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1.
Mol Pharm ; 20(4): 1996-2008, 2023 04 03.
Artículo en Inglés | MEDLINE | ID: mdl-36827081

RESUMEN

Gastric ulcers are a common clinical presentation affecting anyone, regardless of their age or gender. Nanoparticles (NPs) containing Bletilla striata polysaccharide (BSP) and omeprazole (OME) were investigated in the study for their therapeutic effect on gastric ulcers. Ethanol-induced gastric ulcers in rats (240 ± 30 g) were established. Our OME-BSP NPs were more stable than free OME in the acidic environment and can increase the absorption of OME in rat stomach, which was confirmed by in situ gastric absorption and distribution experiments. The extended blood circulation of OME-BSP NPs was also observed in rats with gastric ulcer. More importantly, OME-BSP NPs not only decreased the area of gastric ulcer and inhibited gastric acid secretion but also reversed gastric tissue damage and cell apoptosis, as revealed by HE and TUNEL staining. Subsequent SOD, MDA, PGE2, IL-6, and TNF-α tests further verified the superiority of OME-BSP NPs against rat gastric ulcer, which properly originated from superior antioxidant and anti-inflammatory effects. As a result, our OME-BSP NPs' drug delivery system improved the stability and absorption of OME in the rat stomach and achieved targeted treatment of gastric ulcers.


Asunto(s)
Omeprazol , Úlcera Gástrica , Ratas , Animales , Omeprazol/uso terapéutico , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/tratamiento farmacológico , Etanol/efectos adversos , Polisacáridos/farmacología , Polisacáridos/uso terapéutico
2.
Mol Pharm ; 19(5): 1410-1421, 2022 05 02.
Artículo en Inglés | MEDLINE | ID: mdl-35441510

RESUMEN

This study investigates the protective effect of poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) loaded with scutellarin (SCU), a flavone isolated from the traditional Chinese medicineErigeron breviscapus (Vant.) Hand.-Mazz., in reducing cerebral ischemia/reperfusion (I/R) injury in vivo. The focal cerebral I/R injury model was established by occluding the middle cerebral artery for 1 h in male Sprague-Dawley (SD) rats. Our SCU-PLGA NPs exhibited an extended in vitro release profile and prolonged blood circulation in rats with cerebral ischemia. More importantly, when administered intravenously once a day for 3 days, SCU-PLGA NPs increased the SCU level in the ischemic brain, compared to free SCU, resulting in a significant reduction of the cerebral infarct volume after cerebral I/R. Furthermore, SCU-PLGA NPs reversed the histopathological changes caused by cerebral I/R injury, as well as attenuated cell apoptosis in the brain tissue, as confirmed by hematoxylin and eosin, and TUNEL staining. Our findings have revealed that our injectable SCU-PLGA NPs provide promising protective effects against cerebral I/R injury, which could be used in combination with the existing conventional thrombolytic therapies to improve stroke management.


Asunto(s)
Isquemia Encefálica , Nanopartículas , Daño por Reperfusión , Administración Intravenosa , Animales , Apigenina , Isquemia Encefálica/tratamiento farmacológico , Glucuronatos , Masculino , Ratas , Ratas Sprague-Dawley , Daño por Reperfusión/tratamiento farmacológico , Daño por Reperfusión/prevención & control
3.
Int J Pharm ; 648: 123567, 2023 Dec 15.
Artículo en Inglés | MEDLINE | ID: mdl-37918495

RESUMEN

This study aims to examine the impact of the microfluidic preparation process on the quality of poly (lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) co-delivered with scutellarin (SCU) and paeoniflorin (PAE) in comparison to a conventional emulsification method and to evaluatethe potential cardio-protective effect of SCU-PAE PLGA NPs produced through emulsification method. As compared with microfluidics, the nanoparticles prepared by emulsification method exhibited a smaller size, higher encapsulation efficiency, higher drug loading and lower viscosity for injection. Subsequently, a rat myocardial ischemia (MI) was established using male Sprague-Dawley (SD) rats (250 ± 20 g) subcutaneously injected with 85 mg/kg isoproterenol (ISO) for two consecutive days. The pharmacokinetic findings demonstrated that our SCU-PAE PLGA NPs exhibited prolonged blood circulation time in MI rats, leading to increased levels of SCU and PAE in the heart. This resulted in significant improvements in electrocardiogram and cardiac index, as well as reduced serum levels of CK, LDH, AST. Histopathological analysis using H&E and TUNEL staining provided further evidence of improved cardiac function and decreased apoptosis. Additionally, experiments measuring SOD, MDA, GSH, NO, TNF-α and IL-6 levels indicated that SCU-PAE PLGA NPs may effectively treat MI through oxidative stress and inflammatory pathways, thereby establishing it as a promising therapeutic intervention.


Asunto(s)
Enfermedad de la Arteria Coronaria , Isquemia Miocárdica , Nanopartículas , Ratas , Masculino , Animales , Isoproterenol , Ratas Sprague-Dawley , Isquemia Miocárdica/inducido químicamente , Isquemia Miocárdica/tratamiento farmacológico , Isquemia Miocárdica/prevención & control
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