scholarly journals Kanamycin Sulphate Loaded PLGA-Vitamin-E-TPGS Long Circulating Nanoparticles Using Combined Coating of PEG and Water-Soluble Chitosan

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Sanaul Mustafa ◽  
V. Kusum Devi ◽  
Roopa S. Pai
Keyword(s):  
Vitamin E ◽  
Half Life ◽  
Blood Circulation ◽  
The Body ◽  
Water Soluble ◽  
Controlled Delivery ◽  
Protein Synthesis Inhibitor ◽  
Formulation Development ◽  
Vitamin E Tpgs

Kanamycin sulphate (KS) is a Mycobacterium tuberculosis protein synthesis inhibitor. Due to its intense hydrophilicity, KS is cleared from the body within 8 h. KS has a very short plasma half-life (2.5 h). KS is used in high concentrations to reach the therapeutic levels in plasma, which results in serious nephrotoxicity/ototoxicity. To overcome aforementioned limitations, the current study aimed to develop KS loaded PLGA-Vitamin-E-TPGS nanoparticles (KS-PLGA-TPGS NPs), to act as an efficient carrier for controlled delivery of KS. To achieve a substantial extension in blood circulation, a combined design, affixation of polyethylene glycol (PEG) to KS-PLGA-TPGS NPs and adsorption of water-soluble chitosan (WSC) (cationic deacetylated chitin) to particle surface, was raised for surface modification of NPs. Surface modified NPs (KS-PEG-WSC NPs) were prepared to provide controlled delivery and circulate in the bloodstream for an extended period of time, thus minimizing dosing frequency. In vivo pharmacokinetics and in vivo biodistribution following intramuscular administration were investigated. NPs surface charge was close to neutral +3.61 mV and significantly affected by the WSC coating. KS-PEG-WSC NPs presented striking prolongation in blood circulation, reduced protein binding, and long drew-out the blood circulation half-life with resultant reduced kidney sequestration vis-à-vis KS-PLGA-TPGS NPs. The studies, therefore, indicate the successful formulation development of KS-PEG-WSC NPs with reduced frequency of dosing of KS indicating low incidence of nephrotoxicity/ototoxicity.

Polymer Brush-Stabilized Polyplex for a siRNA Carrier with Long Blood Circulatory Half-Life

2008 ◽  
Vol 47-50 ◽  
pp. 762-764 ◽  
Author(s):  
Arihiro Kano ◽  
Takeshi Yamano ◽  
Sun Won Choi ◽  
Atsushi Maruyama
Keyword(s):  
Delivery System ◽  
Half Life ◽  
Blood Circulation ◽  
Sirna Delivery ◽  
Polymer Brush ◽  
Water Soluble ◽  
Side Chains ◽  
Grafting Ratio ◽  
Interfering Rna

Small interfering RNA (siRNA) holds potential as a therapeutic approach to silence targeted gene of disease, but siRNA has limited stability in vivo. Therefore, delivery system of siRNA is the key to siRNA therapeutic application. We attempted to develop a delivery system, which enables siRNA to demonstrate high stability and long blood circulation. We synthesized a series of bottlebrush-type copolymers (BBCs) possessing polycationic backbone (less than 30 wt%) and abundant water-soluble side chains (more than 70 wt%) as siRNA carrier. A siRNA complexed with the BBC was resistant to nuclease and stable in plasma. Especially, the BBC (10 wt% PLL and 90 wt% PEG) having higher grafting ratio (≈ 90 wt%) of water-soluble side chains showed 100-times enhanced stability of siRNA in mouse bloodstream in vivo. Surprisingly, even when the BBC and siRNA separately injected into mouse at 20 min interval, the BBC increased blood half life of the siRNA. These results suggest that the BBC has higher selectivity in its ionic interaction to siRNA than other anionic substance in blood components. To our knowledge, this is the first report of siRNA delivery carrier which prolonged blood circulation of siRNA without resource-consuming preparation process.

Human Skin Binding and Absorption of Contaminants from Ground and Surface Water During Swimming and Bathing

1989 ◽  
Vol 8 (5) ◽  
pp. 853-859 ◽  
Author(s):  
Ronald C. Wester ◽  
Howard I. Maibach
Keyword(s):  
Surface Water ◽  
Stratum Corneum ◽  
Human Skin ◽  
The Body ◽  
Water Soluble ◽  
Exposure Effect ◽  
Human Stratum Corneum ◽  
Water Dilution

Contaminants exist in ground and surface water. Human skin has the capacity to bind and then absorb these contaminants into the body during swimming and bathing. Powdered human stratum corneum will bind both lipid-soluble (alachlor, polychlorinated biphenyls [PCBs], benzene) and water-soluble (nitroaniline) chemicals. In vitro (human skin) and in vivo (Rhesus monkey) studies show that these chemicals readily distribute into skin, and then some of the chemical is absorbed into the body. Linearity in binding and absorption exists for nitroaniline over a 10-fold concentration range. Multiple exposure to benzene is at least cumulative. Binding and absorption can be significant for exposures as short as 30 min, and will increase with time. Absorption with water dilution increased for alachlor, but not for dinoseb. Soap reversed the partitioning of alachlor between human stratum corneum and water. The PCBs could be removed from skin by soap and water (70% efficiency) for up to 3 h and then decontamination potential decreased, due to continuing skin absorption. The model in vitro and in vivo systems used should permit easy estimation of this area of extensive human exposure effect on risk assessment.

Polyphenols in Food: Cancer Prevention and Apoptosis Induction

2018 ◽  
Vol 25 (36) ◽  
pp. 4740-4757 ◽  
Author(s):  
Ashita Sharma ◽  
Mandeep Kaur ◽  
Jatinder Kaur Katnoria ◽  
Avinash Kaur Nagpal
Keyword(s):  
Cancer Prevention ◽  
Defense Mechanism ◽  
Antioxidant Property ◽  
The Body ◽  
Water Soluble ◽  
Stress Factors ◽  
In Vivo Studies ◽  
Hydroxyl Groups

Polyphenols are a group of water-soluble organic compounds, mainly of natural origin. The compounds having about 5-7 aromatic rings and more than 12 phenolic hydroxyl groups are classified as polyphenols. These are the antioxidants which protect the body from oxidative damage. In plants, they are the secondary metabolites produced as a defense mechanism against stress factors. Antioxidant property of polyphenols is suggested to provide protection against many diseases associated with reactive oxygen species (ROS), including cancer. Various studies carried out across the world have suggested that polyphenols can inhibit the tumor generation, induce apoptosis in cancer cells and interfere in progression of tumors. This group of wonder compounds is present in surplus in natural plants and food products. Intake of polyphenols through diet can scavenge ROS and thus can help in cancer prevention. The plant derived products can also be used along with conventional chemotherapy to enhance the chemopreventive effects. The present review focuses on various in vitro and in vivo studies carried out to assess the anti-carcinogenic potential of polyphenols present in our food. Also, the pathways involved in cancer chemopreventive effects of various subclasses (flavonoids, lignans, stilbenes and phenolic acids) of polyphenols are discussed.

scholarly journals Polysialic Acid Modified Liposomes for Improving Pharmacokinetics and Overcoming Accelerated Blood Clearance Phenomenon

Coatings ◽  
2020 ◽  
Vol 10 (9) ◽  
pp. 834
Author(s):  
Xi Han ◽  
Ting Zhang ◽  
Mengyang Liu ◽  
Yanzhi Song ◽  
Xinrong Liu ◽  
...  
Keyword(s):  
Blood Circulation ◽  
Polysialic Acid ◽  
Repeated Administration ◽  
The Body ◽  
Circulation Time ◽  
Blood Clearance ◽  
In Vivo Evaluation ◽  
Accelerated Blood Clearance ◽  
Abc Phenomenon

Poly (ethylene glycol) (PEG) modified nanocarriers are being used widely in the drug delivery system (DDS). However, the “accelerated blood clearance (ABC) phenomenon” was induced upon repeated administration of PEG-modified liposomes, resulting in reduced blood circulation time, and increased accumulation in liver and spleen. To avoid the unexpected phenomenon, polysialic acid (PSA) was selected to modify liposomes. PSA is a natural, highly hydrophilic polysaccharide polymer for which no receptors exists in the body. It is non-immunogenic, biodegradable and endows the conjugated bioactive macromolecule and drugs with increased circulation time in vivo. In the present study, the in vivo evaluation showed that PSA modified liposomes (PSA-Lip) afford extended blood circulation in wistar rats and beagle dogs. Moreover, the ABC phenomenon did not occur and the IgM antibody was not induced after repeated injections of PSA-Lip. These results strongly suggest that PSA modification represents a promising strategy to afford good stealth of the liposomes without evoking the ABC phenomenon.

scholarly journals Combretastatins: An Overview of Structure, Probable Mechanisms of Action and Potential Applications

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2560 ◽  
Author(s):  
Gökçe Şeker Karatoprak ◽  
Esra Küpeli Akkol ◽  
Yasin Genç ◽  
Hilal Bardakcı ◽  
Çiğdem Yücel ◽  
...  
Keyword(s):  
South African ◽  
Water Solubility ◽  
The Body ◽  
Water Soluble ◽  
In Vivo Studies ◽  
Lead Compounds ◽  
Combretastatin A4 ◽  
Potential Applications

Combretastatins are a class of closely related stilbenes (combretastatins A), dihydrostilbenes (combretastatins B), phenanthrenes (combretastatins C) and macrocyclic lactones (combretastatins D) found in the bark of Combretum caffrum (Eckl. & Zeyh.) Kuntze, commonly known as the South African bush willow. Some of the compounds in this series have been shown to be among the most potent antitubulin agents known. Due to their structural simplicity many analogs have also been synthesized. Combretastatin A4 phosphate is the most frequently tested compounds in preclinical and clinical trials. It is a water-soluble prodrug that the body can rapidly metabolize to combretastatin A4, which exhibits anti-tumor properties. In addition, in vitro and in vivo studies on combretastatins have determined that these compounds also have antioxidant, anti-inflammatory and antimicrobial effects. Nano-based formulations of natural or synthetic active agents such as combretastatin A4 phosphate exhibit several clear advantages, including improved low water solubility, prolonged circulation, drug targeting properties, enhanced efficiency, as well as fewer side effects. In this review, a synopsis of the recent literature exploring the combretastatins, their potential effects and nanoformulations as lead compounds in clinical applications is provided.

Formulation Development and Evaluation of Sustained Release Matrix Tablets of Guaiphenesin

2016 ◽  
Vol 9 (3) ◽  
pp. 3312-3316
Author(s):  
Ganesh D. Basarkar ◽  
Ketan H. Shah ◽  
Madhuri B. Sonawane
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Rice Bran ◽  
Half Life ◽  
Water Soluble ◽  
Matrix Tablet ◽  
Formulation Development ◽  
Sustained Release Formulation ◽  
Rice Bran Wax ◽  
Melt Granulation

In this study we sought to formulate and evaluate sustained release matrix tablet of guaiphenesin by melt granulation technology. The sustained release tablets were prepared by melt granulation technique using rice bran wax as a drug retardant and dibasic calcium phosphate (DCP) as a channelling agent. Guaiphenesin is an expectorant and has a short plasma half-life of one hour. Because of high frequency of administration and short biological half-life, guaiphenesin was considered as model drug. Sustained release formulation that would maintain plasma levels for 12 hours is sufficient for twice daily dosing of guaiphenesin. The compatibility of drug and wax was examined by differential scanning calorimetry (DSC). The effect of waxes at different (drug: wax) concentrations on the release profile of drug from matrix formulation were studied. Drug release was studied at pH 1.2 for 2 hour and pH 6.8 for 10 hours. A significant retardation in the drug release was observed by increasing the wax concentration. The drug release study revealed that wax concentration of 30% to be optimum. Dissolution study showed 99% drug release within 12 hrs. Kinetic modelling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport. These results suggest that the rice bran wax has good release retardant property for highly water-soluble drug such as guaiphenesin.

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