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1.
AAPS PharmSciTech ; 24(7): 189, 2023 Sep 19.
Artigo em Inglês | MEDLINE | ID: mdl-37726501

RESUMO

The rationale for the current investigation is to study the crude banana peel (CBP) powder efficiency as a novel natural time-dependent polymer along with a pH-sensitive polymer to develop flurbiprofen colon-specific tablets. The direct compression method is utilized to prepare the flurbiprofen-CBP matrix tablets using 9 mm punches on the rotary tableting machine and subsequently coated with Eudragit® S 100 by a dip coating method. The tablets were evaluated for various tableting properties and in vitro drug release studies. From the results of dissolution studies, the F6 formulation showed negligible drug release (5.76% in 5 h) in the upper gastrointestinal tract and progressive release in the colon (99.08% in 24 h). Mean dissolution time, T10%, and T80% were found to be 13.33 h, 5.8 h, and 20.7 h, respectively, which explains the efficiency of the present combination of polymers for colon-specific drug release. From the dissolution studies results of stability studies, the similarity index was calculated and found to be 74.75. In conclusion, utilizing CBP as a natural, time-dependent polymer in conjunction with Eudragit® S 100 to develop the flurbiprofen tablets seems like a promising approach for delivering drugs specifically to the colon.


Assuntos
Flurbiprofeno , Musa , Pós , Colo , Polímeros , Comprimidos
2.
Biomed Pharmacother ; 109: 1454-1461, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30551397

RESUMO

The progressive accumulation of amyloid beta (Aß) peptide is neurotoxic and leads to Alzheimer's type dementia. Accumulation of Aß has been associated with dysfunction of hypothalamic-pituitary-adrenal (HPA) axis and elevated pro-inflammatory cytokines. In this study, we investigated the effect of 1`δ-1`-acetoxyeugenol acetate (DAEA), isolated from Alpinia galanga (L.), on Aß(25-35) induced neurodegeneration in mice. Mice were treated with three different doses of DAEA (12.5 mg/kg, 25 mg/kg and 50 mg/kg) for 28 days. Aß(25-35) was injected by intracerebroventricular (i.c.v.) injection on the 15th day of 28 days. Open field, water maze and step-down inhibitory tests were performed on the 27th day to determine the habituation memory, spatial learning, and short- and long-term memory, respectively. Acetylcholinesterase (AChE), Corticosterone, biogenic amines (serotonin and dopamine), tumour necrosis factor-α (TNF-α), and antioxidant parameters such as superoxide dismutase, catalase, glutathione peroxidase and vitamin C were evaluated in brain homogenates after behavioural tests to ascertain the cognitive improvement through neuro-immune-endocrine modulation. The DAEA treatment with 25 mg/kg and 50 mg/kg resulted in significant (p < 0.001) improvement of habituation memory and step-down inhibitory avoidance task. In spatial learning, the cognitive improvement was significantly improved (p < 0.001) by reduction in escape latency. In the biochemical study, the significant (p < 0.001) reduction of AChE indicates the preeminent neuroprotection. Corticosterone and TNF-α were significantly (p < 0.01) reduced and biogenic amines were increased with antioxidant markers, which signify the potential influence of DAEA on neuroprotection. Our investigation revealed that the drug DAEA attenuates stress mediated through the HPA axis and regulates the neuroendocrine and neuroimmune function to improve the cognition. DAEA could be a potential lead candidate for the treatment of neurodegeneration.


Assuntos
Acetatos/farmacologia , Peptídeos beta-Amiloides/metabolismo , Disfunção Cognitiva/tratamento farmacológico , Eugenol/análogos & derivados , Fármacos Neuroprotetores/farmacologia , Acetilcolinesterase , Animais , Antioxidantes/metabolismo , Biomarcadores/metabolismo , Catalase/metabolismo , Disfunção Cognitiva/metabolismo , Corticosterona/metabolismo , Modelos Animais de Doenças , Eugenol/farmacologia , Glutationa Peroxidase/metabolismo , Masculino , Memória/efeitos dos fármacos , Transtornos da Memória/tratamento farmacológico , Transtornos da Memória/metabolismo , Camundongos , Aprendizagem Espacial/efeitos dos fármacos , Superóxido Dismutase/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
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