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1.
ADMET DMPK ; 11(4): 601-613, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37937244

RESUMO

Background and purpose: Wound healing is a biological process that can be difficult to manage clinically. In skin wound healing, the interaction of many cells, growth factors, and cytokines reveals an outstanding biological function mechanism. Wound healing that occurs naturally restores tissue integrity, however, it is usually restricted to wound repair. Curcumin synthesised in a chitosan matrix can be used to heal skin sores. Experimental approach: The ionotropic gelation procedure required crosslinking chitosan with a tripolyphosphate (TPP) crosslinker to generate curcumin nanoparticles encapsulated in chitosan. Key results: The nanoparticles were between 200 and 400 nm in size, with a strong positive surface charge and good entrapment efficacy, according to SEM and TEM investigations. Curcumin and chitosan compatibility was investigated using FTIR spectroscopy. All batches showed consistent drug release, with the F5 batch having the highest curcumin release, at 75% after 16 hours. On L929 cells, scratch assays were utilised to assess wound healing. Wound closure with widths of 59 and 65 mm with curcumin and 45 and 78 mm with curcumin-loaded chitosan nanoparticles was seen after 24 and 48 hours of examination. Conclusions: According to the findings, prepared curcumin chitosan nanoparticles are beneficial in healing skin damage.

2.
Glycoconj J ; 38(2): 261-271, 2021 04.
Artigo em Inglês | MEDLINE | ID: mdl-33687640

RESUMO

Amongst a wide range of biological macromolecules, saccharides exhibit the potential to be specifically recognized by cell-surface receptors and hence can be utilized as ligands in targeted drug delivery. The current study aims to use saccharides viz. Galactose, Pectin and Chitosan to improve targeting of Atenolol by oxalyl chloride mediated grafting. Conjugates were engineered by grafting Atenolol, a cardiovascular agent with the modified saccharide units. The conjugates were characterized by FTIR, DSC and 1H NMR study. Drug release analysis and cellular uptake study was carried out using H9c2 cell lines which represent that concentration of drug in cells treated with all atenolol-saccharide conjugates is enhanced by almost two-folds in comparison with cells treated with atenolol solution. Thus cell line study confers the evidence of selective cardiac delivery. No significant cytotoxicity was observed in case of all synthesized conjugates in the Brine shrimp lethality bioassay. Possible binding of the developed conjugates with the GLUT-4 receptors was assessed by in silico analysis using homology model developed by Swiss Model server. Hence it was concluded that the application of these conjugates with saccharides in selective cardiovascular drug delivery can be a promising approach to increase bioavailability, minimize drug loss by degradation and prevent harmful side effects by increasing specific cell targeting.


Assuntos
Atenolol/química , Atenolol/farmacologia , Portadores de Fármacos/química , Antagonistas de Receptores Adrenérgicos beta 1/química , Antagonistas de Receptores Adrenérgicos beta 1/farmacologia , Animais , Artemia/efeitos dos fármacos , Atenolol/metabolismo , Atenolol/toxicidade , Linhagem Celular , Quitosana/química , Simulação por Computador , Portadores de Fármacos/farmacologia , Portadores de Fármacos/toxicidade , Avaliação Pré-Clínica de Medicamentos , Galactose/química , Transportador de Glucose Tipo 4/química , Transportador de Glucose Tipo 4/metabolismo , Dose Letal Mediana , Espectroscopia de Ressonância Magnética , Miocárdio/citologia , Pectinas/química , Ratos , Espectroscopia de Infravermelho com Transformada de Fourier
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