Polymer–Lipid Microparticles for Pulmonary Delivery

Eleftheriadis, Georgios K.; Akrivou, Melpomeni; Bouropoulos, Nikolaos; Tsibouklis, John; Vizirianakis, Ioannis S.; Fatouros, Dimitrios G.

doi:10.1021/acs.langmuir.7b03645

Cited by 12 publications

(2 citation statements)

References 52 publications

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“…The release of drugs was evaluated in PBS (pH 7.4) with the addition of 1% ( v/v ) Tween ® 80, resembling the lung lining fluid in terms of pH and the presence of surfactant [35,36]. The latter also enables the dissolution of RFB, which is sparingly soluble in aqueous media.…”

Section: Resultsmentioning

confidence: 99%

Inhalable Fucoidan Microparticles Combining Two Antitubercular Drugs with Potential Application in Pulmonary Tuberculosis Therapy

et al. 2018

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The pulmonary delivery of antitubercular drugs is a promising approach to treat lung tuberculosis. This strategy not only allows targeting the infected organ instantly, it can also reduce the systemic adverse effects of the antibiotics. In light of that, this work aimed at producing fucoidan-based inhalable microparticles that are able to associate a combination of two first-line antitubercular drugs in a single formulation. Fucoidan is a polysaccharide composed of chemical units that have been reported to be specifically recognised by alveolar macrophages (the hosts of Mycobacterium ). Inhalable fucoidan microparticles were successfully produced, effectively associating isoniazid (97%) and rifabutin (95%) simultaneously. Furthermore, the produced microparticles presented adequate aerodynamic properties for pulmonary delivery with potential to reach the respiratory zone, with a mass median aerodynamic diameter (MMAD) between 3.6–3.9 µm. The formulation evidenced no cytotoxic effects on lung epithelial cells (A549), although mild toxicity was observed on macrophage-differentiated THP-1 cells at the highest tested concentration (1 mg/mL). Fucoidan microparticles also exhibited a propensity to be captured by macrophages in a dose-dependent manner, as well as an ability to activate the target cells. Furthermore, drug-loaded microparticles effectively inhibited mycobacterial growth in vitro. Thus, the produced fucoidan microparticles are considered to hold potential as pulmonary delivery systems for the treatment of tuberculosis.

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Section: Resultsmentioning

confidence: 99%

Inhalable Fucoidan Microparticles Combining Two Antitubercular Drugs with Potential Application in Pulmonary Tuberculosis Therapy

et al. 2018

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“…Pulmonary delivery is a non-invasive route of administration with many benefits, such as a large lung surface area for absorption (100 m 2 ), elevated blood flow, rapid absorption, and avoidance of hepatic first-pass metabolism [ 1 , 2 ]. These benefits of pulmonary drug and vaccine delivery outweigh the challenges which include, most notably, mucociliary clearance, physiological barriers limiting deep lung deposition, formulation difficulties, and variability in inhaler use [ 2 ]. With respect to drugs, pulmonary delivery enhances the drug concentration locally and can potentially diminish systemic adverse effects [ 3 ].…”

Section: Introductionmentioning

confidence: 99%

Respiratory Tract Deposition and Distribution Pattern of Microparticles in Mice Using Different Pulmonary Delivery Techniques

2018

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Pulmonary delivery of drugs and vaccines is an established route of administration, with particulate-based carriers becoming an attractive strategy to enhance the benefits of pulmonary therapeutic delivery. Despite the increasing number of publications using the pulmonary route of delivery, the lack of effective and uniform administration techniques in preclinical models generally results in poor translational success. In this study, we used the IVIS Spectrum small-animal in vivo imaging system to compare the respiratory tract deposition and distribution pattern of a microsphere suspension (5 µm) in mice after 1, 4, and 24 h when delivered by oropharyngeal aspiration, the Microsprayer® Aerosolizer, and the BioLite Intubation System, three-widely reported preclinical inhalation techniques. We saw no significant differences in microsphere deposition in whole body images and excised lungs (at 1, 4, and 24 h); however, the three-dimensional (3D) images showed more localized deposition in the lungs with the MicroSprayer® and BioLite delivery techniques. Further, oropharyngeal aspiration (at 1 h) showed microsphere deposition in the oral cavity, in contrast to the MicroSprayer® and BioLite systems. The studies shown here will allow researchers to choose the appropriate pulmonary delivery method in animal models based on their study requirements.

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