Potential Tuberculostatic Agent: Micelle‐forming Pyrazinamide Prodrug

Silva, Marcia; Ricelli, Nara Lúcia; Seoud, Omar A. El; Valentim, Celso S.; Ferreira, Antônio Gilberto; Sato, Daisy Nakamura; Leite, Clarice Queico Fujimura; Ferreira, Elizabeth Igne

doi:10.1002/ardp.200500039

Cited by 33 publications

(17 citation statements)

References 14 publications

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“…A 5.6-fold increase in anti-tuberculosis activity against M. tuberculosis was found for micelle-forming prodrug as compared to the free drug [86]. Similar attempts were made to incorporate PYZ and RIF in micelles ( <100 nm) aiming to minimize renal filtration and prolonging mean residence times in the blood stream with improved antimicrobial activity [87,88]. INH lipid derivatives was designed by Jin et al to reduce the resistance.…”

Section: Inh-poly(ethyleneglycol)-poly(aspartic Acid)mentioning

confidence: 99%

Present status of nanoparticle research for treatment of Tuberculosis

2011

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-Nanotechnology has offered enormous improvement in field of therapeutics by means of designing of drug delivery systems and opened the possibility of controlling infections at the molecular level. Nanocarriers can cross biological barriers and are able to target cellular reservoirs of Mycobacterium tuberculosis (M. tuberculosis). Nanoparticle-based systems have significant potential for treatment and prevention of tuberculosis (TB). A variety of nanocarriers have been widely evaluated as potential drug delivery systems for various administration routes. Targeting the drugs to certain physiological sites such as the lymph nodes has emerged as a promising strategy in treating TB with improved drug bioavailability and reduction of the dosing frequency. Nanotechnology based rational targeting may improve therapeutic success by limiting adverse drug effects and requiring less frequent administration regimes, ultimately resulting in more patients compliance and thus attain higher adherence levels. The development of nanoparticle based aerosol vaccine is undergoing which could serve as new platform for immunization. Present article compiles the general physiological aspects of the infection along with new research uptades on nanocarriers used in prevention of tuberculosis. _______________________________________________________________________________________

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Section: Inh-poly(ethyleneglycol)-poly(aspartic Acid)mentioning

confidence: 99%

Present status of nanoparticle research for treatment of Tuberculosis

2011

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“…The mechanism would primarily involve the micelle uptake and the latter intracellular release of the drug after the hydrolysis of the linkage. The same synthetic pathway was pursued in order to encapsulate PYZ [46,47] and RIF [47]. The size of themicelles would prevent renal filtration, increasing the residence times in the blood stream.…”

Section: Polymeric Micellesmentioning

confidence: 99%

Nanotechnology: A focus on Treatment of Tuberculosis.

Kumar¹,

Kumar²,

Kumar³

et al. 2011

Int J Drug Del

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Despite the fact that we live in an era of advanced technology and innovation, infectious diseases, like Tuberculosis (TB), continue to be one of the greatest health challenges worldwide. The main drawbacks of conventional TB treatment are the development of multiple drug resistance, resulting in high dose requirements and subsequent intolerable toxicity. Therefore there is a need of a new system have been receiving special attention with the aim of minimizing the side effects of drug therapy, such as poor bioavailability and the selectivity of drugs. Nanoparticle-based drug delivery systems have considerable potential for treatment of TB. The important technological advantages of nanoparticles used as drug carriers are high stability, high carrier capacity, feasibility of incorporation of both hydrophilic and hydrophobic substances, and feasibility of variable routes of administration, including oral application and inhalation. Nanoparticles can also be designed to allow controlled (sustained) drug release from the matrix. These properties of nanoparticles enable improvement of drug bioavailability and reduction of the dosing frequency, and may resolve the problem of nonadherence to prescribed therapy, which is one of the major obstacles in the control of TB epidemics. In this review, we discuss the challenges with the current treatment of the disease and shed light on the remarkable potential of nanotechnology to provide more effective treatment and prevention for TB.

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“…Applicability of synthetic polypeptide‐based conjugate development has reached multiple areas of medicine, including the elaboration of anti‐microbial, anti‐virus, anti‐cancer, anti‐diabetic, anti‐apoptotic, and anti‐tuberculosis drugs, magnetic resonance imaging (MRI) agents, and theranostic agents . The great advantage of polypeptides is their structural versatility which allows the generation of a myriad of architectures with differential physico‐chemical features, allowing high loading rates and the possibility to conjugate drugs of different origin, polarity, and hydrophilicity.…”

Section: Introductionmentioning

confidence: 99%

Polypeptide‐Based Conjugates as Therapeutics: Opportunities and Challenges

Zagorodko

Arroyo‐Crespo

Nebot

et al. 2016

Macromolecular Bioscience

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Synthetic polypeptides or polyamino acids have become a useful and multifunctional platform in advanced drug delivery studies. Nonetheless, the full potential of these systems has yet to be achieved. The final structure of polypeptide conjugates and their in vivo behavior are dependent on an extraordinarily complex pattern of interconnected physico-chemical and structural parameters, making sophisticated directional design of such systems difficult and often unachievable. In this review, the authors aim to discuss the role of these parameters in the successful design of different drug delivery architectures and to delineate some basic correlations between structure, properties, and the biological behavior of polypeptide-based conjugates.

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Potential Tuberculostatic Agent: Micelle‐forming Pyrazinamide Prodrug

Cited by 33 publications

References 14 publications

Present status of nanoparticle research for treatment of Tuberculosis

Present status of nanoparticle research for treatment of Tuberculosis

Nanotechnology: A focus on Treatment of Tuberculosis.

Polypeptide‐Based Conjugates as Therapeutics: Opportunities and Challenges

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