Nanoliposomal Encapsulation Enhances In Vivo Anti-Tumor Activity of Niclosamide against Melanoma

2019 ◽  
Vol 19 (13) ◽  
pp. 1618-1626 ◽  
Author(s):  
Mahdi Hatamipour ◽  
Mahmoud R. Jaafari ◽  
Amir A. Momtazi-Borojeni ◽  
Mahin Ramezani ◽  
Amirhossein Sahebkar
Keyword(s):  
Particle Size ◽  
Aqueous Solubility ◽  
In Vivo Studies ◽  
Size Analysis ◽  
Parasitic Infections ◽  
B16f10 Melanoma ◽  
Melanoma Tumor ◽  
Anti Tumor Activity

Background: Niclosamide is an FDA-approved and old anti-helminthic drug used to treat parasitic infections. Recent studies have shown that niclosamide has broad anti-tumor effects relevant to the treatment of cancer. However, this drug has a low aqueous solubility hindering its systemic use. Herein, we report the preparation and characterization of niclosamide nanoliposomes and their in vivo anti-tumor effects. Methods: Nanoliposomes were prepared using thin-film method and the drug was encapsulated with a remote loading method. The nanoliposomes were investigated by the observation of morphology, analysis of particle size and zeta potential. Additionally, qualitative and quantitative analyses were performed using HPLC. We assessed the in vitro cytotoxicity of the nanoliposomal niclosamide on B16F10 melanoma cells. Inhibition of tumor growth was investigated in C57BL/6 mice bearing B16F0 melanoma cancer. Results: Analytical results indicated that the nanoliposomal system is a homogeneous and stable colloidal dispersion of niclosamide particles. Atomic force microscopy images and particle size analysis revealed that all niclosamide particles had a spherical shape with a diameter of approximately 108nm. According to in vitro and in vivo studies, nanoliposomal niclosamide exhibited a better anti-tumor activity against B16F10 melanoma tumor compared with free niclosamide. Conclusion: Nanoliposomal encapsulation enhanced the aqueous solubility of niclosamide and improved its anti-tumor properties.

scholarly journals In vitro and in vivo Evaluation of Ibuprofen Nanosuspensions for Enhanced Oral Bioavailability

2021 ◽  
Author(s):  
Mohsen Hedaya ◽  
Farzana Bandarkar ◽  
Aly Nada
Keyword(s):  
Particle Size ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
In Vivo Evaluation ◽  
Poorly Soluble ◽  
Extent Of Absorption ◽  
Better Than

Introduction: The objectives were to prepare, characterize and in vivo evaluate different ibuprofen (IBU) nanosuspensions prepared by ultra-homogenization, after oral administration to rabbits. Methods: The nanosuspensions produced by ultra-homogenization were tested and compared with a marketed IBU suspension for particle size, in vitro dissolution and in vivo absorption. Five groups of rabbits received orally 25 mg/kg of IBU nanosuspension, nanoparticles, unhomogenized suspension, marketed product and untreated suspension. A sixth group received 5 mg/kg IBU intravenously. Serial blood samples were obtained after IBU administration. Results: The formulated nanosuspensions showed significant decrease in particle size. Polyvinyl Pyrrolidone K30 (PP) was found to improve IBU aqueous solubility much better than the other tested polymers. Addition of Tween 80 (TW), in equal amount as PP (IBU: PP:TW, 1:2:2 w/w) resulted in much smaller particle size and better dissolution rate. The Cmax achieved were 14.8±1.64, 11.1±1.37, 9.01±0.761, 7.03±1.38 and 3.23±1.03 μg/ml and the tmax were 36±8.2, 39±8.2, 100±17.3, 112±15 and 105±17 min for the nanosuspension, nanoparticle, unhomogenized suspension, marketed IBU suspension and untreated IBU suspension in water, respectively. Bioavailability of the different formulations relative to the marketed suspension were the highest for nanosuspension> unhomogenized suspension> nanoparticles> untreated IBU suspension. Conclusion: IBU/PP/TW nanosuspensions showed enhanced in vitro dissolution as well as faster rate and higher extent of absorption as indicated from the higher Cmax, shorter tmax and larger AUC. The in vivo data supported the in vitro results. Nanosuspensions prepared by ultra-high-pressure-homogenization technique can be used as a good formulation strategy to enhance the rate and extent of absorption of poorly soluble drugs.

scholarly journals Progress to Improve Oral Bioavailability and Beneficial Effects of Resveratrol

2019 ◽  
Vol 20 (6) ◽  
pp. 1381 ◽  
Author(s):  
Adele Chimento ◽  
Francesca De Amicis ◽  
Rosa Sirianni ◽  
Maria Sinicropi ◽  
Francesco Puoci ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Aqueous Solubility ◽  
In Vivo Studies ◽  
Beneficial Effects ◽  
Lipid Nanocarriers ◽  
Methodological Approaches ◽  
Neuroprotective Actions ◽  
Synthetic Derivatives

Resveratrol (3,5,4′-trihydroxystilbene; RSV) is a natural nonflavonoid polyphenol present in many species of plants, particularly in grapes, blueberries, and peanuts. Several in vitro and in vivo studies have shown that in addition to antioxidant, anti-inflammatory, cardioprotective and neuroprotective actions, it exhibits antitumor properties. In mammalian models, RSV is extensively metabolized and rapidly eliminated and therefore it shows a poor bioavailability, in spite it of its lipophilic nature. During the past decade, in order to improve RSV low aqueous solubility, absorption, membrane transport, and its poor bioavailability, various methodological approaches and different synthetic derivatives have been developed. In this review, we will describe the strategies used to improve pharmacokinetic characteristics and then beneficial effects of RSV. These methodological approaches include RSV nanoencapsulation in lipid nanocarriers or liposomes, nanoemulsions, micelles, insertion into polymeric particles, solid dispersions, and nanocrystals. Moreover, the biological results obtained on several synthetic derivatives containing different substituents, such as methoxylic, hydroxylic groups, or halogens on the RSV aromatic rings, will be described. Results reported in the literature are encouraging but require additional in vivo studies, to support clinical applications.

scholarly journals Preparation and preclinical evaluation of aceclofenac loaded pectinate mucoadhesive microspheres

2012 ◽  
Vol 2 (1) ◽  
pp. 8 ◽  
Author(s):  
Santanu Chakraborty ◽  
Priyanka Nayak ◽  
Bala Murali Krishna ◽  
Madhusmruti Khandai ◽  
Ashoke Kumar Ghosh
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Polymer Concentration ◽  
Research Work ◽  
In Vivo Studies ◽  
Systemic Absorption ◽  
Cross Linking ◽  
Significant Difference

The aim of the present research work was to fabricate aceclofenac loaded pectinate microspheres by ionic gelation method and evaluate the effect of different cross-linking agents and polymer concentration on particle size, encapsulation efficacy and drug release behavior. It was also investigated that whether this pectinate dosage form was able to target the drug release in intestinal region and prevent the different side effect associated with the drug in stomach or not. It was observed that particle size, encapsulation efficacy and in vitro drug release were largely depended on polymer concentration and cross-linking agents. It was also observed that pectinate microspheres showed excellent pH depended mucoadhesive properties and they were able to restrict the drug release in stomach. <em>In vitro</em> drug release study showed that alminium-pectinate microspheres have more sustaining property as compared to barium-pectinate microspheres. Holm-Sidak multiple comparison analysis suggested a significant difference in measured t<sub>50%</sub> values among all the formulations with same cross-linking agent. In vivo studies revealed that the anti inflammatory and analgesic effects induced by pectinate microspheres were significantly high and prolonged as compared to pure drug. So, pectinate microspheres can be an excellent carrier for targeting the delivery of aceclofenac as well as help in improving the patient compliance by prolonging the systemic absorption.

Garcinol-loaded novel cationic nanoliposomes: in vitro and in vivo study against B16F10 melanoma tumor model

Nanomedicine ◽  
2019 ◽  
Vol 14 (15) ◽  
pp. 2045-2065 ◽  
Author(s):  
Brahamacharry Paul ◽  
Raghuvir H Gaonkar ◽  
Ria Mukhopadhyay ◽  
Shantanu Ganguly ◽  
Mita Chatterjee Debnath ◽  
...  
Keyword(s):  
Chromatin Condensation ◽  
Xenograft Model ◽  
Tumor Model ◽  
Tumor Xenograft ◽  
B16f10 Melanoma ◽  
Melanoma Tumor ◽  
Study Gene Expression ◽  
The Difference

Aim: Garcinol (GAR)-loaded cationic nanoliposomes were developed to achieve potential antitumor efficacy on B16F10 melanoma cells in vitro and in vivo. Materials & methods: Two different phospholipids namely, distearoyl phosphatidylcholine (DSPC) and dipalmitoyl phosphatidylcholine (DPPC) were used in formulation to elucidate the difference in cellular uptake, cytotoxicity, in vivo tumor uptake (by scintigraphic imaging after technetium-99m radiolabeling) and therapeutic efficacy. Results: Different in vitro protocols, for example, MTT assay, apoptosis study, gene expression analysis, chromatin condensation and cytoskeleton breakdown analysis in B16F10 cell lines as well as scintigraphic analysis and tumor inhibition studies (B16F10 tumor xenograft model) revealed superiority of GAR-DPPC than GAR-DSPC and free GAR in melanoma prevention. Conclusion: Cationic nanoliposomal formulations could be a future medication for skin cancer treatment.

scholarly journals In Silico, in Vitro and in Vivo Investigation of a Newly Synthesized Ionic Compound As Anti-Alzheimer Multi-Target Dual AChE/BuChE Inhibitor Possessing Neuro-Protective Effects Against Aβ Induced Neurotoxicity in PC12 Cells and Alzheimer Rat Model

2021 ◽  
Author(s):  
Hosna Karami ◽  
somaieh soltani ◽  
Gerhard Wolber ◽  
Saeed Sadigh-Eteghad ◽  
Roghaye Nikbakht ◽  
...  
Keyword(s):  
Pc12 Cells ◽  
Quaternary Ammonium ◽  
Aqueous Solubility ◽  
In Vivo Studies ◽  
Protective Effects ◽  
Rat Models ◽  
Tnf Α ◽  
Neuro Inflammation

Abstract Multi-target anti Alzheimer’s disease (AD) compounds are promising leads for the development of AD modifying agents. Ionic compounds containing quaternary ammonium moiety were synthesized and their multi-targeted anti-AD effects were examined in the current study. Compound 5g possessed suitable aqueous solubility and cell toxicity. It also showed non-competitive dual hAChE/hBuChE inhibition activity. Compound 5g reversed the Aβ-treated PC12 cells’ morphology alteration and reduced PC12 cells’ death. Compound 5g possessed anti-oxidative stress activity through anti-oxidant, anti-ROS production and anti-lipid peroxidation mechanisms. It also reduced the expression of IL-1β and TNF-α genes. Furthermore, compound 5g LDH inhibition, reduction of neuro-inflammation and prevention of autophagy-apoptosis were approved by the results of in vitro studies. Compound 5g delivery to brain was confirmed by in vivo studies. Administration of compound 5g to Aβ-induced AD rat models improved their cognition function and spatial memory learning behavior. TNF-α and NFkB down-regulated in compound 5g treated AD rats’ hippocamp. Besides, compound 5g reversed the up-regulation of AChE in Aβ treated rats’ hippocamp. Molecular modeling studies confirmed the interaction of compound 5g with both steric and catalytic sites of ChE enzymes. The newly synthesized quaternary ammonium containing derivative (compound 5g) possessed multi-target anti-AD efficacy based on in vitro and in vivo studies and its efficacy in AD rat models were approved by behavioral and molecular investigations.

Evaluation of the Anti-Tumor Activity of Niclosamide Nanoliposomes Against Colon Carcinoma

2020 ◽  
Vol 13 (3) ◽  
pp. 245-250
Author(s):  
Mahdi Hatamipour ◽  
Mahmoud R. Jaafari ◽  
Amir A. Momtazi-Borojeni ◽  
Mahin Ramezani ◽  
Amirhossein Sahebkar
Keyword(s):  
Tumor Growth ◽  
Experimental Model ◽  
Colon Carcinoma ◽  
Carcinoma Cells ◽  
In Vivo Studies ◽  
Colon Carcinoma Cells ◽  
Ct26 Colon Carcinoma ◽  
Anti Tumor Activity

Background and Aims: Niclosamide is an established anti-helminthic drug, which has recently been shown to inhibit the growth of various cancer cells. To exploit the potential anti-tumor activity of this drug for systemic use, the problem of low aqueous solubility should be addressed. The present study tested the in vivo anti-tumor effects of a recently developed nanoliposomal preparation of niclosamide in an experimental model of colon carcinoma. Methods : The cytotoxicity of nanoliposomal niclosamide on CT26 colon carcinoma cells was evaluated using the MTT test. Inhibition of tumor growth was investigated in BALB/c mice bearing CT26 colon carcinoma cells. The animals were randomly divided into 4 groups including: 1) untreated control, 2) liposomal doxorubicin (15 mg/kg; single intravenous dose), 3) liposomal niclosamide (1 mg/kg/twice a week; intravenously for 4 weeks), and 4) free niclosamide (1 mg/kg/twice a week; intravenously for 4 weeks). To study therapeutic efficacy, tumor size and survival were monitored in 2-day intervals for 40 days. Results: In vitro results indicated that nanoliposomal and free niclosamide could exert cytotoxic effects with IC50 values of 4.5 and 2.5 μM, respectively. According to in vivo studies, nanoliposomal niclosamide showed a higher growth inhibitory activity against CT26 colon carcinoma cells compared with free niclosamide as revealed by delayed tumor growth and prolongation of survival. Conclusion : Nnaoliposomal encapsulation enhanced anti-tumor properties of niclosamide in an experimental model of colon carcinoma.

Anti-Tumor Efficacy of Pyrvinium Pamoate Nanoliposomes in an Experimental Model of Melanoma.

2021 ◽  
Vol 21 ◽  
Author(s):  
Mahdi Hatamipour ◽  
Mahmoud R. Jaafari ◽  
Mahtab Zangui ◽  
Neda Shakour ◽  
Amirhossein Sahebkar
Keyword(s):  
Particle Size ◽  
Colloidal Suspension ◽  
Drug Carriers ◽  
In Vitro Cytotoxicity ◽  
In Vivo Studies ◽  
Tumor Growth Inhibition ◽  
Proliferative Potential ◽  
Pyrvinium Pamoate

Background: Pyrvinium pamoate (PP) is an old drug approved by the FDA for the treatment of pinworm infections. Recently, PP has been introduced as an antitumor agent. However, low aqueous solubility severely limits its potential effects. In this study, we developed a liposomal formulation of pyrvinium pamoate to investigate its in vitro cytotoxicity and in vivo efficacy against melanoma cells. Materials & Methods: As drug carriers, liposomes were fabricated using thin-film method. PP was encapsulated within liposomes using remote loading method. We evaluated morphology, particle size, and Zeta potential of the liposomes. Additionally, high-performance liquid chromatography (HPLC) was employed for qualitative and quantitative analysis. Then we investigated our liposomal PP for its in vitro cytotoxicity as well as the tumor growth inhibition in C57BL/6 mice bearing B16F0 melanoma tumors. Results: Based on the analytical result, the liposomal drug delivery system is a homogeneous and stable colloidal suspension of PP particles. Images of Atomic force microscopy and particle size data showed that all the prepared nanocarrier were spherical with a diameter of approximately 101 nm. According to both in vitro and in vivo studies, nanoliposomal PP exhibited an improved anti-proliferative potential against B16F10 melanoma tumor compared with free PP. Conclusion: Liposomal encapsulation improves water solubility of PP and enhances its anti-cancer activity.

Sonodynamic cancer therapy by a nickel ferrite/carbon nanocomposite on melanoma tumor: In vitro and in vivo studies

2019 ◽  
Vol 27 ◽  
pp. 27-33 ◽  
Author(s):  
M. Gorgizadeh ◽  
N. Azarpira ◽  
M. Lotfi ◽  
F. Daneshvar ◽  
F. Salehi ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Nickel Ferrite ◽  
In Vivo Studies ◽  
Melanoma Tumor ◽  
Carbon Nanocomposite

In vitro and in vivo studies on the cytotoxicity of irradiated silk fibroin against mouse melanoma tumor cell

2009 ◽  
Vol 78 (7-8) ◽  
pp. 429-431 ◽  
Author(s):  
Eui-Baek Byun ◽  
Nak-Yun Sung ◽  
Sun-Kyu Kwon ◽  
Beom-Seok Song ◽  
Jae-Hun Kim ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Silk Fibroin ◽  
In Vivo Studies ◽  
Melanoma Tumor ◽  
Mouse Melanoma

scholarly journals Pharmaceutical Characterization and In Vivo Evaluation of Orlistat Formulations Prepared by the Supercritical Melt-Adsorption Method Using Carbon Dioxide: Effects of Mesoporous Silica Type

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 333 ◽  
Author(s):  
Heejun Park ◽  
Kwang-Ho Cha ◽  
Seung Hyeon Hong ◽  
Sharif Md Abuzar ◽  
Seungyeol Lee ◽  
...  
Keyword(s):  
Carbon Dioxide ◽  
Particle Size ◽  
Side Effects ◽  
Mesoporous Silica ◽  
Dissolution Rate ◽  
Lipase Activity ◽  
Pore Volume ◽  
In Vivo Studies

Orlistat, an anti-obesity drug, has two critical issues—the first is its low efficacy due to low water solubility and the second is side effects such as oily spotting due to its lipase inhibition. The present study was designed to propose a solution using a formulation with mesoporous silica to simultaneously overcome two issues. Orlistat was loaded onto mesoporous silica by the supercritical melt-adsorption (SCMA) method, using carbon dioxide (CO2). Various types of mesoporous silica were used as adsorbents, and the effects of the pore volume, diameter and particle size of mesoporous silica on the pharmaceutical characteristics were evaluated by various solid-state characterization methods and in vitro and in vivo studies in relation to pharmacological efficacy and the improvement of side effects. The results showed that the pore volume and diameter determine loadable drug amount inside pores and crystallinity. The dissolution was significantly influenced by crystallinity, pore diameter and particle size, and the inhibition of lipase activity was in proportion to the dissolution rate. In vivo studies revealed that the serum triglyceride (TG) concentration was significantly decreased in the group administered amorphous orlistat-loaded Neuisilin®UFL2 with the highest in vitro dissolution rate and lipase activity inhibition in comparison to the commercial product. Furthermore, oily spotting tests in rats revealed that undigested oil was adsorbed onto mesoporous silica after orlistat was released in the gastro-intestinal tract, and it correlated with in vitro result that oil adsorption capacity was dependent on the surface area of empty mesoporous silica. Therefore, it was concluded that mesoporous silica type plays a major role in determining the pharmaceutical characteristics of orlistat formulation prepared using SCMA with CO2 for improving the low solubility and overcoming the side effects.

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