Characterization and evaluation of nanoencapsulated diethylcarbamazine in model of acute hepatic inflammation

Rodrigues, Gabriel Barros; Oliveira, Elquio Eleamen; Mendonça, Francisco Jaime Bezerra; Santos, Laise Aline Martins dos; Oliveira, W.; França, Maria Eduarda Rocha de; Lós, Deniele Bezerra; Gabínio, Brennda Martins; Lira, Fábia Cristiane Melo Leite de; Peixoto, Christina Alves

doi:10.1016/j.intimp.2017.07.014

Cited by 6 publications

(9 citation statements)

References 31 publications

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“…Zeta [20] and [35] are thought to favor the best stability due to repulsive forces preventing aggregation upon aging. By contrast, zeta potential values close to 0 are related to the biocompatibility of the nanoparticles [24]. The addition of 6CN10 (free or complex) did not induce any drastic modification in the size and zeta potential of the nanoparticles (Table 1).…”

Section: Discussionmentioning

confidence: 93%

Incorporation of 2-amino-thiophene derivative in nanoparticles: enhancement of antifungal activity

Neves

Macêdo

et al. 2020

Braz J Microbiol

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The objective of this study was to evaluate the effects of nanoparticles (nanospheres and nanocapsules) of the promising antifungal 2-amino-thiophene (6CN10) and 6CN10 complexed with 2-hydroxypropyl-β-cyclodextrin (6CN10:HP-β-CD) in vitro and compared with free drug against Candida and Cryptococcus, using a microdilution method to measure susceptibility. The Candida and Cryptococcus clinical strains were identified using phenotypic methods and matrix-assisted laser desorption/ ionization-time of flight (MALDI-TOF). To measure in vitro antifungal susceptibility, we used microdilution trials. Serial drug or nanoparticle dilutions were prepared according to the CLSI M27-A3 guidelines. Anti-biofilm activity was verified for Cryptococcus neoformans. All Candida isolates were sensitive to the free drug (MIC = 41.66-333.33 μg/mL) and were able to grow even at the higher concentration tested for all 6CN10 nanoparticles. However, the Cryptococcus neoformans strains presented MIC values of 0.32-83.33 μg/mL for 6CN10 nanoparticles, and MIC values of 0.1-0.2 μg/mL for 6CN10:HP-β-CD nanoparticles, i.e., 3333 times more active than the free drug (MIC values 166.66-333.33 μg/mL), and presenting activity greater than that of the reference drug amphotericin B (MIC = 0.5-0.125 μg/mL). 6CN10:HP-β-CD nanosphere also showed high antibiofilm potential. The in vitro study showed that the nanoparticles allowed better drug efficiency against Cryptococcus than did the free drug. These results suggest that 6CN10-loaded nanoparticles may become a future alternative for cryptococcosis and candidiasis therapy. In vivo experiments are essential prior to clinical use.

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Section: Discussionmentioning

confidence: 93%

Incorporation of 2-amino-thiophene derivative in nanoparticles: enhancement of antifungal activity

Neves

Macêdo

et al. 2020

Braz J Microbiol

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“…In filarial cystitis bladder mucosa shows a normal urothelium with mild degree of inflammation comprising of lymphocytes and eosinophils and microfilariae of Wuchereria bancrofti can be seen in the bladder wall rarely [ 6 , 7 ]. In our patient, microfilariae were not seen in the biopsy specimen and serum IFAT for filariasis was negative though there was a good response to DEC. Several recent studies have investigated the efficacy of DEC in inflammatory conditions like lung injury and acute hepatitis [ 8 , 9 ]. Accordingly DEC has strong anti-inflammatory effects which may have lead to improvement of the chronic cystitis of our patient.…”

Section: Discussionmentioning

confidence: 99%

A case of follicular cystitis treated successfully with diethylcarbamazine

Kumara

Thiranagama

Sosai

et al. 2021

Asian Journal of Urology

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Follicular cystitis is a non-specific inflammatory condition of the bladder where the aetiology is unknown. The extent of the disease can be mild or proliferative and bulky. Antibiotics, steroids, therapies used for interstitial cystitis, palliative cystectomy and radiotherapy have been reported as successful treatment options. We report a case of follicular cystitis that responded to a course of oral diethyl carbamazine.

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“…For example, ramelteon and fluoxetine can relieve neuroinflammation [ 33 , 47 , 48 ], and rilmenidine and vinburnine have been reported to have neuroprotective effects [ 49 , 50 , 51 ]. Moreover, nepafenac, diphenylpyraline [ 52 , 53 ], sufentanil [ 54 ], dutasteride [ 55 ], and diethylcarbamazine [ 56 , 57 ] have also been found to have anti-inflammatory effects, indicating that this strategy contributes to identifying potential compounds having anti-neuroinflammation properties among approved and marketed drugs. The lengthy time to develop new drugs and the hindrance posed by the BBB are the main obstructions for uncovering novel treatments for neuroinflammation [ 58 ].…”

Section: Discussionmentioning

confidence: 99%

LINCS Dataset-Based Repositioning of Dutasteride as an Anti-Neuroinflammation Agent

Luo¹,

Han²,

Gao³

et al. 2021

Brain Sciences

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Neuroinflammation is often accompanied by central nervous system (CNS) injury seen in various CNS diseases, with no specific treatment. Drug repurposing is a strategy of finding new uses for approved or investigational drugs, and can be enabled by the Library of Integrated Network-based Cellular Signatures (LINCS), a large drug perturbation database. In this study, the signatures of Lipopolysaccharide (LPS) were compared with the signatures of compounds contained in the LINCS dataset. To the top 100 compounds obtained, the Quantitative Structure-Activity Relationship (QSAR)-based tool admetSAR was used to identify the top 10 candidate compounds with relatively high blood–brain barrier (BBB) penetration. Furthermore, the seventh-ranked compound, dutasteride, a 5-α-reductase inhibitor, was selected for in vitro and in vivo validation of its anti-neuroinflammation activity. The results showed that dutasteride significantly reduced the levels of IL-6 and TNF-α in the supernatants of LPS-stimulated BV2 cells, and decreased the levels of IL-6 in the hippocampus and plasma, and the number of activated microglia in the brain of LPS administration mice. Furthermore, dutasteride also attenuated the cognitive impairment caused by LPS stimulation in mice. Taken together, this study demonstrates that the LINCS dataset-based drug repurposing strategy is an effective approach, and the predicted candidate, dutasteride, has the potential to ameliorate LPS-induced neuroinflammation and cognitive impairment.

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Characterization and evaluation of nanoencapsulated diethylcarbamazine in model of acute hepatic inflammation

Cited by 6 publications

References 31 publications

Incorporation of 2-amino-thiophene derivative in nanoparticles: enhancement of antifungal activity

Incorporation of 2-amino-thiophene derivative in nanoparticles: enhancement of antifungal activity

A case of follicular cystitis treated successfully with diethylcarbamazine

LINCS Dataset-Based Repositioning of Dutasteride as an Anti-Neuroinflammation Agent

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