Pulmonary delivery of rifampicin microspheres using lower generation polyamidoamine dendrimers as a carrier

Rajabnezhad, Saeid; Casettari, Luca; Lam, Jenny K.W.; Nomani, Alireza; Torkamani, Mohammad Reza; Palmieri, Gianni; Rajabnejad, Mohammad Reza; Darbandi, Mohammad Ali

doi:10.1016/j.powtec.2015.12.037

Cited by 39 publications

(13 citation statements)

References 53 publications

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“…It is a hydrophobic drug in the form of reddish brown/orange crystalline powder, slightly soluble in ethanol, methanol, and acetonitrile. Its solubility in water is low and may vary according to the pH of the medium because of its amphoteric nature, reaching its maximum in acidic conditions in the pH range between 1 and 2. − …”

Section: Introdutionmentioning

confidence: 99%

“…The drug has greater stability around pH 6, close to neutrality. Under stomach conditions, the azomethine (−NCH) bond present in the structure of the molecule undergoes rapid hydrophilic cleavage leading to the formation of 3-formyl rifamycin SV (3-FRSV), a low permeability product. ,, Therefore, it is necessary to administer high doses throughout the day, about 10 mg/kg, to achieve the desired therapeutic efficacy. ,, …”

Section: Introdutionmentioning

confidence: 99%

“…For chronic diseases such as TB, high relative doses of the drug are required to maintain therapeutic concentrations for longer periods for the required treatment time. Thus, the administration of RIF can lead to the triggering of potentially toxic side effects, including hepatitis, anorexia, rash, flu syndrome, and renal failure. ,,, In addition, because RIF is usually given in combination with other antibiotics, its toxicity may increase because of drug interactions …”

Section: Introdutionmentioning

confidence: 99%

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Obtaining and Applying Nanohybrid Palygorskite-Rifampicin in the pH-Responsive Release of the Tuberculostatic Drug

et al. 2020

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Despite having good efficacy in the treatment and prevention of tuberculosis, the administration of rifampicin (RIF) can cause serious side effects, resulting from the prolonged use of this substance. Thus, it is necessary to seek new systems for administering tuberculostatic drugs, to avoid unwanted adverse effects, increase their bioavailability and, consequently, improve their therapeutic efficacy. The present work describes the achievement of a pH-responsive system for RIF, using palygorskite, a fibrous clay mineral, as a nanocarrier. To evaluate the influence of some operational variables on the drug adsorption process, a 2 4 factorial experimental design was used. The experiment using a maximum concentration (0.125 mg/mL), lower mass of PAL (300 mg), and lower pH (pH 2) was more efficient compared to other experiments, resulting in a higher dose of the incorporated drug, equivalent to 33.62 mg/g. To elucidate the mechanism of interaction between the materials, the hybrid obtained was characterized by different characterization techniques (Fourier transform infrared spectroscopy, X-ray diffraction, thermogravimetry/derived thermogravimetry, zeta potential, scanning electron microscopy, and dispersive energy spectroscopy). In addition, kinetic models and adsorption isotherms were applied to the experimental data. Through in vitro release studies, it was possible to verify the effectiveness of the pH-dependent system obtained. The adjustment of experimental release data to the theoretical model of Higuchi indicated that the release of rifampicin occurs in a prolonged way from the palygorskite.

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Section: Introdutionmentioning

confidence: 99%

Section: Introdutionmentioning

confidence: 99%

Section: Introdutionmentioning

confidence: 99%

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Obtaining and Applying Nanohybrid Palygorskite-Rifampicin in the pH-Responsive Release of the Tuberculostatic Drug

et al. 2020

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“…For example, a previous in vitro study by Bellini et al ( 88 ) reported that fourth-generation polyamidoamide (G4-PAMAM) dendrimers containing the anti-tuberculosis drug rifampicin had high stability under physiological pH conditions, and the PAMAM dendrimers could be used as a pH switch to rapidly release drugs in the acidic area of macrophages. Similarly, Rajabnezhad et al ( 89 ) synthesized different generations of PAMAM dendrimers encapsulating rifampicin to produce inhalable nanodrugs for the treatment of tuberculosis. Their results showed that compared with intravenous administration, third generation PAMAM dendrimers achieved sustained drug release, and significantly improved drug absorption and bioavailability.…”

Section: Application Of Nps In Respiratory Systemsmentioning

confidence: 99%

Application of nanotechnology in drug delivery systems for respiratory diseases (Review)

2021

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Respiratory disease is a common disease with a high incidence worldwide, which is a serious threat to human health, and is considered a societal and economic burden. The application of nanotechnology in drug delivery systems has created new treatments for respiratory diseases. Within this context, the present review systematically introduced the physicochemical properties of nanoparticles (NPs); reviewed the current research status of different nanocarriers in the treatment of respiratory diseases, including liposomes, solid lipid nanocarriers, polymeric nanocarriers, dendrimers, inorganic nanocarriers and protein nanocarriers; and discussed the main advantages and limitations of therapeutic nanomedicine in this field. The application of nanotechnology overcomes drug inherent deficiencies to a certain extent, and provides unlimited potential for the development of drugs to treat respiratory diseases. However, most of the related research work is in the preclinical experimental stage and safety assessment is still a challenging task. Future studies are needed to focus on the performance modification, molecular mechanism and potential toxicity of therapeutic nanomedicine.

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“…Furthermore, interestingly, after pulmonary insufflation, G3rifampicin microspheres exhibited 30 and 4-fold improvement in mean residence time and plasma drug concentration compared to intravenous administration of drug alone. Simply, polycationic dendrimer-based microspheres can play important role in the pulmonary delivery of rifampicin like therapeutic agents [44].…”

Section: Dendrimersmentioning

confidence: 99%

Potential of dry powder inhalers for tuberculosis therapy: facts, fidelity and future

Mehta

Bothiraja

Kadam

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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Tuberculosis (TB) is a contagious and airborne infectious disease caused by the pathogen Mycobacterium tuberculosis (Mtb). In spite of substantial research efforts, continuous multiple high-dose drug therapy regularly for 4-7 months can impede patient quality of life. The pathology of TB and biology of pulmonary airways permits for a variety of drug delivery strategies and natural route of infection denotes a more logical remedial approach for treatment of TB. Pulmonary delivery is non-invasive, allow easy transcytosis in alveolar region, avoids first-pass metabolism and extensive vascularization facilitates delivery of therapeutic agents to infection site. It also potentially reduces the frequency with dose requirement and linked side effects. Dry powder is a most preferred inhalation option due to their greater physiochemical stability over liquid or suspension based formulations. Dry powder inhalers (DPIs) are easy to handle and appropriate for high-dose formulations. Moreover, the progress of disciplines such as nanotechnology, particle engineering, material science and molecular biology permits further expansion of treatment capability and efficiency. Thus, this article will focus on the role of novel DPIs systems for treatment of TB. This article also contains a dedicated section discussing about technical limitations and clinical challenges with help of strengths, weaknesses, opportunities and threats (SWOT) analysis. Additionally, it will also offer some basic background information for drug repurposing, formulation development and drug delivery systems.

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Pulmonary delivery of rifampicin microspheres using lower generation polyamidoamine dendrimers as a carrier

Cited by 39 publications

References 53 publications

Obtaining and Applying Nanohybrid Palygorskite-Rifampicin in the pH-Responsive Release of the Tuberculostatic Drug

Obtaining and Applying Nanohybrid Palygorskite-Rifampicin in the pH-Responsive Release of the Tuberculostatic Drug

Application of nanotechnology in drug delivery systems for respiratory diseases (Review)

Potential of dry powder inhalers for tuberculosis therapy: facts, fidelity and future

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