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1.
Langmuir ; 38(33): 10173-10182, 2022 08 23.
Artículo en Inglés | MEDLINE | ID: mdl-35947770

RESUMEN

Polyoxyethylene sorbitan monooleate is commonly used to obtain stable dispersions of nanoparticles (NPs) such as carbon nanotubes (CNTs) and graphene. However, the mechanism underlying dispersion is poorly understood. The present study aimed at investigating the mechanism of stabilization of carbon NPs (CNPs), namely, single-walled CNTs (SWCNTs), multi-walled CNTs (MWCNTs), and graphene, by Tween-80 using attenuated total internal reflection-Fourier transform infrared and nuclear magnetic resonance (NMR) spectroscopy. Molecular dynamics (MD) simulations were performed to identify, at the atomic scale, the significant interactions that underlie the adsorption and the stabilizing effect of Tween-80 on CNPs, in this way corroborating the spectroscopy results. Spectroscopic analysis revealed that the alkyl chain tether to SWCNT, MWCNT, and graphene surface, presumably through π-π interactions between the carbon-carbon double bond in the alkyl chain and the aromatic rings of CNPs. The hydrophilic polyethoxylate chains extend into the aqueous environment and stabilize the suspension by steric hindrance. MD simulations also showed that Tween-80 molecules interact with the CNP surface via the alkyl chain, thus corroborating spectroscopy results. MD simulations additionally revealed that Tween-80 aggregates on the CNP surface shifted from planar to micelle-like with increasing Tween-80 ratios, underscoring concentration-dependent changes in the nature of these interactions.


Asunto(s)
Grafito , Nanotubos de Carbono , Adsorción , Nanotubos de Carbono/química , Polisorbatos , Análisis Espectral
2.
Drug Deliv Transl Res ; 12(10): 2501-2517, 2022 10.
Artículo en Inglés | MEDLINE | ID: mdl-34782995

RESUMEN

Azelaic acid (AzA) is a USFDA bioactive prescribed against acne vulgaris. It possesses delivery challenges like poor aqueous solubility, low skin-penetrability, and dose-dependent side effects, which could be overcome by its synergistic combination with tea tree oil (TTO) as a microemulsion (ME)-based hydrogel composite. AzA-TTO ME was prepared to employ pseudo-ternary phase diagram construction. The best AzA-TTO ME was of uniform size (polydispersity index < 0.7), nano-range (~357.4 ± 2% nm), transmittance (> 90%), and negative zeta potential (-1.42 ± 0.25% mV) values. ME hydrogel composite with optimum rheological and textural attributes showed better permeation, retention, and skin-compliant characteristics, vis-a-vis marketed formulation (Aziderm™) when evaluated in Wistar rat skin. In vitro antibacterial efficacy in bacterial strains, i.e., Staphylococcus aureus, Propionibacterium acne, and Staphylococcus epidermidis, was evaluated employing agar well plate diffusion and broth dilution assay. ME hydrogel has shown an increase in zone of inhibition by two folds and a decrease in minimum inhibitory concentration (MIC) by eightfold against P. acnes vis-a-vis AzA. Finally, ME hydrogel composite exhibited a better reduction in the papule density (93.75 ± 1.64%) in comparison to Aziderm™ 72.69 ± 4.67%) on acne as developed in rats by inducing testosterone. Thus, the developed AzA-TTO ME hydrogel composite promises an efficacious and comparatively safer drug delivery system for the topical therapy of acne vulgaris.


Asunto(s)
Acné Vulgar , Aceite de Árbol de Té , Acné Vulgar/inducido químicamente , Acné Vulgar/tratamiento farmacológico , Acné Vulgar/microbiología , Animales , Ácidos Dicarboxílicos , Hidrogeles/uso terapéutico , Propionibacterium , Ratas , Ratas Wistar , , Testosterona/uso terapéutico , Árboles
3.
Ther Deliv ; 13(1): 13-29, 2022 01.
Artículo en Inglés | MEDLINE | ID: mdl-34842461

RESUMEN

Aim: Azelaic acid (AzA), a comedolytic, antibacterial, anti-inflammatory anti-melanogenic agent, prescribed against acne vulgaris is safe on skin. Its combination with another widely used anti-acne agent, tea tree oil (EO) whose delivery is limited by volatility, instability and lipophilicity constraints was attempted. Method: Solvent injection was used to prepare AzA-EO integrated ethosomes. Result: Ethosomes were transformed into carbopol hydrogel, which exhibited pseudo-plastic properties with appreciable firmness, work of shear, stickiness and work of adhesion. The hydrogel showed better permeation and retention characteristics vis-a-vis commercial formulation (AzidermTM), when evaluated in Wistar rat skin. Further, ethosome hydrogel composite was better tolerated with no side effects. Conclusion: The findings suggests that the aforementioned strategy could be a potential treatment used for acne management.


Asunto(s)
Acné Vulgar , Melaleuca , Aceite de Árbol de Té , Acné Vulgar/tratamiento farmacológico , Animales , Antibacterianos , Ácidos Dicarboxílicos , Excipientes , Hidrogeles , Ratas , Ratas Wistar , Aceite de Árbol de Té/uso terapéutico
4.
BMC Complement Altern Med ; 19(1): 334, 2019 Nov 27.
Artículo en Inglés | MEDLINE | ID: mdl-31771651

RESUMEN

BACKGROUND: Psoriasis, a recurrent, chronic inflammatory disorder of skin, is a common problem in middle age and elderly people. Thymoquinone (TQ), a lipid soluble benzoquinone is the major active ingredient of volatile oil of Nigella sativa (NS), possesses good anti-psoriatic activity. However, its hydrophobicity, poor aqueous solubility, and photosensitive nature obstructs its development. Therefore, in the present research work, ethosomal vesicles (EVs) loaded with TQ were assessed for its anti-psoriatic potential employing mouse-tail model. METHODS: TQ-loaded EVs were prepared by cold method, and characterized for various essential attributes, viz. particle size, morphology, percent drug entrapment, flexibility, rheological and textural analysis, and skin absorption. The optimized formulation was finally evaluated for anti-psoriatic activity on Swiss albino mice employing mouse-tail model for psoriasis. RESULTS: The spherical shaped vesicles were in the nanosize range, and had high flexibility. The EVs incorporated hydrogel was rheologically acceptable and resulted in substantial TQ retention in the skin layers. The % anti-psoriatic drug activity was observed to be substantially better in the case of TQ-loaded ethosomal gel vis-à-vis plain TQ, NS extract, and marketed formulation. CONCLUSIONS: The promising outcomes of the current studies ratify the superiority of TQ-loaded phospholipid-based vesicular systems for the management of psoriasis over other studied test formulations. This study, thus open promising avenues for topical application of TQ in the form of EV hydrogel.


Asunto(s)
Benzoquinonas , Portadores de Fármacos , Nanomedicina/métodos , Fosfolípidos , Psoriasis , Animales , Benzoquinonas/administración & dosificación , Benzoquinonas/química , Benzoquinonas/farmacocinética , Modelos Animales de Enfermedad , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Portadores de Fármacos/farmacología , Ratones , Nigella sativa/química , Fosfolípidos/química , Fosfolípidos/farmacocinética , Fosfolípidos/farmacología , Psoriasis/metabolismo , Psoriasis/patología , Piel/efectos de los fármacos , Piel/metabolismo , Piel/patología , Absorción Cutánea/efectos de los fármacos
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