Isoniazid-gelatin conjugate microparticles containing rifampicin for the treatment of tuberculosis

Manca, Maria Letizia; Cassano, Roberta; Valenti, Donatella; Trombino, Sonia; Ferrarelli, Teresa; Picci, Nevio; Fadda, Anna Maria; Manconi, Maria

doi:10.1111/jphp.12094

Cited by 44 publications

(11 citation statements)

References 37 publications

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“…Rawat et al reported that heparin-loaded PLGA microspheres produced by double emulsion techniques were within the inhalable size range, but both the entrapment efficiency (up to 55%) and half-life (up to 6-fold) were only increased by the addition of chemical additives (Rawat et al, 2008). Manca and co-workers also developed carriers for pulmonary administration of rifampicin based on gelatin (Manca et al, 2013) and polymer-coated liposomes (Manca et al, 2014), which displayed good aerodynamic properties and an efficient drug internalization by A540 cells.…”

Section: Introductionmentioning

confidence: 99%

Development of ciprofloxacin-loaded poly(vinyl alcohol) dry powder formulations for lung delivery

Silva

Paleco

Traini

et al. 2018

International Journal of Pharmaceutics

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Polymeric microparticles are micro carriers for the sustained drug delivery of drugs in the lungs, used as alternatives to the use of established excipients. This study aims to develop and characterize inhalable ciprofloxacin (CPx)-loaded poly(vinyl alcohol) (PVA) microparticles by a single-step spray-drying procedure. The optimization of the processing parameters was achieved by an orthogonal design of the most relevant processing parameters (polymer concentration, feed rate and inlet temperature). The obtained spray-dried particles showed a drug encapsulation efficiency higher than 90%. Furthermore, PVA-CPx formulations, with drug contents up to 10 wt%, showed a morphology and size suitable for inhalation, with a sustained release profile over 24 h. Data from Fourier transformed infra-red spectroscopy and differential scanning calorimetry indicated absence of interaction between the polymer matrix and the drug. Aerodynamic assessment of PVA-CPx 10 wt% was determined by the next generation impactor (NGI), using spray-dried CPx as a control. The results showed improved values of mass median aerodynamic diameter (5.06±0.10μm) and a fine particle fraction (39.78±0.98%) when comparing with the CPx alone (5.33±0.39μm and 30.43±1.38%). This study highlights the potential of spray-dried PVA microparticles as drug carriers for lung local delivery of antibiotics.

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Section: Introductionmentioning

confidence: 99%

Development of ciprofloxacin-loaded poly(vinyl alcohol) dry powder formulations for lung delivery

Silva

Paleco

Traini

et al. 2018

International Journal of Pharmaceutics

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“…For instance, antibiotics for inhalation can be packaged in synthetic nanoparticles or natural polymeric microparticles, such as gelatin. 120 In the future, nanotechnology may be used to target antibiotics to particular regions of the lung to allow drug delivery to specific sites of disease. One way of doing this is by delivering magnetic nanoparticles with the antibiotic solution.…”

Section: Inhaled Antibiotic Delivery Systems-innovationsmentioning

confidence: 99%

Inhaled Antibiotics in Cystic Fibrosis (CF) and Non-CF Bronchiectasis

Tay

Reid

Bell

2015

Semin Respir Crit Care Med

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Bronchiectasis is a pathological diagnosis describing dilatation of the airways and is characterized by chronic lung sepsis. Bronchiectasis has multiple etiologies, but is usually considered in terms of whether it is due to the genetic disorder cystic fibrosis (CF) or secondary to other causes (non-CF bronchiectasis, NCFB). Inhaled antibiotics are used in bronchiectasis to suppress bacterial pathogens and reduce long-term lung function decline. The majority of the literature on inhaled antibiotics comes from studies on CF where the dominant bacterial pathogen in the airway is usually Pseudomonas aeruginosa. Thus, most aerosolized antibiotic regimens target this bacterium, but the emergence of molecular diagnostic methods has questioned this approach and more tailored strategies may need to be considered in CF based on the community composition of the lung microbiome. Similarly, the lung microbiome in NCFB has been found to be a complex polymicrobial one and the current practice of employing the same inhaled antibiotic regimes as are used in CF may no longer be appropriate in many patients. In this article, the use of inhaled antibiotics in CF and NCFB is considered in the light of improved understanding of the lung microbiome and why more tailored therapy may be needed based on molecular identification of the microbial pathogens present. The evidence for the use of currently available inhaled antibiotics and advances in inhaled drug packaging and delivery devices are discussed. Finally, the urgent need for prospective randomized clinical trials in CF and NCFB is highlighted and areas for future research identified.

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“…While these have shown satisfactory in vitro performance and stability, the nebulized formulation still needs refinement of endotoxin levels to meet regulatory standards. Finally, Manca et al (198) developed a nebulized suspension of isoniazid-gelatin conjugate microparticles containing rifampicin, which reduced toxicity to A549 alveolar epithelial cells compared to a rifampicin solution. This demonstrated that the use of nebulized antibiotics for diseases not conventionally treated by nebulization.…”

Section: New Therapeuticsmentioning

confidence: 99%

Advances in Device and Formulation Technologies for Pulmonary Drug Delivery

et al. 2014

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Inhaled pharmaceuticals are formulated and delivered differently according to the therapeutic indication. However, specific device-formulation coupling is often fickle, and new medications or indications also demand new strategies. The discontinuation of chlorofluorocarbon propellants has seen replacement of older metered dose inhalers with dry powder inhaler formulations. High-dose dry powder inhalers are increasingly seen as an alternative dosage form for nebulised medications. In other cases, new medications have completely bypassed conventional inhalers and been formulated for use with unique inhalers such as the Staccato® device. Among these different devices, integration of software and electronic assistance has become a shared trend. This review covers recent device and formulation advances that are forming the current landscape of inhaled therapeutics.

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Isoniazid-gelatin conjugate microparticles containing rifampicin for the treatment of tuberculosis

Abstract: Overall, microparticles based on gelatin covalently bound to ISN and containing RFP showed a promising behaviour for pulmonary drug delivery.

Cited by 44 publications

References 37 publications

Development of ciprofloxacin-loaded poly(vinyl alcohol) dry powder formulations for lung delivery

Development of ciprofloxacin-loaded poly(vinyl alcohol) dry powder formulations for lung delivery

Inhaled Antibiotics in Cystic Fibrosis (CF) and Non-CF Bronchiectasis

Advances in Device and Formulation Technologies for Pulmonary Drug Delivery

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