Spray-drying of konjac glucomannan to produce microparticles for an application as antitubercular drug carriers

Guerreiro, Filipa; Pontes, Jorge F.; Costa, Ana M. Rosa da; Grenha, Ana

doi:10.1016/j.powtec.2018.09.068

Cited by 33 publications

(15 citation statements)

References 37 publications

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“…This has been explored as a method of sustained insulin release, following pulmonary delivery [86]. Other naturally occurring carbohydrate polymers have also been proposed as respirable microparticle drug carriers such as konjac glucomannan which is biodegradable by β-mannosidase [87] and chitosan degradation which is biodegradable by lysozyme [88].…”

Section: Metabolism Of Biologic Drugs and Excipientsmentioning

confidence: 99%

Drug metabolism in the lungs: opportunities for optimising inhaled medicines

Enlo-Scott

Bäckström

Mudway

et al. 2021

Expert Opinion on Drug Metabolism & Toxicology

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Introduction:The lungs possess many xenobiotic metabolizing enzymes which influence the pharmacokinetics and safety of inhaled medicines. Anticipating metabolism in the lungs provides an opportunity to optimize new inhaled medicines and overcome challenges in their development.Areas covered: This article summarizes current knowledge on xenobiotic metabolizing enzymes in the lungs. The impact of metabolism on inhaled medicines is considered with examples of how this impacts small molecules, biologics and macromolecular formulation excipients. Methods for measuring and predicting xenobiotic lung metabolism are critically reviewed and the potential for metabolism to influence inhalation toxicology is acknowledged. Expert opinion: Drugs can be optimized by molecular modification to (i) reduce systemic exposure using a 'soft drug' approach, (ii) improve bioavailability by resisting metabolism, or (iii) use a prodrug approach to overcome pharmacokinetic limitations. Drugs that are very labile in the lungs may require a protective formulation. Some drug carriers being investigated for PK-modification rely on lung enzymes to trigger drug release or biodegrade. Lung enzyme activity varies with age, race, smoking status, diet, drug exposure and preexisting lung disease. New experimental technologies to study lung metabolism include tissue engineered models, improved analytical capability and in silico models.

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Section: Metabolism Of Biologic Drugs and Excipientsmentioning

confidence: 99%

Drug metabolism in the lungs: opportunities for optimising inhaled medicines

Enlo-Scott

Bäckström

Mudway

et al. 2021

Expert Opinion on Drug Metabolism & Toxicology

View full text Add to dashboard Cite

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“…Very frequently, the developed carriers involve strategies of surface chemical functionalization, namely mannosylation. The rationale behind this approach is based on the fact that bacterial hosts, the macrophages, have several surface receptors that are likely to be used as therapeutic targets [70,71]. The mannose receptor is one of the main, which may provide a favorable interaction with some units and chemical groups present on the carriers' surface, including the mannose units, but also others like fucose and N-acetylglucosamine [72].…”

Section: Delivery Of Antibioticsmentioning

confidence: 99%

Multifunctional Nanocarriers for Lung Drug Delivery

Pontes

Grenha

2020

Nanomaterials

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Nanocarriers have been increasingly proposed for lung drug delivery applications. The strategy of combining the intrinsic and more general advantages of the nanostructures with specificities that improve the therapeutic outcomes of particular clinical situations is frequent. These include the surface engineering of the carriers by means of altering the material structure (i.e., chemical modifications), the addition of specific ligands so that predefined targets are reached, or even the tuning of the carrier properties to respond to specific stimuli. The devised strategies are mainly directed at three distinct areas of lung drug delivery, encompassing the delivery of proteins and protein-based materials, either for local or systemic application, the delivery of antibiotics, and the delivery of anticancer drugs—the latter two comprising local delivery approaches. This review addresses the applications of nanocarriers aimed at lung drug delivery of active biological and pharmaceutical ingredients, focusing with particular interest on nanocarriers that exhibit multifunctional properties. A final section addresses the expectations regarding the future use of nanocarriers in the area.

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“…Moreover, the obtained carriers showed limited solubility under acidic conditions and enzymatic degradation, which allows them to be used in the acidic environment, such as the human stomach [ 26 ]. Moreover, the konjac glucomannan microparticles containing two drugs, isoniazid (INH) and rifabutin (RFB), were developed to antitubercular therapy for the pulmonary delivery system [ 27 ]. The PLGA microparticles incorporated with rosmarinic acid had antioxidant and antibacterial activity.…”

Section: Introductionmentioning

confidence: 99%

Freeze-Dried Matrices Composed of Degradable Polymers with Surfactant-Loaded Microparticles Based on Pectin and Sodium Alginate

Stachowiak

Kowalonek

2021

Materials

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Gelatin/polyvinylpyrrolidone/hydroxyethyl cellulose/glycerol porous matrices with microspheres made of sodium alginate or pectin and sodium alginate were produced. A surfactant was loaded into these microparticles. The microspheres were characterized using optical microscopy, scanning electron microscopy SEM, and laser diffraction particle size analyzer. For the matrices, the density, porosity, swelling capacity, dissolution in phosphate saline buffer were determined and SEM, mechanical, and thermogravimetric studies were applied. The results showed that the size of the two-component microspheres was slightly larger than that of single-ingredient microparticles. The images confirmed the spherical shape of the microparticles. The prepared matrices had high water uptake ability and porosity due to the presence of hydrophilic polymers. The presence of microparticles in the matrices caused a decrease in these parameters. Degradation of the composites with the microspheres was significantly faster than the matrix without them. The addition of microparticles increased the stiffness and toughness of the prepared materials. The efficiency of the thermal decomposition main stage was reduced in the samples with microspheres, whereas a char residue increased in these composites.

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Spray-drying of konjac glucomannan to produce microparticles for an application as antitubercular drug carriers

Cited by 33 publications

References 37 publications

Drug metabolism in the lungs: opportunities for optimising inhaled medicines

Drug metabolism in the lungs: opportunities for optimising inhaled medicines

Multifunctional Nanocarriers for Lung Drug Delivery

Freeze-Dried Matrices Composed of Degradable Polymers with Surfactant-Loaded Microparticles Based on Pectin and Sodium Alginate

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