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1.
Pharm Dev Technol ; 27(7): 853-863, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-36124550

RESUMO

This study aims to develop, characterize, and examine olanzapine-loaded solid lipid nanocarriers (OLAN-SLNs) for effective brain delivery. OLAN has poor water solubility and low penetration through blood-brain barrier (BBB). Herein, OLAN-SLNs were fabricated using high-pressure homogenization (HPH) method followed by their investigation for particle properties. Moreover, in vitro release and in vivo pharmacokinetics profiles of OLAN-SLNs were compared with pure drug. Anti-psychotic activity was performed in LPS-induced psychosis mice model. Furthermore, expressions of the COX-2 and NF-κB were measured trailed by histopathological examination. The optimized formulation demonstrated nanoparticle size (149.1 nm) with rounded morphology, negative zeta potential (-28.9 mV), lower PDI (0.334), and excellent entrapment efficiency (95%). OLAN-SLNs significantly retarded the drug release and showed sustained release pattern as compared to OLAN suspension. Significantly enhanced bioavailability (ninefold) was demonstrated in OLAN-SLNs when compared with OLAN suspension. Behavioral tests showed significantly less immobility and more struggling time in OLAN-SLNs treated mice group. Additionally, reduced expression of COX-2 and -NF κB in brain was found. Altogether, it can be concluded that SLNs have the potential to deliver active pharmaceutical ingredients to brain, most importantly to enhance their bioavailability and antipsychotic effect, as indicated for OLAN in this study.


Assuntos
Antipsicóticos , Produtos Biológicos , Nanopartículas , Animais , Camundongos , Ciclo-Oxigenase 2 , Preparações de Ação Retardada , Portadores de Fármacos/química , Lanosterol/análogos & derivados , Lipopolissacarídeos , Lipossomos , Nanopartículas/química , NF-kappa B , Olanzapina , Tamanho da Partícula , Suspensões
2.
Neuro Endocrinol Lett ; 41(4): 205-212, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-33307655

RESUMO

AIM: This study was aimed to investigate the effects of sodium benzoate in chronic unpredictable mild stress (CUMS)-induced depression model in rats. MATERIAL AND METHOD: Male rats were exposed to CUMS stress for 6 weeks which includes with multiple unpredictable stressors to induce depression related symptoms and the treatment with sodium benzoate was started at the 4th week of stress protocol (i.e. on the 22nd day) for 21 days during stress protocol . RESULTS: CUMS significantly increased the immobility period in the forced swimming test and decrease sucrose consumption in the sucrose preference test in rats. In the prefrontal cortex region (PFC) of the brain, a significant decline in the Brain-derived neurotrophic factor (BDNF) levels and Protein kinase A (PKA) was observed in rats. However, sodium benzoate (400 and 800 mg/kg i.p.) significantly restored sucrose preference behavior as well as reduced immobility in CUMS-subjected rats in a dose-dependent manner, suggesting the antidepressant potential of sodium benzoate. Also, sodium benzoate treatment significantly increased BDNF levels and PKA activity in the PFC region of the stress subjected rat brain. Moreover, co-administration of H-89, PKA inhibitor (1 and 5 mg/kg) along with sodium benzoate (800 mg/kg) in CUMS subjected rats notably attenuated antidepressant effects of sodium benzoate. H-89 also abolished sodium benzoate-mediated increase in BDNF levels and PKA activity in stress-subjected rats. CONCLUSION: Sodium benzoate mediated antidepressant actions may be due to a decrease in the d-amino oxidase activity, an increase in BDNF, and PKA levels in PFC region of the brain. Sodium benzoate-mediated modulation of BDNF/PKA signaling may contribute to attenuating depressive-symptoms in unpredictable stress-subjected rats.


Assuntos
Depressão , Transtorno Depressivo , Animais , Antidepressivos/farmacologia , Antidepressivos/uso terapêutico , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Depressão/tratamento farmacológico , Depressão/etiologia , Transtorno Depressivo/tratamento farmacológico , Transtorno Depressivo/etiologia , Modelos Animais de Doenças , Hipocampo/metabolismo , Masculino , Ratos , Benzoato de Sódio , Estresse Psicológico/complicações , Estresse Psicológico/tratamento farmacológico
3.
Appl Opt ; 59(10): 3093-3096, 2020 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-32400590

RESUMO

A dual-fiber point diffraction interferometer is built to measure the wavefront aberration of an imaging system with high precision. The optical intensity of the test light and reference light are controlled independently, so that high interference contrast can be obtained. The interferometer has several advantages: high precision, a flexible structure, and a quasi-common optical path. System errors of the interferometer that influence the measurement accuracy are considered and calibrated. In the experiments, a projection lens with numerical aperture of 0.3 is measured. The measured wavefront error is 1.5 nm rms, and the measurement repeatability is 35 pm rms.

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