Engineering of konjac glucomannan into respirable microparticles for delivery of antitubercular drugs

Guerreiro, Filipa; Swedrowska, Magda; Patel, Rajnikant; Flórez‐Fernández, Noelia; Torres, M.D.; Costa, Ana M. Rosa da; Forbes, Ben; Grenha, Ana

doi:10.1016/j.ijpharm.2021.120731

Cited by 25 publications

(12 citation statements)

References 40 publications

(52 reference statements)

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“…The development of drug carriers for inhaled medicine is challenging due to the required suitable physicochemical properties for deposition in the desired region of the lungs [46]. In the case of tuberculosis, the mycobacterium tuberculosis invades alveolar macrophages in the peripheral lung and multiplies inside these cells [38,47]. To target the alveolar macrophages harboring mycobacteria, particles of aerodynamic diameter in the range of 1 to 5 µm and geometric diameter of 1-3 µm were aimed to be synthesized.…”

Section: Optimization Of Formulation and Spray-drying Conditionsmentioning

confidence: 99%

“…The spray drying allows the engineering of microparticles with the desired physicochemical properties by optimizing processing parameters such as feed rate, atomizing air pressure, inlet and outlet air temperature, etc. [38]. The spray drying conditions were optimized in initial experiments and used as follows: inlet air temperature 120 • C, outlet temperature = 70 to 90 • C, solution feed rate = 2 mL/min and atomizing air pressure = 5.5 bar.…”

Section: Optimization Of Formulation and Spray-drying Conditionsmentioning

confidence: 99%

“…Spray drying allows the synthesis of microparticles with the desired physicochemical properties by optimizing processing parameters [38]. Spray drying is a simple, fast and one-step processing of microparticles synthesis for pulmonary delivery [39].…”

Section: Introductionmentioning

confidence: 99%

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Polymeric Microparticles: Synthesis, Characterization and In Vitro Evaluation for Pulmonary Delivery of Rifampicin

et al. 2022

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Rifampicin, a potent broad-spectrum antibiotic, remains the backbone of anti-tubercular therapy. However, it can cause severe hepatotoxicity when given orally. To overcome the limitations of the current oral therapy, this study designed inhalable spray-dried, rifampicin-loaded microparticles using aloe vera powder as an immune modulator, with varying concentrations of alginate and L-leucine. The microparticles were assessed for their physicochemical properties, in vitro drug release and aerodynamic behavior. The spray-dried powders were 2 to 4 µm in size with a percentage yield of 45 to 65%. The particles were nearly spherical with the tendency of agglomeration as depicted from Carr’s index (37 to 65) and Hausner’s ratios (>1.50). The drug content ranged from 0.24 to 0.39 mg/mg, with an association efficiency of 39.28 to 96.15%. The dissolution data depicts that the in vitro release of rifampicin from microparticles was significantly retarded with a higher L-leucine concentration in comparison to those formulations containing a higher sodium alginate concentration due to its hydrophobic nature. The aerodynamic data depicts that 60 to 70% of the aerosol mass was emitted from an inhaler with MMAD values of 1.44 to 1.60 µm and FPF of 43.22 to 55.70%. The higher FPF values with retarded in vitro release could allow sufficient time for the phagocytosis of synthesized microparticles by alveolar macrophages, thereby leading to the eradication of M. tuberculosis from these cells.

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Section: Optimization Of Formulation and Spray-drying Conditionsmentioning

confidence: 99%

Section: Optimization Of Formulation and Spray-drying Conditionsmentioning

confidence: 99%

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Polymeric Microparticles: Synthesis, Characterization and In Vitro Evaluation for Pulmonary Delivery of Rifampicin

et al. 2022

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“…Interestingly, recent studies have raised the potential of GMs for targeting nanocarriers to specific receptors, namely the mannose receptors on the cell surface. The presence of mannose on the particle surface increases the uptake of mannose receptors by M cells and macrophages (Guerreiro et al, 2021). Several GM modifications as shown in Table 2 are useful for expanding GM applications, such as:…”

Section: Application Of Glucomannanmentioning

confidence: 99%

“…The results showed that the microparticles consisting only of KGM displayed the most suitable characteristics compared to other spray drying excipients such as mannitol. The drugs isoniazid and rifabutin are mostly associated with microparticles of biocompatible GM (88-104% efficiency) and the obtained microparticles have an aerodynamic diameter of about 3 µm which allows deeper lung penetration (Guerreiro et al, 2021;Wardhani et al, 2020).…”

Section: Glucomannan-based Microparticlesmentioning

confidence: 99%

Modifications and Pharmaceutical Applications of Glucomannan as Novel Pharmaceutical Excipient in Indonesia: Review Article

Aanisah

Wardhana²,

Chaerunisaa³

2022

J. Pharm. Sci. Clin. Res.

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<p>Currently, Indonesia is excessively dependent on imported raw materials, such as pharmaceutical excipients. In this regard, the current pandemic should remind the critical nature of independence in purchasing raw resources to cope with future dynamics. One of the causes of dependence is the lack of raw materials management, specifically from biological sources abundantly available. A significant advantage is directed towards natural excipients because large quantities of more affordable plants ensure sustained availability in nature. Therefore, this study highlighted the possibility of using excipients derived from natural resources that are commonly used yet underutilized in Indonesia, such as glucomannan (GM). Indonesia has the potential to produce GM, considering the high natural resources as its source. However, it has not been applied extensively in pharmaceutical preparations due to diverse uses in several countries' drug, food, and cosmetic industries. This study aimed to discuss the modifications of GM and their use as pharmaceutical excipients with better physical properties. Additionally, the potential of melinjo seeds that have not been widely used was also analyzed. Melinjo seeds can be used as a source of GM due to their fairly large polysaccharide of about 64.11%. This issue will promote national autonomy in developing novel pharmaceutical excipients derived from natural resources that are highly economical and innovative.</p>

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Konjac glucomannan: A functional biopolymer for multifaceted drug delivery applications

Kulkarni,

Agnihotri,

Bhinge

et al. 2024

Polymers for Advanced Techs

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Konjac glucomannan (KGM) is a hydrophilic, neutral polysaccharide obtained from the corm of Amorphophallus konjac (Araceae). Excellent biodegradability, biocompatibility, and nontoxicity has marked the utilization of KGM in variety of drug delivery and biomedical applications. KGM has generally regarded as safe (GRAS) status approved by the United States Food and Drug Administration. The gelling, and film‐forming properties possessed by native KGM has attracted a widespread attention of the researchers for exploring its drug delivery potential. Additionally, the versatility of KGM modifications further extends the drug delivery opportunities through ever‐increasing array of functional properties of KGM. Present review is aimed at presenting the state‐of‐the‐art collection of structure, functional properties, biosynthesis, in vitro and in vivo degradation, chemical modifications, and finally, the drug delivery applications of the KGM. Authors tried to cover the aspects of the KGM relevant to the formulation personnel, and academicians involved in the investigation on variety of pharmaceutical, biotechnological, and biomedical applications of KGM. This article may encourage the investigators to explore the use of KGM, owing to its beneficial traits, as pharmaceutical excipient for drug delivery applications.

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Engineering of konjac glucomannan into respirable microparticles for delivery of antitubercular drugs

Cited by 25 publications

References 40 publications

Polymeric Microparticles: Synthesis, Characterization and In Vitro Evaluation for Pulmonary Delivery of Rifampicin

Polymeric Microparticles: Synthesis, Characterization and In Vitro Evaluation for Pulmonary Delivery of Rifampicin

Modifications and Pharmaceutical Applications of Glucomannan as Novel Pharmaceutical Excipient in Indonesia: Review Article

Konjac glucomannan: A functional biopolymer for multifaceted drug delivery applications

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