Spray dried inhalable ciprofloxacin powder with improved aerosolisation and antimicrobial activity

Osman, Rihab; Kan, Pei; Awad, Gehanne A.S.; Mortada, Nahed D.; EL-Shamy, Abd-Elhameed; Alpar, Oya

doi:10.1016/j.ijpharm.2013.04.009

Cited by 61 publications

(39 citation statements)

References 46 publications

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“…LVX-loaded MS (10 ± 1mg) were submitted to an extraction process with 20 mL of 0.1M hydrochloric acid [36] for 3 h at room temperature, under magnetic stirring (300 rpm) and protected from light. An aliquot (1 mL) of each suspension was collected and centrifuged at 3500 rpm for 5 min (Hettich ® Zentrifugen Universal 320R, Germany).…”

Section: -Drug Loading and Entrapment Efficiencymentioning

confidence: 99%

Optimization of levofloxacin-loaded crosslinked chitosan microspheres for inhaled aerosol therapy

Gaspar

Sousa

Pais

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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The aim of this work was the development of innovative levofloxacin-loaded swellable microspheres (MS) for the dry aerosol therapy of pulmonary chronic Pseudomonas aeruginosa infections in Cystic Fibrosis patients. In a first step, a factorial design was applied to optimize formulations of chitosan-based MS with glutaraldehyde as crosslinker. After optimization, other crosslinkers (genipin, glutaric acid and glyceraldehyde) were tested. Analyses of MS included aerodynamic and swelling properties, morphology, drug loading, thermal and chemical characteristics, in vitro antibacterial activity and drug release studies. The prepared MS presented a drug content ranging from 39.8 to 50.8 % of levofloxacin in an amorphous or dispersed state, antibacterial activity and fast release profiles. The highest degree of swelling was obtained for MS crosslinked with glutaric acid and genipin. These formulations also presented satisfactory aerodynamic properties, making them a promising alternative, in dry-powder inhalers, to levofloxacin solution for inhalation.3

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Section: -Drug Loading and Entrapment Efficiencymentioning

confidence: 99%

Optimization of levofloxacin-loaded crosslinked chitosan microspheres for inhaled aerosol therapy

Gaspar

Sousa

Pais

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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“…Previous research has demonstrated that a high content of dispersibility enhancers and carriers is required to increase effectively the aerodynamics of drugs delivered as powder aerosols [4,55,56]. The present study shows that increasing polymer concentration beyond 20% did not give any significant improvement in dispersibility, and hence formulations containing 20% octanoyl chitosan would be favourable for use, incorporating the maximum amount of antibiotic for delivery of a high localized dose of levofloxacin.…”

Section: In-vitro Aerosol Propertiesmentioning

confidence: 50%

Engineering hydrophobically modified chitosan for enhancing the dispersion of respirable microparticles of levofloxacin

Merchant

Taylor

Stapleton

et al. 2014

European Journal of Pharmaceutics and Biopharmaceutics

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a b s t r a c tThe potential of amphiphilic chitosan formed by grafting octanoyl chains on the chitosan backbone for pulmonary delivery of levofloxacin has been studied. The success of polymer synthesis was confirmed using FT-IR and NMR, whilst antimicrobial activity was assessed against Pseudomonas aeruginosa. Highly dispersible dry powders for delivery as aerosols were prepared with different amounts of chitosan and octanoyl chitosan to study the effect of hydrophobic modification and varying concentration of polymer on aerosolization of drug. Powders were prepared by spray-drying from an aqueous solution containing levofloxacin and chitosan/amphiphilic octanoyl chitosan. L-leucine was also used to assess its effect on aerosolization. Following spray-drying, the resultant powders were characterized using scanning electron microscopy, laser diffraction, dynamic light scattering, HPLC, differential scanning calorimetry, thermogravimetric analysis and X-ray powder diffraction. The in vitro aerosolization profile was determined using a Next Generation Impactor, whilst in vitro antimicrobial assessment was performed using MIC assay. Microparticles of chitosan have the property of mucoadhesion leading to potential increased residence time in the pulmonary mucus, making it important to test the toxicity of these formulations. In-vitro cytotoxicity evaluation using MTT assay was performed on A549 cell line to determine the toxicity of formulations and hence feasibility of use. The MTT assay confirmed that the polymers and the formulations were non-cytotoxic. Hydrophobically modifying chitosan showed significantly lower MIC (4-fold) than the commercial chitosan against P. aeruginosa. The powders generated were of suitable aerodynamic size for inhalation having a mass median aerodynamic diameter less than 4.5 lm for formulations containing octanoyl chitosan. These highly dispersible powders have minimal moisture adsorption and hence an emitted dose of more than 90% and a fine particle fraction (FPF) of 52%. Powders with non-modified chitosan showed lower dispersibility, with an emitted dose of 72% and FPF of 20%, as a result of high moisture adsorption onto the chitosan matrix leading to cohesiveness and subsequently decreased dispersibility.

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“…In accordance with this, after preclinical studies Bend research Inc. proposed dextran as a suitable DPI excipient [25]. Osman et al made use of chitosan to impart mucoadhesive properties to inhaled dextran sulfate microparticles [26]. Hydrophilic polymers are however recognized as poor drug carriers due to their burst release properties.…”

Section: Introductionmentioning

confidence: 95%

Cationic, amphiphilic dextran nanomicellar clusters as an excipient for dry powder inhaler formulation

Vadakkan

Raj

et al. 2015

Acta Biomaterialia

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Spray dried inhalable ciprofloxacin powder with improved aerosolisation and antimicrobial activity

Cited by 61 publications

References 46 publications

Optimization of levofloxacin-loaded crosslinked chitosan microspheres for inhaled aerosol therapy

Optimization of levofloxacin-loaded crosslinked chitosan microspheres for inhaled aerosol therapy

Engineering hydrophobically modified chitosan for enhancing the dispersion of respirable microparticles of levofloxacin

Cationic, amphiphilic dextran nanomicellar clusters as an excipient for dry powder inhaler formulation

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