Sustained release of isoniazid from polylactide microspheres prepared using solid/oil drug loading method for tuberculosis treatment

Zhang, Limei; Liu, Ying; Zhang, Yun; Zhu, Chunyan

doi:10.1007/s11427-016-5051-4

Cited by 11 publications

(2 citation statements)

References 26 publications

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“…This approach of associating antitubercular drugs in a single formulation meets the recommendations of the WHO regarding the need to establish a combined therapy for TB [12]. The selected theoretical drug loadings (8.7% for INH and 4.4% for RFB) are similar to those reported in other works [18]. INH is present in a higher amount than RFB, because the latter is a more potent drug [19], and also has a more toxic profile, as demonstrated in Section 3.4.…”

Section: Resultssupporting

confidence: 70%

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: Resultssupporting

confidence: 70%

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

et al. 2018

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“…More modern models take into account changes in the diffusion coefficients of the dopants due to plasticization of the polymer matrix as a result of swelling in water or due to a decrease in molecular weight during hydrolysis (see, for example, [26,29]). Models that take into account diffusion in pores formed in polymer matrices seem to be more correct [30,31]. However, the available physicochemical models are primarily based not only on experimental data but also on speculative assumptions not supported by experiments.…”

Section: Introductionmentioning

confidence: 99%

New Insight into the Mechanism of Drug Release from Poly(d,l-lactide) Film by Electron Paramagnetic Resonance

et al. 2020

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A novel approach based on convolution of the electron paramagnetic resonance (EPR) spectra was used for quantitative study of the release kinetics of paramagnetic dopants from poly(d,l-lactide) films. A non-monotonic dependence of the release rate on time was reliably recorded. The release regularities were compared with the dynamics of polymer structure changes determined by EPR, SEM, and optic microscopy. The data obtained allow for the conclusion that the main factor governing dopant release is the formation of pores connected with the surface. In contrast, the contribution of the dopant diffusion through the polymer matrix is negligible. The dopant release can be divided into two phases: release through surface pores, which are partially closed with time, and release through pores initially formed inside the polymer matrix due to autocatalytic hydrolysis of the polymer and gradually connected to the surface of the sample. For some time, these processes co-occur. The mathematical model of the release kinetics based on pore formation is presented, describing the kinetics of release of various dopants from the polymer films of different thicknesses.

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Microparticles, Microspheres, and Microemulsions as Pulmonary Drug Delivery Systems for the Treatment of Respiratory Diseases

Padhi

Hassan

Jain

et al. 2022

Advanced Drug Delivery Strategies for Targeting Chronic Inflammatory Lung Diseases

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Sustained release of isoniazid from polylactide microspheres prepared using solid/oil drug loading method for tuberculosis treatment

Cited by 11 publications

References 26 publications

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

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

New Insight into the Mechanism of Drug Release from Poly(d,l-lactide) Film by Electron Paramagnetic Resonance

Microparticles, Microspheres, and Microemulsions as Pulmonary Drug Delivery Systems for the Treatment of Respiratory Diseases

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