Supramolecular assembly of rifampicin and PEGylated PAMAM dendrimer as a novel conjugate for tuberculosis

Ahmed, Rami M. Y.; Aucamp, Marique; Ebrahim, Naushaad; Samsodien, Halima

doi:10.1016/j.jddst.2021.102773

Cited by 16 publications

(12 citation statements)

References 41 publications

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“…Figure 2 showed the FT-IR spectrum of mPEG-NPC, G3.0 and G3.0@mPEG. In the spectra of mPEG-NPC, the peak at 2888 cm −1 was C-H stretching vibration, the peak at 1114 cm −1 was the C-O asymmetric stretch and the peak at 1768 cm −1 indicated vibration of C=O stretch of carbonate group [ 35 , 36 ]. In spectra of G3.0, the appearance of peak at 3415–3265 cm −1 was attributed to secondary amine group (-NH-).…”

Section: Resultsmentioning

confidence: 99%

“…The strong peak at 1645 cm −1 was C=O stretch of amide group, and the one at 1556 cm −1 was N-H bending vibration. In the spectra of G3.0@mPEG, there were peaks of G3.0 at 3345–3356 cm −1 (N-H) and 1641 cm −1 (C=O of amide); and peak of PEG at 1112 cm −1 (C-O) [ 35 , 37 ]. Besides, the disappearance of peak at 1768 cm −1 was due to the replacement of carbonate group by carbamate group, which demonstrate that PEG was conjugated with G3.0 [ 36 ].…”

Section: Resultsmentioning

confidence: 99%

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Retrovirus Drugs-Loaded PEGylated PAMAM for Prolonging Drug Release and Enhancing Efficiency in HIV Treatment

Nguyen

et al. 2021

Polymers

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Polyamidoamine dendrimer (PAMAM) with its unique characteristics emerges as a potential drug delivery system which can prolong releasing time, reduce the side effects but still retaining treatment efficiency. In this study, methoxy polyethylene glycol modified PAMAM generation 3.0 (G3.0@mPEG) is prepared and characterized via 1H-NMR, FT-IR, and TEM. Subsequently, two antiretroviral agents (ARV) including lamivudine (3TC) and zidovudine (AZT) are individually encapsulated into G3.0@mPEG. The drug-loading efficiency, drug release profile, cytotoxicity and anti-HIV activity are then evaluated. The results illustrate that G3.0@mPEG particles are spherical with a size of 34.5 ± 0.2 nm and a drug loading content of about 9%. Both G3.0@mPEG and ARV@G3.0@mPEG show no cytotoxicity on BJ cells, and G3.0@mPEG loading 3TC and AZT performs sustained drug release behavior which is best fitted with the Korsmeyer–Peppas model. Finally, the anti-HIV activity of ARV via Enzymatic Assay of Pepsin is retained after being loaded into the G3.0@mPEG, in which about 36% of pepsin activity was inhibited by AZT at the concentration of 0.226 mM. Overall, PAMAM G3.0@mPEG is a promising nanocarrier system for loading ARV in HIV treatment and prevention.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Retrovirus Drugs-Loaded PEGylated PAMAM for Prolonging Drug Release and Enhancing Efficiency in HIV Treatment

Nguyen

et al. 2021

Polymers

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“…The synthetic DDSs, such as NPs [ 136 , 137 , 138 ], liposomes [ 139 , 140 , 141 , 142 ], dendrimers [ 143 , 144 , 145 ], micelles [ 146 , 147 , 148 ], nanocapsules [ 149 , 150 , 151 ], nanosponges [ 152 , 153 ], peptide-based nanoparticles [ 154 ], etc., have good drug encapsulation efficiency (EE), drug loading (DL) capacity, flexibility in functionalization, easy/robust production, and theragnostic functions. However, conjugation of a PEG polymer, peptide, antibody, etc.…”

Section: Conclusion and Future Perspectivesmentioning

confidence: 99%

Targeted Drug Delivery to the Central Nervous System Using Extracellular Vesicles

et al. 2022

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The blood brain barrier (BBB) maintains the homeostasis of the central nervous system (CNS) and protects the brain from toxic substances present in the circulating blood. However, the impermeability of the BBB to drugs is a hurdle for CNS drug development, which hinders the distribution of the most therapeutic molecules into the brain. Therefore, scientists have been striving to develop safe and effective technologies to advance drug penetration into the CNS with higher targeting properties and lower off-targeting side effects. This review will discuss the limitation of artificial nanomedicine in CNS drug delivery and the use of natural extracellular vesicles (EVs), as therapeutic vehicles to achieve targeted delivery to the CNS. Information on clinical trials regarding CNS targeted drug delivery using EVs is very limited. Thus, this review will also briefly highlight the recent clinical studies on targeted drug delivery in the peripheral nervous system to shed light on potential strategies for CNS drug delivery. Different technologies engaged in pre- and post-isolation have been implemented to further utilize and optimize the natural property of EVs. EVs from various sources have also been applied in the engineering of EVs for CNS targeted drug delivery in vitro and in vivo. Here, the future feasibility of those studies in clinic will be discussed.

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“…The PEGylation of a dendrimer showed negligible toxicity for formulation with 100% functionalization. Thus, formulated PEGylated 4.0 G PAMAM dendrimers are proven to be the choice of drug carrier with high loading, negligible toxicity, and extended-release pattern for rifampicin (Ahmed et al, 2021).…”

Section: Dendrimersmentioning

confidence: 99%

Nanocarrier-Based Approaches for the Efficient Delivery of Anti-Tubercular Drugs and Vaccines for Management of Tuberculosis

2021

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Drug-resistant species of tuberculosis (TB), which spread faster than traditiona TB, is a severely infectious disease. The conventional drug therapy used in the management of tuberculosis has several challenges linked with adverse effects. Hence, nanotherapeutics served as an emerging technique to overcome problems associated with current treatment. Nanotherapeutics helps to overcome toxicity and poor solubility issues of several drugs used in the management of tuberculosis. Due to their diameter and surface chemistry, nanocarriers encapsulated with antimicrobial drugs are readily taken up by macrophages. Macrophages play a crucial role as they serve as target sites for active and passive targeting for nanocarriers. The surface of the nanocarriers is coated with ligand-specific receptors, which further enhances drug concentration locally and indicates the therapeutic potential of nanocarriers. This review highlights tuberculosis’s current facts, figures, challenges associated with conventional treatment, different nanocarrier-based systems, and its application in vaccine development.

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Supramolecular assembly of rifampicin and PEGylated PAMAM dendrimer as a novel conjugate for tuberculosis

Cited by 16 publications

References 41 publications

Retrovirus Drugs-Loaded PEGylated PAMAM for Prolonging Drug Release and Enhancing Efficiency in HIV Treatment

Retrovirus Drugs-Loaded PEGylated PAMAM for Prolonging Drug Release and Enhancing Efficiency in HIV Treatment

Targeted Drug Delivery to the Central Nervous System Using Extracellular Vesicles

Nanocarrier-Based Approaches for the Efficient Delivery of Anti-Tubercular Drugs and Vaccines for Management of Tuberculosis

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