation statements)

References 18 publications

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“…[29][30][31][32][33] To the best of our knowledge, this is the only study demonstrating the use of agglomerated nanoparticles of theophylline as a dry powder for inhalers. Therefore, the aim of this study was to formulate self-assembled, theophylline nanoparticle agglomerates as a dry powder for inhalers.…”

Section: Introductionmentioning

confidence: 99%

Nanosized rods agglomerates as a new approach for formulation of a dry powder inhaler

Salem¹,

Abdelrahim²,

Eid³

et al. 2011

IJN

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Background: Nanosized dry powder inhalers provide higher stability for poorly water-soluble drugs as compared with liquid formulations. However, the respirable particles must have a diameter of 1–5 μm in order to deposit in the lungs. Controlled agglomeration of the nanoparticles increases their geometric particle size so they can deposit easily in the lungs. In the lungs, they fall apart to reform nanoparticles, thus enhancing the dissolution rate of the drugs. Theophylline is a bronchodilator with poor solubility in water. Methods: Nanosized theophylline colloids were formed using an amphiphilic surfactant and destabilized using dilute sodium chloride solutions to form the agglomerates. Results: The theophylline nanoparticles thus obtained had an average particle size of 290 nm and a zeta potential of −39.5 mV, whereas the agglomerates were 2.47 μm in size with a zeta potential of −28.9 mV. The release profile was found to follow first-order kinetics (r 2 > 0.96). The aerodynamic characteristics of the agglomerated nanoparticles were determined using a cascade impactor. The behavior of the agglomerate was significantly better than unprocessed raw theophylline powder. In addition, the nanoparticles and agglomerates resulted in a significant improvement in the dissolution of theophylline. Conclusion: The results obtained lend support to the hypothesis that controlled agglomeration strategies provide an efficient approach for the delivery of poorly water-soluble drugs into the lungs.

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Section: Introductionmentioning

confidence: 99%

Nanosized rods agglomerates as a new approach for formulation of a dry powder inhaler

Salem¹,

Abdelrahim²,

Eid³

et al. 2011

IJN

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show abstract

“…The scanning rates were 40°C/min a and 5°C/min b particle size decreased from the micron to the nano range as the VRSAs were changed from 1:1 to 1:5. This is explained by increase in local supersaturation ratio (S) and retardance in particle growth kinetics (36). Here, the local supersaturation is defined by the ratio of local drug concentration to the equilibrium solubility of drug in the mixture of solvent-antisolvent.…”

Section: Discussion and Future Studiesmentioning

confidence: 99%

Isoxyl Aerosols for Tuberculosis Treatment: Preparation and Characterization of Particles

Wang

Hickey

2010

AAPS PharmSciTech

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Abstract. Isoxyl is a potent antituberculosis drug effective in treating various multidrug-resistant strains in the absence of known side effects. Isoxyl has been used exclusively, but infrequently, via the oral route and has exhibited very poor and highly variable bioavailability due to its sparing solubility in water. These properties resulted in failure of some clinical trials and, consequently, isoxyl's use has been limited. Delivery of isoxyl to the lungs, a major site of Mycobacterium tuberculosis infection, is an attractive alternative route of administration that may rescue this abandoned drug for a disease that urgently requires new therapies. Particles for pulmonary delivery were prepared by antisolvent precipitation. Nanofibers with a width of 200 nm were obtained by injecting isoxyl solution in ethanol to water at a volume ratio of solvent to antisolvent of 1:5. Based on this preliminary result, a well-controlled method, involving nozzle mixing, was employed to prepare isoxyl particles. All the particles were 200 to 400 nm in width but had different lengths depending on properties of the solvents. However, generating these nanoparticles by simultaneous spray drying produced isoxyl microparticles (Feret's diameter, 1.19-1.77 μm) with no discernible nanoparticle substructure. The bulking agent, mannitol, helped to prevent these nanoparticles from agglomeration during process and resulted in nanoparticle aggregates in micron-sized superstructures. Future studies will focus on understanding difference of these isoxyl microparticles and nanoparticles/nanoparticle aggregates in terms of in vivo disposition and efficacy.

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“…The bioavailability of poor water-soluble hydrophobic drugs with high permeability through biomembrane can be increased by their dissolution rate in the gastrointestinal tract (Amidon et al, 1995). Common approaches to improve dissolution of poor water soluble drugs include application of cosolvents and lipids (Porter et al, 2007(Porter et al, , 2008Pole, 2008), complexing agents (Carrier et al, 2007;Brewster and Loftsson, 2007;Davis and Brewster, 2004), the formation of emulsions and solid dispersions (Fini et al, 2008;Kennedy et al, 2008;Tran et al, 2008;Lakshman et al, 2008), particle size reduction (Rabinow, 2004;Kesisoglou et al, 2007;Keck et al, 2007;Merskio-Liversidge and Liversidge, 2008) or lipid carriers (Tran et al, 2009;Simovic et al, 2009), or control of the API's polymorphic form (Crowley and Zografi, 2002;Schmidt et al, 2003;Strachan et al, 2004;Karjalainen et al, 2005;Masuda et al, 2006;Muster and Prestidge, 2002) Currently, considerable studies have been conducted to increase the dissolution of drugs by creating active pharmaceutical ingredients (API) nanoparticles (Wang et al, 2007;Zhao et al, 2009;Yang et al, 2008;Zhang and Shen, 2006) because formulation of nanoparticles can provide a way of sustained, controlled and targeted drug delivery to improve the therapeutic effect especially for waterinsoluble drug (Praetorius and Mandal, 2007;Medina et al, 2007;Zhang and Feng, 2006). However, the properties of nanoparticles always make them difficult to process into dry powders (Tam et al, 2008;Sepassi et al, 2007;…”

Section: Introductionmentioning

confidence: 99%

Formation of bicalutamide nanodispersion for dissolution rate enhancement

et al. 2011

International Journal of Pharmaceutics

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Preparation of microsized spherical aggregates of ultrafine ciprofloxacin particles for dry powder inhalation (DPI)

Cited by 25 publications

References 18 publications

Nanosized rods agglomerates as a new approach for formulation of a dry powder inhaler

Nanosized rods agglomerates as a new approach for formulation of a dry powder inhaler

Isoxyl Aerosols for Tuberculosis Treatment: Preparation and Characterization of Particles

Formation of bicalutamide nanodispersion for dissolution rate enhancement

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