In vitro and in vivo antitumor study of folic acid-conjugated carboxymethyl chitosan and phenylboronic acid–based nanoparticles

2017 ◽  
Vol 66 (10) ◽  
pp. 495-506 ◽  
Author(s):  
Zhipeng Cao ◽  
Xin Wang ◽  
Xu Cheng ◽  
Jun Wang ◽  
Rupei Tang
Keyword(s):  
Folic Acid ◽  
Phenylboronic Acid ◽  
Carboxymethyl Chitosan

scholarly journals Inhibition of Kirsten-Ras reduces fibrosis and protects against renal dysfunction in a mouse model of chronic folic acid nephropathy

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Lucy J. Newbury ◽  
Jui-Hui Wang ◽  
Gene Hung ◽  
Bruce M. Hendry ◽  
Claire C. Sharpe
Keyword(s):  
Folic Acid ◽  
Kidney Disease ◽  
Mouse Model ◽  
Renal Dysfunction ◽  
Antisense Oligonucleotides ◽  
Underlying Mechanism ◽  
Therapeutic Benefit ◽  
End Stage

Abstract Chronic Kidney Disease is a growing problem across the world and can lead to end-stage kidney disease and cardiovascular disease. Fibrosis is the underlying mechanism that leads to organ dysfunction, but as yet we have no therapeutics that can influence this process. Ras monomeric GTPases are master regulators that direct many of the cytokines known to drive fibrosis to downstream effector cascades. We have previously shown that K-Ras is a key isoform that drives fibrosis in the kidney. Here we demonstrate that K-Ras expression and activation are increased in rodent models of CKD. By knocking down expression of K-Ras using antisense oligonucleotides in a mouse model of chronic folic acid nephropathy we can reduce fibrosis by 50% and prevent the loss of renal function over 3 months. In addition, we have demonstrated in vitro and in vivo that reduction of K-Ras expression is associated with a reduction in Jag1 expression; we hypothesise this is the mechanism by which targeting K-Ras has therapeutic benefit. In conclusion, targeting K-Ras expression with antisense oligonucleotides in a mouse model of CKD prevents fibrosis and protects against renal dysfunction.

Folic Acid Functionalized Chlorin e6-Superparamagnetic Iron Oxide Nanocarriers as a Theranostic Agent for MRI-Guided Photodynamic Therapy

2021 ◽  
Vol 17 (2) ◽  
pp. 205-215
Author(s):  
Zhenbo Sun ◽  
Mingfang Luo ◽  
Jia Li ◽  
Ailing Wang ◽  
Xucheng Sun ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Folic Acid ◽  
Iron Oxide ◽  
Near Infrared ◽  
Biological Fluids ◽  
Superparamagnetic Iron Oxide ◽  
Chlorin E6 ◽  
Theranostic Agent

Imaging-guided cancer theranostic is a promising strategy for cancer diagnostic and therapeutic. Photodynamic therapy (PDT), as an approved treatment modality, is limited by the poor solubility and dispersion of photosensitizers (PS) in biological fluids. Herein, it is demonstrated that superparamagnetic iron oxide (SPIO)-based nanoparticles (SCFs), prepared by conjugated with Chlorin e6 (Ce6) and modified with folic acid (FA) on the surface, can be used as versatile drug delivery vehicles for effective PDT. The nanoparticles are great carriers for photosensitizer Ce6 with an extremely high loading efficiency. In vitro fluorescence imaging and in vivo magnetic resonance imaging (MRI) results indicated that SCFs selectively accumulated in tumor cells. Under near-infrared laser irradiation, SCFs were confirmed to be capable of inducing low cell viability of RM-1 cells In vitro and displaying efficient tumor ablation with negligible side effects in tumor-bearing mice models.

Formulation development of folic acid conjugated PLGA nanoparticles for improved cytotoxicity of Caffeic acid phenethyl ester

2021 ◽  
Vol 09 ◽  
Author(s):  
Harshad S Kapare ◽  
Sathiyanarayanan L ◽  
Arulmozhi S ◽  
Kakasaheb Mahadik
Keyword(s):  
Folic Acid ◽  
Drug Release ◽  
Caffeic Acid ◽  
Caffeic Acid Phenethyl Ester ◽  
Therapeutic Effects ◽  
Formulation Development ◽  
Sustained Drug Release ◽  
Active Constituent

Background: Honey bee propolis is one of the natural product reported in various traditional systems of medicines including Ayurveda. Caffeic acid phenethyl ester (CAPE) is an active constituent of propolis which is well known for its anticancer potential. The therapeutic effects of CAPE are restricted owing to its less aqueous solubility and low bioavailability. Objective: In this study CAPE loaded folic acid conjugated nanoparticle system (CLFPN) was investigated to enhance solubility, achieve sustained drug release and improved cytotoxicity of CAPE. Methods: Formulation development, characterization and optimization were carried out by design of experiment approach. In vitro and in vivo cytotoxicity study was carried out for optimized formulations. Results: Developed nanoparticles showed particle size and encapsulation efficiency of 170 ± 2 - 195 ± 3 nm and 75.66 ± 1.52 - 78.80 ± 1.25 % respectively. Optimized formulation CLFPN showed sustained drug release over a period of 42 h. GI50 concentration was decreased by 46.09% for formulation as compared to CAPE in MCF-7 cells indicating targeting effect of CLFPN. An improved in vitro cytotoxic effect was reflected in in-vivo Daltons Ascites Lymphoma model by reducing tumor cells count. Conclusion: The desired nanoparticle characteristic with improved in vivo and in vitro cytotoxicity was shown by developed formulation. Thus it can be further investigated for biomedical applications.

In vitro and in vivo study of carboxymethyl chitosan/polyvinyl alcohol for wound dressing application

2021 ◽  
pp. 51764
Author(s):  
Alireza Akbari ◽  
Shahram Rabbani ◽  
Shiva Irani ◽  
Mojgan Zandi ◽  
Fereshteh Sharifi ◽  
...  
Keyword(s):  
Polyvinyl Alcohol ◽  
Wound Dressing ◽  
Carboxymethyl Chitosan ◽  
In Vivo Study

Stealth doxorubicin conjugated bimetallic selenium/silver nanoparticles for targeted cervical cancer therapy

2021 ◽  
Vol 12 (4) ◽  
pp. 045006
Author(s):  
Thoko Malinga ◽  
Tukayi Kudanga ◽  
Londiwe Simphiwe Mbatha
Keyword(s):  
Cervical Cancer ◽  
Folic Acid ◽  
Colloidal Stability ◽  
Controlled Drug Release ◽  
Delivery Systems ◽  
Drug Binding ◽  
Cervical Cancer Cells ◽  
Diphenyl Tetrazolium Bromide

Abstract Bimetallic nanosized delivery systems are attracting a lot of research interest as alternatives to monometallic delivery systems. This study evaluated the ability of bimetallic selenium silver chitosan pegylated folic acid targeted nanoparticles (SeAgChPEGFA NPs) to deliver doxorubicin (DOX) in cervical cancer cells. Comparison studies using monometallic selenium chitosan pegylated folic acid (SeChPEGFA NPs) targeted NPs and free DOX were also conducted. The prepared NPs and their drug nanocomplexes were characterised morphologically and physico-chemically. Drug binding and releasing studies were conducted under a simulated environment in vitro. The cytotoxicity and apoptosis studies were studied using the 3-[(4, 5-dimethylthiazol-2-yl)−2, 5-diphenyl tetrazolium bromide] (MTT) assay and the dual dye staining. The findings revealed that the bimetallic SeAgChPEGFA NPs displayed better colloidal stability, superior physico-chemical qualities, and higher binding abilities in comparison with monometallic SeChPEGFA NPs. In addition, the SeAgChPEGFA NPs showed the pH-triggered controlled drug release and cell-specific cytotoxicity. These findings suggest that the bimetallic NPs are superior delivery systems when compared to their monometallic NPs and free drug counterparts, thus, setting a platform for further in vivo examination.

Doxorubicin-Loaded Micelles Based on Folic Acid Conjugated pH-Dependent Thermo-Sensitive Copolymer: In Vitro and In Vivo Evaluation

2015 ◽  
Vol 15 (8) ◽  
pp. 5553-5558 ◽  
Author(s):  
Hongli Zhao ◽  
Liang Tao ◽  
Ronghua Yu ◽  
Huihui Yuan ◽  
Minbo Lan
Keyword(s):  
Folic Acid ◽  
Ph Dependent

COMPARATIVE EVALUATION OF POLYMER COMBINATION IN THE DESIGN OF BRIMONIDINE TARTRATE OCULAR INSERTS

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (07) ◽  
pp. 30-35
Author(s):  
P Goudanavar ◽  
◽  
N Ambhore ◽  
D. Hiremath ◽  
R Udupi
Keyword(s):  
Polymer Concentration ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Carboxymethyl Chitosan ◽  
Moisture Loss ◽  
In Vivo Release ◽  
Weight Variation ◽  
Brimonidine Tartrate

Brimonidine is an anti-glaucoma agent useful in treatment of intraocular pressure. In the present study an attempt was made to formulate ophthalmic inserts of brimonidine tartrate (BT) in combination with polymers like methylcellulose, carboxymethyl chitosan and HPMC. Prepared ocular films were evaluated for uniformity in thickness, weight variation, % moisture absorption, % moisture loss, in vitro and in vivo release studies. The physical characteristics of the films were found to be within acceptable limits. The study confirmed that brimonidine tartrate can be delivered through films made of methyl cellulose, carboxymethyl chitosan and HPMC combination matrix cast with ethyl cellulose (EC). In vitro release study revealed that increasing the proportion of polymer concentration decreased the rate of release of brimonidine tartrate. In vivo release profile of ocular inserts revealed controlled release of drug over a period of 24 h. Optimized formulation CH3 was evaluated for in vivo release characteristics using rabbits as animal model. The optimized formulation CH3 was found to be stable at accelerated storage condition of 40/75 % RH.

Folate: In Vitro and in Vivo Effects on VLDL and LDL Oxidation

2007 ◽  
Vol 77 (1) ◽  
pp. 66-72 ◽  
Author(s):  
McEneny ◽  
Couston ◽  
McKibben ◽  
Young ◽  
Woodside
Keyword(s):  
Folic Acid ◽  
Low Density Lipoprotein ◽  
Density Lipoprotein ◽  
Folic Acid Supplementation ◽  
Serum Folate ◽  
Ldl Oxidation ◽  
Low Density ◽  
Acid Supplementation

Raised total homocysteine (tHcy) levels may be involved in the etiology of cardiovascular disease and can lead to damage of vascular endothelial cells and arterial wall matrix. Folic acid supplementation can help negate these detrimental effects by reducing tHcy. Recent evidence has suggested an additional anti-atherogenic property of folate in protecting lipoproteins against oxidation. This study utilized both an in vitro and in vivo approach. In vitro: Very-low-density lipoprotein (VLDL) and low density lipoprotein (LDL) were isolated by rapid ultracentrifugation and then oxidized in the presence of increasing concentrations (0→ μmol/L) of either folic acid or 5-methyltetrahydrofolate (5-MTHF). In vivo: Twelve female subjects were supplemented with folic acid (1 mg/day), and the pre- and post-VLDL and LDL isolates subjected to oxidation. In vitro: 5-MTHF, but not folic acid, significantly increased the resistance of VLDL and LDL to oxidation. In vivo: Following folic acid supplementation, tHcy decreased, serum folate increased, and both VLDL and LDL displayed a significant increase in their resistance to oxidation. These results indicated that in vitro, only the active form of folate, 5-MTHF, had antioxidant properties. In vivo results demonstrated that folic acid supplementation reduced tHcy and protected both VLDL and LDL against oxidation. These findings provide further support for the use of folic acid supplements to aid in the prevention of atherosclerosis.

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