Development of Liposomal Ciprofloxacin to Treat Lung Infections

Cipolla, David; Blanchard, Jim; Gonda, Igor

doi:10.3390/pharmaceutics8010006

Cited by 149 publications

(148 citation statements)

References 64 publications

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“…For some drugs with high water solubility and fast systemic absorption such as ciprofloxacin HCl, there may be a need to develop controlled released formulations to achieve high local drug concentrations for longer time (63). However, for poorly water soluble drugs, there is a need to improve the dissolution and maintain drug concentrations in the lung lining fluid above minimum inhibitory concentrations (16,64,65), particularly for azithromycin which has to enter the bacterial cells to be effective (34).…”

Section: Discussionmentioning

confidence: 99%

Physico-Chemical Properties, Aerosolization and Dissolution of Co-Spray Dried Azithromycin Particles with L-Leucine for Inhalation

Mangal

Nie

et al. 2018

Pharm Res

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Purpose Inhalation therapy is popular to treat lower respiratory tract infections. Azithromycin is effective against some bacteria that cause respiratory tract infections; but it has poor water solubility that may limit its efficacy when administrated as inhalation therapy. In this study, dry powder inhaler formulations were developed by co-spray drying azithromycin with L-leucine with a purpose to improve dissolution. Methods The produced powder formulations were characterized regarding particle size, morphology, surface composition and in-vitro aerosolization performance. Effects of L-leucine on the solubility and in-vitro dissolution of azithromycin were also evaluated. Results The spray dried azithromycin alone formulation exhibited a satisfactory aerosol performance with a fine particle fraction (FPF) of 62.5 ± 4.1%. Addition of L-leucine in the formulation resulted in no significant change in particle morphology and FPF, which can be attributed to enrichment of azithromycin on the surfaces of composite particles. Importantly, compared with the spray-dried amorphous azithromycin alone powder, the co-spray dried powder formulations of azithromycin and L-leucine demonstrated a substantially enhanced in-vitro dissolution rate. Such enhanced dissolution of azithromycin could be attributed to the formation of composite system and the acidic microenvironment around azithromycin molecules created by the dissolution of acidic L-leucine in the co-spray dried powder. Fourier transform infrared spectroscopic data showed intermolecular interactions between azithromycin and L-leucine in the co-spray dried formulations. Conclusions We developed the dry powder formulations with satisfactory aerosol performance and enhanced dissolution for a poorly water soluble weak base, azithromycin, by co-spray drying with an amino acid, L-leucine.

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Section: Discussionmentioning

confidence: 99%

Physico-Chemical Properties, Aerosolization and Dissolution of Co-Spray Dried Azithromycin Particles with L-Leucine for Inhalation

Mangal

Nie

et al. 2018

Pharm Res

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“…Nevertheless, several formulations are currently in preclinical studies and clinical trials, and some are commercially available 139 . For example, liposomal ciprofloxacin and amikacin have shown promise in the management of chronic lung infection in cystic fibrosis 140,141 . The potential of liposomes to function as delivery agents for other antimicrobials, such as NO, has demonstrated significantly reduced S. aureus biofilm mass compared to controls in a sheep model of chronic rhinosinusitis 142 .…”

Section: The Promise Of New Technologiesmentioning

confidence: 99%

Targeting microbial biofilms: current and prospective therapeutic strategies

et al. 2017

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Biofilm formation is a key virulence factor for a wide range of microorganisms that cause chronic infections. The multifactorial nature of biofilm development and drug tolerance imposes great challenges for the use of conventional antimicrobials, and indicates the need for multi-targeted or combinatorial therapies. In this review, we focus on current therapeutic strategies and those that are under development that target vital structural and functional traits of microbial biofilms and drug tolerance mechanisms, including the extracellular matrix and dormant cells. We emphasize strategies that are supported by in vivo or ex vivo studies, highlight emerging biofilm-targeting technologies, and provide a rationale for multi-targeted therapies that are aimed at disrupting the complex biofilm microenvironment.

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“…This form of ciprofloxacin is delivered using a PARI LC Sprint ® nebulizer and PARI TurboBoy-S ® compressor [21,67]. A phase 2 study of 36 patients with NCFB explored the effects of once a day inhaled liposomal ciprofloxacin at two different doses for 28 days [105].…”

Section: Non-cystic Fibrosis Bronchiectasismentioning

confidence: 99%

Inhaled Antibiotic Therapy in Chronic Respiratory Diseases

Maselli

Keyt

Restrepo

2017

IJMS

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The management of patients with chronic respiratory diseases affected by difficult to treat infections has become a challenge in clinical practice. Conditions such as cystic fibrosis (CF) and non-CF bronchiectasis require extensive treatment strategies to deal with multidrug resistant pathogens that include Pseudomonas aeruginosa, Methicillin-resistant Staphylococcus aureus, Burkholderia species and non-tuberculous Mycobacteria (NTM). These challenges prompted scientists to deliver antimicrobial agents through the pulmonary system by using inhaled, aerosolized or nebulized antibiotics. Subsequent research advances focused on the development of antibiotic agents able to achieve high tissue concentrations capable of reducing the bacterial load of difficult-to-treat organisms in hosts with chronic respiratory conditions. In this review, we focus on the evidence regarding the use of antibiotic therapies administered through the respiratory system via inhalation, nebulization or aerosolization, specifically in patients with chronic respiratory diseases that include CF, non-CF bronchiectasis and NTM. However, further research is required to address the potential benefits, mechanisms of action and applications of inhaled antibiotics for the management of difficult-to-treat infections in patients with chronic respiratory diseases.

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Development of Liposomal Ciprofloxacin to Treat Lung Infections

Cited by 149 publications

References 64 publications

Physico-Chemical Properties, Aerosolization and Dissolution of Co-Spray Dried Azithromycin Particles with L-Leucine for Inhalation

Physico-Chemical Properties, Aerosolization and Dissolution of Co-Spray Dried Azithromycin Particles with L-Leucine for Inhalation

Targeting microbial biofilms: current and prospective therapeutic strategies

Inhaled Antibiotic Therapy in Chronic Respiratory Diseases

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