A Novel Inhalable Form of Rifapentine

Chan, John Gar Yan; Duke, Colin C.; Ong, Hui Xin; Chan, Jason C. K.; Tyne, Anneliese S.; Chan, Hak‐Kim; Britton, Warwick J.; Young, Paul M.; Traini, Daniela

doi:10.1002/jps.23911

Cited by 45 publications

(44 citation statements)

References 34 publications

(71 reference statements)

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“…In contrast, amorphous rifapentine was chemically unstable under ambient (60% RH) and dry (0% RH) conditions after storage for one month. 27 Therefore, Chan et al developed a novel inhalable powder formulation of rifapentine in crystalline form, which was stable for 3 months when stored in 60% RH. 27 We further advanced the production …”

Section: ■ Introductionmentioning

confidence: 99%

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Novel Inhaled Combination Powder Containing Amorphous Colistin and Crystalline Rifapentine with Enhanced Antimicrobial Activities against Planktonic Cells and Biofilm of Pseudomonas aeruginosa for Respiratory Infections

et al. 2014

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Colistin has been increasingly used for the treatment of respiratory infections caused by Gram-negative bacteria. Unfortunately parenteral administration of colistin can cause severe adverse effects. This study aimed to develop an inhaled combination dry powder formulation of colistin and rifapentine for the treatment of respiratory infections. The combination formulation was produced by spray-drying rifapentine particles suspended in an aqueous colistin solution. The combination dry powder had enhanced antimicrobial activities against planktonic cells and biofilm cultures of Pseudomonas aeruginosa, with both minimum inhibitory concentration (MIC) and minimum biofilm inhibitory concentration (MBIC) values (2 and 4 mg/L, respectively) being half that of pure colistin (MIC 4 mg/L and MBIC 8 mg/L) and 1/16th that of pure rifapentine (MIC 32 mg/L and MBIC 64 mg/L). High aerosol performance, as measured via an Aerolizer device, was observed with emitted doses>89% and fine particle fraction (FPF) total>76%. The proportion of submicron particles of rifapentine particles was minimized by the attachment of colistin, which increased the overall particle mass and aerodynamic size distribution. Using the spray-drying method described here, stable particles of amorphous colistin and crystalline rifapentine were distributed homogeneously in each stage of the impinger. Unlike the colistin alone formulation, no deterioration in aerosol performance was found for the combination powder when exposed to a high relative humidity of 75%. In our previous study, surface coating by rifampicin contributed to the moisture protection of colistin. Here, a novel approach with a new mechanism was proposed whereby moisture protection was attributed to the carrier effect of elongated crystalline rifapentine particles, which minimized contact between hygroscopic colistin particles. This inhaled combination antibiotic formulation with enhanced aerosol dispersion efficiency and in vitro efficacy could become a superior treatment for respiratory infections.

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Section: ■ Introductionmentioning

confidence: 99%

“…27 Therefore, Chan et al developed a novel inhalable powder formulation of rifapentine in crystalline form, which was stable for 3 months when stored in 60% RH. 27 We further advanced the production …”

Section: ■ Introductionmentioning

confidence: 99%

Novel Inhaled Combination Powder Containing Amorphous Colistin and Crystalline Rifapentine with Enhanced Antimicrobial Activities against Planktonic Cells and Biofilm of Pseudomonas aeruginosa for Respiratory Infections

et al. 2014

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“…These include drug delivery directly to the infected area, increasing local drug concentration which will impact in bacterial burden and reduce the systemic dosage of the drug [4][5][6][7][8][9][10][11][12][13]. Additionally, inhalable systems avoid unwanted side effects often caused by drug metabolism in the gastrointestinal tract before the drug reaches the systemic circulation [4][5][6][7][8][9][10][11][12][13]. Unlike the injectable route, inhalation is a pain free and self-administrable delivery means favoring patient convenience and compliance to the treatment.…”

Section: Advantages Of the Pulmonary Routementioning

confidence: 99%

Exploring inhalable polymeric dry powders for anti-tuberculosis drug delivery

Miranda

Rodrigues

Domingues

et al. 2018

Materials Science and Engineering: C

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The growing interest on polymeric delivery systems for pulmonary administration of drugs anticipates a more direct and efficient treatment of diseases such as tuberculosis (TB) that uses the pulmonary route as the natural route of infection. Polymeric microparticles or nano-in-microparticles offer target delivery of drugs to the lungs and the potential to control and sustain drug release within TB infected macrophages improving the efficiency of the anti-TB treatment and reducing side effects. In a dry powder form these inhalable delivery systems have increased stability and prolonged storage time without requiring refrigeration, besides being cost-effective and patient convenient. Thus, this review aims to compile the recent innovations of inhalable polymeric dry powder systems for the delivery of anti-TB drugs exploring the methods of production, aerodynamic characterization and the efficacy of targeted drug delivery systems using in vitro and in vivo models of the disease. Advanced knowledge and promising outcomes of these systems are anticipated to simplify and revolutionize the pulmonary drug delivery and to contribute towards more effective anti-TB treatments.

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“… 56 Particle engineering approaches are also employed to produce particles using different core materials and more recently of only pure drug. 57 …”

Section: Dry Powder Inhalersmentioning

confidence: 99%

Inhalation drug delivery devices: technology update

Ibrahim¹,

Verma²,

García-Contreras³

2015

MDER

118

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The pulmonary route of administration has proven to be effective in local and systemic delivery of miscellaneous drugs and biopharmaceuticals to treat pulmonary and non-pulmonary diseases. A successful pulmonary administration requires a harmonic interaction between the drug formulation, the inhaler device, and the patient. However, the biggest single problem that accounts for the lack of desired effect or adverse outcomes is the incorrect use of the device due to lack of training in how to use the device or how to coordinate actuation and aerosol inhalation. This review summarizes the structural and mechanical features of aerosol delivery devices with respect to mechanisms of aerosol generation, their use with different formulations, and their advantages and limitations. A technological update of the current state-of-the-art designs proposed to overcome current challenges of existing devices is also provided.

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A Novel Inhalable Form of Rifapentine

Cited by 45 publications

References 34 publications

Novel Inhaled Combination Powder Containing Amorphous Colistin and Crystalline Rifapentine with Enhanced Antimicrobial Activities against Planktonic Cells and Biofilm of Pseudomonas aeruginosa for Respiratory Infections

Novel Inhaled Combination Powder Containing Amorphous Colistin and Crystalline Rifapentine with Enhanced Antimicrobial Activities against Planktonic Cells and Biofilm of Pseudomonas aeruginosa for Respiratory Infections

Exploring inhalable polymeric dry powders for anti-tuberculosis drug delivery

Inhalation drug delivery devices: technology update

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