Micronization of Anti-Inflammatory Drugs for Pulmonary Delivery by a Controlled Crystallization Process

Rasenack, Norbert; Steckel, Hartwig; Müller, Bernd W.

doi:10.1002/jps.10274

Cited by 103 publications

(61 citation statements)

References 22 publications

(21 reference statements)

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…29,[40][41][42][43] However, many different techniques can be used to achieve this goal, such as using the nanoparticles, 44 using the micronized form of poorly water-soluble drugs 45,46 and even using four-fluid spray driers to prepare microparticles containing water-insoluble drugs. [47][48][49] In this study, the theophylline agglomerate was prepared at a respirable particle size (1-5 µm) using the solvent antisolvent technique.…”

Section: Resultsmentioning

confidence: 99%

“…[47][48][49] In this study, the theophylline agglomerate was prepared at a respirable particle size (1-5 µm) using the solvent antisolvent technique. 29,[45][46][47][48][49][50] First, the drug was dissolved with stearic acid in an organic solvent and then precipitated as nanoparticles by dropping this solution into an antisolvent. For a gglomeration, the addition of monovalent cations is a well known procedure resulting in the agglomeration of phospholipids, solid lipid nanoparticles, and nanosuspensions.…”

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

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

Salem¹,

Abdelrahim²,

Eid³

et al. 2011

IJN

View full text Add to dashboard Cite

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.

show abstract

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

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

Salem¹,

Abdelrahim²,

Eid³

et al. 2011

IJN

View full text Add to dashboard Cite

show abstract

“…168 This process involves antisolvent precipitation of drug solution in a water-miscible organic solvent, followed by addition of a bridging solvent, which is immiscible or partially miscible with water. Growth-retarding stabilizing additives, such as hydroxylpropylmethylcellulose (HPMC), is usually added in the medium to yield particles with small size.…”

Section: Antisolvent Precipitationmentioning

confidence: 99%

Nanomedicine in pulmonary delivery

Mansour¹,

Rhee²,

Wu³

2009

IJN

401

269

View full text Add to dashboard Cite

“…Direct controlled crystallization, for example, enables the production of uniform crystal drug particles with better physical stability due to a lower amorphous content compared to micronized material [42]. Through the use of an antisolvent precipitation technique with growth-retarding stabilizers like hydroxypropylmethylcellulose, characteristic particle morphologies depending on crystalline polymorphs can be achieved [47]. Elongated particles show improved lung delivery because the aerodynamic diameter of a fiber is mainly determined by its width rather than by its length [48].…”

Section: Engineered Particlesmentioning

confidence: 99%