Novel biosurfactant and lipid core-shell type nanocapsular sustained release system for intravenous application of methotrexate.
Int J Pharm
; 557: 86-96, 2019 Feb 25.
Article
en En
| MEDLINE
| ID: mdl-30584909
In an attempt to prepare novel core shell nanocapsules, lipid and Stearic acid-Valine conjugate (Biosurfactant) based nanosystem was prepared to attain high drug loading of hydrophilic drug methotrexate (MTX), with sustained release. Antisolvent nanoprecipitation technique was employed for the formulation of nanoparticles (NPs). Optimized formulation depicted 209.6⯱â¯31.3â¯nm particle size, 0.209⯱â¯0.072 PDI and 14.98⯱â¯1.33 %w/w drug loading. In vitro release depicted biphasic release for 12â¯h with initial burst phase followed by sustained release phase. In vitro Haemolytic study on RBCs revealed haemocompatible nature of MTX-Biosurfactant NPs compared to Biotrexate® (Zydus). In vitro cell culture studies showed 3.33 folds and 3.50 folds increase in cellular uptake of MTX at 10⯵g/ml and 15⯵g/ml concentration respectively for developed nanoparticles with 4.16 folds decrease in IC50 value. Higher apoptosis and increased lysosomal membrane permeability were obtained in MTX-Biosurfactants NPs. AUC and T1/2 was found to increase by 2.55 and 3.25 folds respectively in pharmacokinetic study. Significant reduction in tumor burden and serum toxicity marker level depicted efficacy and safety respectively of the formulation as compared to Biotrexate®. RBCs morphology was retained after MTX-Biosurfactants NPs exposure proving its haemocompatibility in vivo.
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MEDLINE
Asunto principal:
Tensoactivos
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Valina
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Metotrexato
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Nanopartículas
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Lípidos
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Antineoplásicos
Idioma:
En
Revista:
Int J Pharm
Año:
2019
Tipo del documento:
Article