scholarly journals Evaluation of Quetiapine Fumarate and its Solid Lipid Nanoparticles as antipsychotic drug in rat model of schizophrenia

2017 ◽  
Vol 4 (08) ◽  
pp. 1480 ◽  
Author(s):  
Said M. M. ◽  
Gehan A. Elmenoufy
Keyword(s):  
Side Effects ◽  
Rat Model ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Brain Regions ◽  
Control Group ◽  
High Dose ◽  
Dependent Manner ◽  
Quetiapine Fumarate ◽  
Solid Lipid

Background: The present study compares the efficacy of quetiapine fumarate (QF) and QF-loaded solid lipid nanoparticles (QFSLN) as antipsychotic drugs for schizophrenia. Methods: To induce schizophrenia-like symptoms, a group of rats was injected intraperitoneally (i.p.) with ketamine (25mg/kg b.w.) for 1 week to establish a rat model of schizophrenia. The incidence of schizophrenic symptoms was estimated to be equivalent to the control group. To estimate the pronounced antipsychotic effect of QF, a low dose (LD) of 10 mg/kg b.w. and a high dose (HD) of 30 mg /kg b.w. were orally administrated to two groups of rats (designated L.QF and H.QF) for 3 weeks (2 weeks without ketamine injection; the last week with ketamine). To achieve the optimal therapeutic response of QF drug, 2 other groups of rats were administered orally the equivalent low and high doses of QF in its solid lipid nanoparticle form (L.QFSLN) and (H.QFSLN) for 3 weeks in the same manner. The treatments were given after 1 h of ketamine injection. To assess the effect of different doses of treatment on hyperlocomotion and cognitive impairment induced by ketamine, an open field test and passive avoidance test were conducted. In addition, excitatory and inhibitory amino acids, as well as catecholamines, were estimated in brain regions (cortex and hippocampus). The study was extended to estimate the side effects of different treatments on hepatorenal functions and lipid profile. Additionally, samples were subjected to immunohistochemical analysis. Results: QFSLN treatment showed enhanced effect over QF in a dose-dependent manner with minimal side effects in schizophrenic rats. In addition, immunohistochemical examinations of brain tissues confirmed the biochemical data.

The Effect of Minor Doses of Olanzapine-Solid Lipid Nanoparticles on an Animal Model of Schizophrenia (Neurochemical and Behavioral Study) and the Side Effect

2019 ◽  
Vol 9 (4) ◽  
pp. 308-320
Author(s):  
Areeg Abd-Elrazek ◽  
Tayseer Elnawawy
Keyword(s):  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Brain Regions ◽  
Free Form ◽  
High Dose ◽  
Solid Lipid ◽  
The Brain ◽  
Different Doses

Background and Objective:Olanzapine (OLZ) is an atypical psychotic agent; the poor bioavailability of olanzapine is the most important issue in its treatment. The present work was carried out to evaluate the oral form of olanzapine solid lipid nanoparticles (OLZ-SLN) to overcome its poor bioavailability and compare between the effect of different doses of OLZ and OLZ-SLN on ketamineinduced schizophrenic-like symptoms. The study was extended to evaluate the adverse effects of subchronic administration of these doses of OLZ and its SLN.Methods:OLZ-SLN was prepared by hot homogenization, particle size, zeta potential and in vitro release and entrapping efficiency studies were performed. In order to assess the effective dose in the treatment of schizophrenia, the effect of different doses of OLZ and OLZ-SLN on open field was assessed and passive avoidance tests were carried out. The test was performed to examine the effects of excitatory and inhibitory amino acids, as well as dopamine and serotonin levels in the brain regions.Results and Conclusion:The new oral formula showed high stability and sustained release. The administration of low and high dose of OLZ-SLN equivalent to (1/10 and 1/20 from the therapeutic dose before ketamine attenuated the behavioral abnormalities by blocking the effect of ketamine-induced increase in glutamate, dopamine and serotonin levels and enhanced apoptosis were studied in the brain areas. In addition, the sub-chronic treatment with OLZ-SLN showed no adverse effect while the treatment with OLZ free form did.

Antileishmanial activity of conventional and solid lipid nanoparticles of Amphotericin B on Leishmania major

2019 ◽  
Vol 19 ◽  
Author(s):  
Shahrzad Soltani ◽  
Hoda Mojiri -Forushani ◽  
Sheyda Soltani ◽  
Mehdi Sagha Kahvaz ◽  
Masoud Foroutan
Keyword(s):  
Amphotericin B ◽  
Solid Lipid Nanoparticles ◽  
Leishmania Major ◽  
Colorimetric Assay ◽  
Lipid Nanoparticles ◽  
Antileishmanial Activity ◽  
Control Group ◽  
Dependent Manner ◽  
Solid Lipid

Background: Obligate intracellular parasites of Leishmania genus belong to family Trypanosomatidae and more than twenty species causes this neglected vector-borne infection throughout the globe. The current study was aimed to assess the antileishmanial activity of Amphotericin B (AmB) and AmB formulated into solid lipid nanoparticles (SLNs) in vitro and in vivo. Materials and methods: In the present research, microemulsification and high shear homogenization methods were used to prepare SLNs. Leishmania major (L. major) promastigotes were cultured in RPMI 1640 and incubated for three time points of 24, 48 and 72 h at 25±1°C. Then, the MTT colorimetric assay was employed for obtaining of 50% inhibitory concentration (IC50). Finally, we evaluated the efficacy of AmB and AmB-SLN for the treatment of experimental cutaneous leishmaniasis (CL) in BALB/c mice. Results: The average diameter sizes of prepared AmB-SLN were <180 nm and monodisperse preparations with polydispersity index 0.21±0.29. The antileishmanial activity of AmB and AmB-SLN revealed a dose and time-dependent manner in vitro. The IC50 values of AmB (38.18±1.33, 25.06±2.00, and 13.87±0.61 μg/ml) and AmB-SLN (0.40±0.02, 0.26±0.02, and 0.14±0.01 μg/ml) were estimated after 24, 48 and 72 hours, respectively. In all BALB/c treatment groups, the diameter of lesions were significantly smaller than the control group. Conclusion: Discovery of new effective drugs based on nanocarriers, such as SLN, is practical and opens a new window for the treatment of CL. More studies are needed in the future.

Enhanced Oral Absorption of All-trans Retinoic Acid upon Encapsulation in Solid Lipid Nanoparticles

2020 ◽  
Vol 8 (6) ◽  
pp. 495-510
Author(s):  
Manoj Kumar ◽  
Garima Sharma ◽  
Dinesh Singla ◽  
Sukhjeet Singh ◽  
Vandita Kakkar ◽  
...  
Keyword(s):  
Retinoic Acid ◽  
Side Effects ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Trans Retinoic Acid ◽  
All Trans Retinoic Acid ◽  
Vitro Release

Background:: All-trans retinoic acid (ATRA) is widely employed in the treatment of various proliferative and inflammatory diseases. However, its therapeutic efficacy is imperiled due to its poor solubility and stability. Latter was surmounted by its incorporation into a solid matrix of lipidic nanoparticles (SLNs). Methods:: ATRA loaded SLNs (ATRA-SLNs) were prepared using a novel microemulsification technique (USPTO 9907758) and an optimal composition and were characterized in terms of morphology, differential scanning calorimetry (DSC), and powder X-ray diffraction studies (PXRD). In vitro release, oral plasma pharmacokinetics (in rats) and stability studies were also done. Results:: Rod-shaped ATRA-SLNs could successfully incorporate 3.7 mg/mL of ATRA, increasing its solubility (from 4.7 μg/mL) by 787 times, having an average particle size of 131.30 ± 5.0 nm and polydispersibility of 0.283. PXRD, DSC, and FTIR studies confirmed the formation of SLNs. Assay/total drug content and entrapment efficiency of ATRA-SLNs was 92.50 ± 2.10% and 84.60 ± 3.20% (n=6), respectively, which was maintained even on storage for one year under refrigerated conditions as an aqueous dispersion. In vitro release in 0.01 M phosphate buffer (pH 7.4) with 3% tween 80 was extended 12 times from 2h for free ATRA to 24 h for ATRA-SLNs depicting Korsmeyer Peppas release. Oral administration in rats showed 35.03 times enhanced bioavailability for ATRA-SLNs. Conclusion:: Present work reports preparation and evaluation of bioenhanced ATRA-SLNs containing a high concentration of ATRA (>15 times than that reported by others). Latter is attributed to the novel preparation process and intelligent selection of components. Lay Summary: All-trans retinoic acid (ATRA) shows an array of pharmacological activities but its efficacy is limited due to poor solubility, stability and side effects. In present study its solubility and efficacy is improved by 787 and 35.5 times, respectively upon incorporation into solid lipid nanoparticles (ATRA-SLNs). Latter extended its release by 12 times and provided stability for at least a year under refrigeration. A controlled and sustained release will reduce dose related side effects. ATRA-SLNs reported presently can thus be used in treatment /prophylaxis of disorders like cancers, tuberculosis, age related macular degeneration and acne and as an immune-booster.

Nephrotoxicity of Albendazole and Albendazole-Loaded Solid Lipid Nanoparticles in Mice with Experimental Hydatidosis

2021 ◽  
Author(s):  
Kobra Kohansal ◽  
Abdollah Rafiei ◽  
Heibatullah Kalantari ◽  
Ali Jelowdar ◽  
Anayatollah Salimi ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Physicochemical Characterization ◽  
Public Health Problem ◽  
New Product ◽  
Lipid Nanoparticles ◽  
Control Group ◽  
Histopathological Study ◽  
Normal Range ◽  
Solid Lipid

Purposes: Cystic echinococcosis (CE) is a serious contemporary public health problem. Different CE treatment methods are of considerable importance, with albendazole (ABZ) being one of the most preferred drugs for CE treatment and prophylaxis. In this study, we evaluated the nephrotoxicity caused by ABZ and ABZ-loaded solid lipid nanoparticles (SLNs) in mice with experimental hydatid cyst. Methods: ABZ-loaded SLNs were produced by micro-emulsification and a high shear homogenization technique. Thereafter, we evaluated the physicochemical characterization of the product. Live protoscolices were injected into mice to induce experimental hydatidosis. Mice were then treated with ABZ and ABZ-loaded SLNs. The nephrotoxicity effects were evaluated by biochemical and histopathological surveys. Results: Significantly different blood urea nitrogen (BUN) levels were observed between the two infected groups (ABZ treatment and ABZ-loaded SLN treatment) and the control group. The kidney malondialdehyde (MDA) and glutathione (GSH) levels of the infected groups were not significantly different from those of the control group. The histopathological study revealed nephropathic and pathologic changes in the ABZ and ABZ-loaded SLN groups. Conclusion: ABZ formulated for ABZ-loaded SLNs had a more prominent chemoprophylactic efficacy on CE and fewer side effects than ABZ alone. Neither ABZ nor ABZ-loaded SLNs caused significant biochemical and histopathological defects on the kidney, and all functional biochemical markers stayed within the normal range. Therefore, ABZ-loaded SLNs could be a potential new product for CE treatment.

scholarly journals Development of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers of Loteprednol Etabonate: Physicochemical Characterization and Ex Vivo Permeation Studies

2021 ◽  
Author(s):  
Burcu Üner ◽  
Samet Özdemir ◽  
Çetin Taş ◽  
Yıldız Özsoy ◽  
Melike Üner
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Physicochemical Characterization ◽  
Lipid Nanoparticles ◽  
Nanostructured Lipid Carriers ◽  
Fickian Diffusion ◽  
Control Group ◽  
Loteprednol Etabonate ◽  
Solid Lipid

Abstract Purpose Loteprednol etabonate (LE) is a new generation corticosteroid that is used for the treatment of inflammatory and allergic conditions of the eye, and management of seasonal allergic rhinitis nasally. LE which is a poorly soluble drug with insufficient bioavailability, has a high binding affinity to steroid receptors. Sophisticated colloidal drug delivery systems of LE could present an alternative for treatment of inflammatory and allergic conditions of the skin. For this purpose, solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were attempted to improve for transdermal LE delivery for the first time. Methods SLN and NLC were produced by hot homogenization and ultrasonication technique. Formulations were characterized by dynamic light scattering, scanning electron microscopy, fourier transform infrared spectroscopy and differential scanning calorimetry. Their physical stability was monitored for 3 months of storage. Drug release profiles and permeation properties of SLN and NLC through the porcine skin were investigated. Results It was determined that SLN and NLC below 150 nm particle size had a homogeneous particle size distribution as well as high drug loading capacities. They were found to be stable both physically and chemically at room temperature for 90 days. In terms of release kinetics, it was determined that they released from SLN and NLC in accordance with Fickian diffusion release. Formulations prepared in this study were seen to significantly increase drug penetration through pig skin compared to the control group (p ≤ 0.05). Conclusion SLN and NLC formulations of LE can be stated among the systems that can be an alternative to conventional systems with less side-effect profile in the treatment of inflammatory problems on the skin.

scholarly journals Antineuroinflammatory Activities and Neurotoxicological Assessment of Curcumin Loaded Solid Lipid Nanoparticles on LPS-Stimulated BV-2 Microglia Cell Models

Molecules ◽  
2019 ◽  
Vol 24 (6) ◽  
pp. 1170 ◽  
Author(s):  
Palanivel Ganesan ◽  
Byungwook Kim ◽  
Prakash Ramalingam ◽  
Govindarajan Karthivashan ◽  
Vishnu Revuri ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Brain Cells ◽  
No Production ◽  
Dependent Manner ◽  
Microglia Cell ◽  
Solid Lipid ◽  
Cytokine Levels ◽  
The Central Nervous System ◽  
Dose Dependent

Curcumin, which is a potential antineuroinflammatory and neuroprotective compound, exhibits poor bioavailability in brain cells due to its difficulty in crossing the blood–brain barrier and its rapid metabolism during circulation, which decreases its efficacy in treating chronic neuroinflammatory diseases in the central nervous system. The bioavailability and potential of curcumin can be improved by using a nanodelivery system, which includes solid lipid nanoparticles. Curcumin-loaded solid lipid nanoparticles (SLCN) were efficiently developed to have a particle size of about 86 nm and do not exhibit any toxicity in the endothelial brain cells. Furthermore, the curcumin-loaded solid lipid nanoparticles (SLCN) were studied to assess their efficacy in BV-2 microglial cells against LPS-induced neuroinflammation. The SLCN showed a higher inhibition of nitric oxide (NO) production compared to conventional curcumin in a dose-dependent manner. Similarly, the mRNA and proinflammatory cytokine levels were also reduced in a dose-dependent manner when compared to those with free curcumin. Thus, SLCN could be a potential delivery system for curcumin to treat microglia-mediated neuroinflammation.

scholarly journals Formulation and Development of Transferrin Targeted Solid Lipid Nanoparticles for Breast Cancer Therapy

2020 ◽  
Vol 11 ◽  
Author(s):  
Geeta S. Bhagwat ◽  
Rajani B. Athawale ◽  
Rajeev P. Gude ◽  
Shadab Md ◽  
Nabil A. Alhakamy ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Solid Lipid Nanoparticles ◽  
Human Breast Cancer ◽  
Lipid Nanoparticles ◽  
Dependent Manner ◽  
Human Breast ◽  
Solid Lipid ◽  
Receptor Modulation ◽  
Tamoxifen Citrate ◽  
Mcf 7

Breast cancer is conventionally treated by surgery, chemotherapy and radiation therapy followed by post operational hormonal therapy. Tamoxifen citrate is a best option to treat breast cancer because its selective estrogen receptor modulation activity. Owing to its antiestrogenic action on breast as well as uterine cells, Tamoxifen citrate shows uterine toxicity. The dose 20 mg per day of Tamoxifen citrate required to show therapeutic effect causes side effects and toxicity to vital organs such as liver, kidney and uterus. In the present study, transferrin-conjugated solid lipid nanoparticles (SLNs) were successfully prepared to enhance the active targeting of tamoxifen citrate in breast cancer. Developed formulations were evaluated for particle size, surface charge, surface morphology and in vitro dissolution studies. Developed formulations exhibited more cytotoxicity as compared to pure Tamoxifen citrate solution in time as well as concentration dependent manner on human breast cancer MCF-7 cells. Further, cell uptake and flow cytometry studies confirmed the qualitative uptake of developed D-SLN and SMD-SLN by human breast cancer MCF-7 cells. Overall, proposed study highlights that transferrin engineered nanocarriers could enhance the therapeutic response of nanomedicines for breast cancer treatment.

Improvement of memory deficits in the rat model of Alzheimer's disease by erythropoietin-loaded solid lipid nanoparticles

2019 ◽  
Vol 166 ◽  
pp. 107082 ◽  
Author(s):  
Tahereh Dara ◽  
Alireza Vatanara ◽  
Mohammad Sharifzadeh ◽  
Samira Khani ◽  
Molood Alsadat Vakilinezhad ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Rat Model ◽  
Solid Lipid Nanoparticles ◽  
Memory Deficits ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Model Of Alzheimer’S Disease
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