Association of the anti-tuberculosis drug rifampicin with a PAMAM dendrimer

Bellini, Reinaldo G.; Guimarães, Ana P.; Pacheco, Marco Aurélio Cavalcanti; Dias, Douglas Mota; Furtado, Vanessa R.; Alencastro, Ricardo Bicca de; Horta, Bruno A. C.

doi:10.1016/j.jmgm.2015.05.012

Cited by 71 publications

(32 citation statements)

References 100 publications

(106 reference statements)

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“…MKTOP is topology generation tool that has been widely used in the study of various compounds in molecular dynamics. The charges of the inhibitors generated by this server have also been validated in similar compounds (47)(48)(49)(50)(51)(52)(53)(54). The protein along with TBO was solvated in a periodic cubic box of dimension 6.884 nm with 10,298 water molecules using a simple point charge (SPC 216) model (55).…”

Section: Methodsmentioning

confidence: 99%

Elucidation of Binding Mechanism of Photodynamic Therapeutic Agent Toluidine Blue O with Chicken Egg White Lysozyme by Spectroscopic and Molecular Dynamics Studies

Shanmugaraj

Umadevi

Lakshmipathi

et al. 2017

Photochem & Photobiology

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The nature of binding mechanism of toluidine blue O (TBO) with chicken egg white lysozyme was studied comprehensively by various spectroscopic and computational methods. Both steady state and time-resolved fluorescence studies unambiguously point to the prevalence of static quenching mechanism in lysozyme-TBO system. Thermodynamic parameters revealed that the association of TBO with lysozyme was a spontaneous process in which hydrophobic and hydrogen bond interactions played a pivotal role in the binding process. The secondary and tertiary conformational changes of lysozyme in the presence of TBO were unraveled using absorption, Fourier transform infrared spectroscopy (FT-IR) and circular dichroism (CD) techniques. Molecular docking studies of lysozyme-TBO system substantiated the findings of site marker experiment and revealed TBO adjacent to Trp-63 and Trp-108 residues of lysozyme. Molecular dynamics (MD) simulation studies of lysozyme-TBO system indicate a stable and effective complexation of TBO with lysozyme. It is hoped that the results presented here will enable further understanding of TBO toxicity.

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Section: Methodsmentioning

confidence: 99%

Elucidation of Binding Mechanism of Photodynamic Therapeutic Agent Toluidine Blue O with Chicken Egg White Lysozyme by Spectroscopic and Molecular Dynamics Studies

Shanmugaraj

Umadevi

Lakshmipathi

et al. 2017

Photochem & Photobiology

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“…It has limited aqueous solubility which also limits its clinical applications (Agrawal et al, 2004; Sosnik et al, 2010). Bellini et al investigated RIF in combination with a G4-PAMAM dendrimer and reported that approximately 20 RIF molecules were getting loaded per molecule of the dendrimer (Bellini et al, 2015). The study reported that the drug-dendrimer complex was stable at neutral pH conditions while it was labile at acidic pH conditions where the drug molecules were rapidly releasing from the complex.…”

Section: Solubilization Of Existing Drugsmentioning

confidence: 99%

Impact of Dendrimers on Solubility of Hydrophobic Drug Molecules

et al. 2017

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Adequate aqueous solubility has been one of the desired properties while selecting drug molecules and other bio-actives for product development. Often solubility of a drug determines its pharmaceutical and therapeutic performance. Majority of newly synthesized drug molecules fail or are rejected during the early phases of drug discovery and development due to their limited solubility. Sufficient permeability, aqueous solubility and physicochemical stability of the drug are important for achieving adequate bioavailability and therapeutic outcome. A number of different approaches including co-solvency, micellar solubilization, micronization, pH adjustment, chemical modification, and solid dispersion have been explored toward improving the solubility of various poorly aqueous-soluble drugs. Dendrimers, a new class of polymers, possess great potential for drug solubility improvement, by virtue of their unique properties. These hyper-branched, mono-dispersed molecules have the distinct ability to bind the drug molecules on periphery as well as to encapsulate these molecules within the dendritic structure. There are numerous reported studies which have successfully used dendrimers to enhance the solubilization of poorly soluble drugs. These promising outcomes have encouraged the researchers to design, synthesize, and evaluate various dendritic polymers for their use in drug delivery and product development. This review will discuss the aspects and role of dendrimers in the solubility enhancement of poorly soluble drugs. The review will also highlight the important and relevant properties of dendrimers which contribute toward drug solubilization. Finally, hydrophobic drugs which have been explored for dendrimer assisted solubilization, and the current marketing status of dendrimers will be discussed.

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“…Tuberculosis is the leading cause of preventable deaths worldwide. Nanoparticle-based drug delivery systems may be considered for the treatment of tuberculosis due to the slow and sustained release of drugs such as classic tuberculostatic agents from the solid lipid nanoparticles both in vitro and in vivo, thus meaning the patients will undergo treatment fewer times per week, therefore increasing adherence to treatment and also the quality of life (50,59,60).…”

Section: Discussionmentioning

confidence: 99%

Nanoparticles in the treatment of chronic lung diseases

Alexescu¹,

Ţărmure²,

Negrean³

et al. 2019

JMMS

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Nanoparticles, although considered a topic of modern medicine, actually have an interesting history. Currently, advances in nanomedicine hold great promise as drug carrier systems for sustained release and targeted delivery of diverse therapeutic agents. Nanoparticles can be defined as complex drug carrier systems which incorporate and protect a certain drug or particle. Nanoparticles can be administered via different routes, such as intravenous injection, oral administration, or pulmonary inhalation. Even though the use of nano-carriers via pulmonary inhalation is heavily debated, this system represents an attractive alternative to the intravenous or oral routes, due to the unique anatomical and physiological features of the lungs and the minimal interactions between the targeted site and other organs. Some of the widely used nano-carriers for the treatment of chronic pulmonary diseases, via pulmonary route, are as follows: polymeric nanoparticles, liposomal nano-carriers, solid lipid nanoparticles, and submicron emulsions. Nanocarrier systems provide the advantage of sustained-drug release in the lung tissue resulting in reduced dosing frequency and improved patient compliance. Further studies focusing on understanding the mechanisms of action of nanoparticles and improving their chemical structure are required in order to better understand the potential long-term risk of excipient toxicity and nanoscale carriers.

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Association of the anti-tuberculosis drug rifampicin with a PAMAM dendrimer

Cited by 71 publications

References 100 publications

Elucidation of Binding Mechanism of Photodynamic Therapeutic Agent Toluidine Blue O with Chicken Egg White Lysozyme by Spectroscopic and Molecular Dynamics Studies

Elucidation of Binding Mechanism of Photodynamic Therapeutic Agent Toluidine Blue O with Chicken Egg White Lysozyme by Spectroscopic and Molecular Dynamics Studies

Impact of Dendrimers on Solubility of Hydrophobic Drug Molecules

Nanoparticles in the treatment of chronic lung diseases

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