Application of a Four-fluid Nozzle Spray Drier to Prepare Inhalable Rifampicin-containing Mannitol Microparticles

Mizoe, Takuto; Ozeki, Tetsuya; Okada, Hiroaki

doi:10.1208/s12249-008-9109-x

Cited by 44 publications

(18 citation statements)

References 35 publications

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“…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. 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.…”

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

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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: Resultsmentioning

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 aerosolisation pattern of rifampicin was improved when microencapsulated with mannitol. However, intratracheal of the drug remained in the lung after 1 h) (Mizoe et al, 2008), indicating an efficacy below the desired level to attain a therapeutic effect. This result was rather predictable, as mannitol is very soluble in aqueous medium and even in the presence of a small quantity of medium, as that existing in the alveolar zone, rapid dissolution of the microparticle matrix is expected, releasing the drug and enabling its rapid elimination.…”

Section: Polyalcohol Microparticlesmentioning

confidence: 99%

“…Lung drug concentration was 10-times higher after direct lung delivery (Hwang et al, 2008) Mannitol Rifampicin Intratracheal Microparticles Drug elimination is very rapid, with only 4% of drug remaining in the lung 1h after administration (Mizoe et al, 2008) Alginate Chitosan…”

Section: Declaration Of Interestmentioning

confidence: 99%

Natural carriers for application in tuberculosis treatment

Costa

Grenha

2012

Journal of Microencapsulation

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“…38 Mizoe et al 39 successfully prepared respirable rifampin (RFP)-mannitol (MAN) microparticles using a four-fluidnozzle spray drier. They found that RFP-MAN microparticles were effective in pro-releasing RFP in the lungs.…”

Section: Inhalable Rifampin-containing Mannitol Microparticlesmentioning

confidence: 99%

“…However, further research on such DDSs that target alveolar macrophages for the sustained release of RFP and other drugs is required. 39 …”

Section: Inhalable Rifampin-containing Mannitol Microparticlesmentioning

confidence: 99%

Controlled-release approaches towards the chemotherapy of tuberculosis

Saifullah

Hussein

Ali³

2012

IJN

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Tuberculosis (TB), caused by the bacteria Mycobacterium tuberculosis, is notorious for its lethality to humans. Despite technological advances, the tubercle bacillus continues to threaten humans. According to the World Health Organization's 2011 global report on TB, 8.8 million cases of TB were reported in 2010, with a loss of 1.7 million human lives. As drugsusceptible TB requires long-term treatment of between 6 and 9 months, patient noncompliance remains the most important reason for treatment failure. For multidrug-resistant TB, patients must take second-line anti-TB drugs for 18-24 months and many adverse effects are associated with these drugs. Drug-delivery systems (DDSs) seem to be the most promising option for advancement in the treatment of TB. DDSs reduce the adverse effects of drugs and their dosing frequency as well as shorten the treatment period, and hence improve patient compliance. Further advantages of these systems are that they target the disease area, release the drugs in a sustained manner, and are biocompatible. In addition, targeted delivery systems may be useful in dealing with extensively drug-resistant TB because many side effects are associated with the drugs used to cure the disease. In this paper, we discuss the DDSs developed for the targeted and slow delivery of anti-TB drugs and their possible advantages and disadvantages.

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Application of a Four-fluid Nozzle Spray Drier to Prepare Inhalable Rifampicin-containing Mannitol Microparticles

Cited by 44 publications

References 35 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

Natural carriers for application in tuberculosis treatment

Controlled-release approaches towards the chemotherapy of tuberculosis

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