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1.
Turk J Pharm Sci ; 17(3): 271-279, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32636704

RESUMO

OBJECTIVES: There is an increasing demand for wound healing products of natural origin. Our objective was to develop a spray formulation from Jatropha curcas (J. curcas) L. latex extracts for wound healing applications. MATERIALS AND METHODS: J. curcas L. latex was subjected to solvent extraction. The phytochemical structure was elucidated by 1H-NMR and confirmed by liquid chromatography-mass spectrometer spectrometry. A topical spray formulation prepared from J. curcas latex extracts was evaluated in terms of its antimicrobial activity and radical scavenging activity. The toxicity of the formulation on fibroblast cell lines, collagen production, and wound healing activities were tested. RESULTS: The 1H-NMR and mass spectrometric analyses revealed the pure compound as curcacycline A. The J. curcas latex extract formulation had radical scavenging and antibacterial activities. Moreover, the formulation was not toxic to the human fibroblast cells and it stimulated collagen production and healed cell injury in 24 h. CONCLUSION: The J. curcas latex extract promoted wound healing after cell injury. Our findings indicate the possibility of utilizing the J. curcas latex extract spray formulation as a potential antibacterial, antioxidant, and wound healing product from nature.

2.
Colloids Surf B Biointerfaces ; 182: 110374, 2019 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-31330430

RESUMO

This work presents the outcomes of a comparative study of molecular interactions of polymyxin B (PMB) and F12 and F13 formulations in the mole ratios of 1:2 and 1:3 of PMB:sodium deoxycholate sulfate (SDCS), respectively, and a commercial PMB formulation (CPMB) with lipopolysaccharides (LPS). Several spectroscopic and interfacial studies were performed to obtain LPS-peptide interactions at a molecular level. The fluorescence titrimetry method revealed that the F12 formulation (325 nM) exhibited a lower number of binding sites to the LPS compared to CPMB and F13 as well as PMB alone (537 nM). Similarly, in the presence of LPS, the F12 formulation (88 nm) exhibited smaller particle sizes in the dynamic light scattering study compared to PMB (116 nm), CPMB, and the F13 formulation. An interfacial study and circular dichroism spectroscopy revealed PMB and CPMB insertion into the LPS micelles to destabilize and disrupt the LPS membrane, whereas the F12 and F13 formulations may induce pseudo-aggregation. The NMR and IR studies showed that the presence of SDCS, the hydrophobicity of PMB increased by hydrogen bonding and electrostatic interactions and formed stabilized PMB-SDCS micelles. The PMB-SDCS formulation is likely to release PMB for easy penetration into the lipid membrane and cause disruption of the complex LPS micelles. Furthermore, the PMB-SDCS formulations neutralized and detoxified the LPS micelles with minimal toxicity to normal kidney tubular cells as well as an immortalised kidney cell line. The antimicrobial properties of PMBloaded SDCS nanomicelles were effective against a resistant strain of Pseudomonas aeruginosa.


Assuntos
Ácido Desoxicólico/química , Lipopolissacarídeos/química , Polimixina B/química , Sulfatos/química , Antibacterianos/química , Antibacterianos/farmacologia , Sítios de Ligação , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Ácido Desoxicólico/metabolismo , Resistência Microbiana a Medicamentos/efeitos dos fármacos , Células Epiteliais/citologia , Células Epiteliais/efeitos dos fármacos , Escherichia coli/química , Humanos , Interações Hidrofóbicas e Hidrofílicas , Lipopolissacarídeos/metabolismo , Lipopolissacarídeos/farmacologia , Polimixina B/metabolismo , Polimixina B/farmacologia , Pseudomonas aeruginosa/efeitos dos fármacos , Eletricidade Estática , Sulfatos/metabolismo
3.
J Pharm Sci ; 106(12): 3574-3582, 2017 12.
Artigo em Inglês | MEDLINE | ID: mdl-28847478

RESUMO

This study presents the mode of interaction, structural features, and micellization of amphotericin B (AmB) with sodium deoxycholate sulfate (SDCS) as small lipid molecule at different ratios, as revealed by molecular docking simulations and nuclear magnetic resonance (NMR). AmB-SDCS micelles were synthesized by single pot rinsing method. Solid-state 13C NMR revealed hydrogen (H)-bonding as the main interaction, occurring at different positions between AmB and SDCS at various ratios. Molecular docking elucidated that AmB-SDCS complex was stabilized by multiple H-bonds and van der Waals forces between SDCS and AmB. SDCS molecules wrap around the AmB in a head-to-tail fashion into a nanomicellar structure. AmB-SDCS micelles were stable after freeze-drying and presented zeta potential values between -27.5 and -42.6 mV and particle size in the range of 63.9 to 203.1 nm, upon rehydration in water. Hematological toxicity of AmB was controlled by exposure versus release of drug from SDCS micelles and concentration of SDCS to envelop the drug. Hemolysis of human erythrocytes was significantly reduced as compared to market formulation Fungizone® and pure AmB. This study explained the chemical interaction of micellization of AmB in lipids, which can have greater implications in designing toxicologically safe formulations of hydrophobic drugs.


Assuntos
Anfotericina B/química , Lipídeos/química , Nanopartículas/química , Química Farmacêutica/métodos , Ácido Desoxicólico/química , Portadores de Fármacos/química , Eritrócitos/efeitos dos fármacos , Liofilização , Hemólise/efeitos dos fármacos , Humanos , Interações Hidrofóbicas e Hidrofílicas , Espectroscopia de Ressonância Magnética/métodos , Micelas , Simulação de Acoplamento Molecular/métodos , Tamanho da Partícula
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