Some new congeners of the anticancer agent 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) synthesis of bifunctional analogs and water soluble derivatives and preliminary evaluation of their chemotherapeutic potential

1976 ◽  
Vol 86 (3) ◽  
pp. 279-286 ◽  
Author(s):  
G. Eisenbrand ◽  
H. H. Fiebig ◽  
W. J. Zeller
Keyword(s):  
Anticancer Agent ◽  
Water Soluble ◽  
Preliminary Evaluation

scholarly journals Synthesis of bioactive polyaniline-b-polyacrylic acid copolymer nanofibrils as an effective antibacterial and anticancer agent in cancer therapy, especially for HT29 treatment

RSC Advances ◽  
2020 ◽  
Vol 10 (42) ◽  
pp. 25290-25304
Author(s):  
Nazanin Bagheri ◽  
Moslem Mansour Lakouraj ◽  
Seyed Reza Nabavi ◽  
Hamed Tashakkorian ◽  
Mojtaba Mohseni
Keyword(s):  
Cancer Therapy ◽  
Polyacrylic Acid ◽  
Anticancer Agent ◽  
Water Soluble ◽  
Acid Copolymer ◽  
Water Soluble Copolymer

In this work, a new highly water-soluble copolymer of polyacrylic acid with polyaniline is introduced.

A Novel pH-Sensitive Microsphere Composed of CM-Chitosan and Alginate for Sulforaphane Delivery

2011 ◽  
Vol 687 ◽  
pp. 539-547 ◽  
Author(s):  
Hui Wang ◽  
Hao Liang ◽  
Qi Peng Yuan ◽  
Tian Xin Wang
Keyword(s):  
Sodium Sulfate ◽  
Anticancer Agent ◽  
Ph Sensitive ◽  
Water Soluble ◽  
Ph Values ◽  
Swelling Studies ◽  
The Stability ◽  
Carboxymethylated Chitosan

Sulforaphane (SF) has been proved to be an effective anticancer agent according to its experiments bothin vitroandin vivo. To date, there is few reported method to deliver SF for increasing its bioactivity and stability. In this study, a novel pH-sensitive microsphere composed of water-soluble carboxymethylated chitosan (CMCS) and alginate mixed with sodium sulfate was developed for SF delivery. Swelling studies and release characteristics under different pH values of microspheres were investigated. Then, the release of SF from test microspheres was studied in simulated gastric and segmented intestinal media. It has been found that the SF cumulated release in 5h was increased from 55.89% to 76.73% when the microspheres mixed with sodium sulfate. In addition, the stability of SF embedded in CMCS/alginate microspheres was also significantly improved. Under pH 7.4, free SF had a severe degradation of approximate 100% within 210 min, whereas the change of the SF in microspheres was only a decrease of about 10%. The results suggested that the microspheres of CMCS and alginate could be a suitable pH-sensitive carrier to increase the stability of SF in the segmented intestine.

Design, Optimization and in vitro Characterization of Dasatinib loaded PLGA Nano carrier for Targeted cancer therapy: A Preliminary Evaluation

2021 ◽  
pp. 2095-2100
Author(s):  
Shyam S Kumar ◽  
G. Gopalakrishnan ◽  
N. L. Gowrishankar
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Surface Morphology ◽  
Dissolution Rate ◽  
Water Soluble ◽  
Spherical Particles ◽  
Preliminary Evaluation ◽  
Pluronic F68

Objective: Drug nanoparticles offer a versatile platform for enhancing the dissolution rate and bioavailability of poorly water soluble drugs The present study was aimed to design and develop dasatinib (DAS) loaded Poly lactide co glycolic acid (PLGA) to enhance the dissolution rate and to study the effect of formulation variables for the BCS class II drug dasatinib for the treatment of chronic myeloid leukemia. Methods: The DAS loaded Nps were prepared by using modified double emulsion solvent evaporation method (DESE) using different stabilizers, the formulated Nps were characterized for particle size, zeta potential, Poly Dispersity Index, Surface morphology, Drug entrapment and Invitro drug release. Results: The DAS loaded NP s showed the lowest particles size of 123 nm and zeta potential of – results of Pluronic F68 loaded NP showed the lowest particle size of – and highest zeta potential of --. Surface morphology of NPs with DMAB showed distinct smooth spherical particles with the size range of 50nm. Morphology of Pluronic F68 formulated NPs showed the high degree of aggregation. In vitro drug release showed up to 24hrs in a sustained manner. Conclusion: The result of our study indicates the use of PLGA as a sustained release polymer and using DMAB as a stabilizer for better stable formulation.

Abstract C166: Preclinical studies of Ureidomustin, a potent water-soluble anticancer agent.

2011 ◽  
Author(s):  
Tsann-Long Su ◽  
Yi-Ren Chen ◽  
Rajesh Kakadiya ◽  
Pei-Wen Hsiao ◽  
Te-Chang Lee ◽  
...  
Keyword(s):  
Anticancer Agent ◽  
Water Soluble ◽  
Preclinical Studies

A novel surface-coated nanocarrier for efficient encapsulation and delivery of camptothecin to cells

MedChemComm ◽  
2014 ◽  
Vol 5 (10) ◽  
pp. 1515-1519 ◽  
Author(s):  
Rie Wakabayashi ◽  
Ryutaro Ishiyama ◽  
Noriho Kamiya ◽  
Masahiro Goto
Keyword(s):  
Anticancer Agent ◽  
Water Soluble ◽  
Poorly Water Soluble

In the present study, we developed a novel surface-coated nanocarrier (SCN) for efficient and stable encapsulation of a poorly water-soluble anticancer agent, camptothecin (CPT).

Enhance of Tumor Targeting by Receptor-Mediated Endocytosis Using Low Molecular Water-Soluble Chitosan Nanoparticles Loaded with Anticancer Agent

2007 ◽  
Vol 342-343 ◽  
pp. 469-472 ◽  
Author(s):  
Dong Gon Kim ◽  
Min Ja Jang ◽  
Chang Yong Choi ◽  
Tae Hyeong Kim ◽  
Mi Kyeong Jang ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Anticancer Agent ◽  
Drug Carrier ◽  
Chitosan Nanoparticles ◽  
Water Soluble ◽  
Molecular Water ◽  
Low Molecular Weight ◽  
Receptor Mediated Endocytosis ◽  
Chitosan Nanoparticle ◽  
High Antitumor Activity

In this study, we prepared using low molecular weight water-soluble chitosan nanoparticle loaded paclitaxel (LMWSC-NPT) and investigated the potential as a drug carrier which is able to accumulate in the tumor site. In the experiment of receptor-mediated endocytosis, LMWSC-NPT was treated with sodium azid (NaN3) as an inhibitor of endocytosis process. As results, the antitumor activity of LMWSC-NPT treated with sodium azid didn’t show but LMWSC-NPT was shown the high antitumor activity. Therefore, LMWSC-NPs modified with hydrophobic group will be useful anticancer agent carrier via receptor-mediated endocytosis.

scholarly journals High loading of trimethylglycine promotes aqueous solubility of poorly water-soluble cisplatin

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Riki Kadokawa ◽  
Tetsuo Fujie ◽  
Gyanendra Sharma ◽  
Kojiro Ishibashi ◽  
Kazuaki Ninomiya ◽  
...  
Keyword(s):  
Aqueous Solution ◽  
Anticancer Agent ◽  
Hepatic Arterial Infusion ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
High Loading ◽  
High Concentration ◽  
High Solubility ◽  
Arterial Infusion ◽  
Poorly Water Soluble

AbstractTrimethylglycine (TMG) is a cheap, natural, and highly biocompatible compound. Therefore, it has been used in the fields of food and life sciences, but the application of solid TMG is limited to utilisation as an “additive”. In the present study, we focussed on the high solubility of TMG in water, derived from the aprotic zwitterionic structure, and proposed TMG as the chemical accounting for a major portion of the aqueous solution (e.g., 50 wt%). High loading of TMG shifted the properties of water and enabled the dissolution of poorly water-soluble cisplatin, an anticancer agent, at high concentration (solubility of cisplatin: 0.15 wt% in water vs 1.7 wt% in TMG aqueous solution). For hepatic arterial infusion, this can reduce the amount of cisplatin administered from 40 to 4 mL. It enables simple injection using a syringe, without the need for catheters and automatic pumps, leading to critical alleviation of the risk to patients. Furthermore, we produced a dry powder from a cisplatin-containing TMG aqueous solution via freeze-drying. Powders can be conveniently stored and transported. Furthermore, cisplatin is often used as a mixture with other drugs, and cisplatin aqueous solutions are not preferred as they dilute the other drugs.

scholarly journals GC-MS analysis and in silico activity prediction of phytocompounds in the roots of Chrysopogon zizanioides (L.) Roberty

2021 ◽  
Vol 8 (1) ◽  
pp. 218-224
Author(s):  
V C N Shanti ◽  
I Neerakkal
Keyword(s):  
In Silico ◽  
Skin Diseases ◽  
Carbonic Acid ◽  
Biological Activities ◽  
Acid Methyl Ester ◽  
Climatic Conditions ◽  
Water Soluble ◽  
Root Extract ◽  
Preliminary Evaluation ◽  
Chrysopogon Zizanioides

Chrysopogon zizanioides (L.) Roberty (Poaceae) commonly known as Ramachamis an aromatic, vigorous growing perennial grass with medicinal properties. The plant is tolerant to extreme soil and climatic conditions and is known for its cooling properties. Roots of the plant are widely used as body scrubber and is suggested for skin diseases in Ayurveda. The present work aims to identify the components in the crude methanolic root extract of C. zizanioides using GC-MS and also to predict the pharmacokinetic behaviour of selected compounds in silico using Swiss ADME online server . 41 compounds were identified of which sesquiterpenes formed the major group. Sesquiterpene Vetivenic acid was the compound with a maximum peak area of 38.9%. Components identified is reported to possess a range of biological activities like anti oxidant, antibacterial, anti cancer, anti inflammatory, anti ulcer, analgesic and insecticidal activities. Compounds with higher peak area like Vetivenic acid, beta vatirenene, beta.-Cedren-9-.alpha.-ol, D Viridiflorol, Gamma muurolene, (Z,E)-alpha-farnesene, Nootkatone, Aromadendrene oxide-(2), 7-Acetyl-2-hydroxy-2methyl-5isopropylbicyclo[4.3.0] nonane, Rosifoliol, 9,10-dehydro isolongifolene, Ylangenol, 4,7,10,13,16,19-Docosahexaenoic acid methyl ester, Carbonic acid, propargyl 2,2,2-tri chloroethyl ester, Oxacyclotetradeca-4,11-diyne, beta eudesmol and longifolene were evaluated in silico. All these compounds proved to obey Lipinski's rule-of-five and were water soluble. Vetivenic acid showed a good bioavailability score of 85% while the others showed 55%. None of the compounds were substrates to P glycoprotein. The values predicted may be used for preliminary evaluation of pharmacological properties of C. zizanioides and also as monographs for the development of potential semisynthetic or synthetic drugs.

Wheat yields and indices of available soil nitrogen in Southern NSW - A preliminary evaluation

1971 ◽  
Vol 11 (50) ◽  
pp. 295 ◽  
Author(s):  
RR Storrier ◽  
AT Hanly ◽  
TB Spence ◽  
AN Smith
Keyword(s):  
Soil Nitrogen ◽  
Nitrogen Fertilizer ◽  
Nitrate Nitrogen ◽  
New South ◽  
Water Soluble ◽  
Soluble Nitrogen ◽  
Preliminary Evaluation ◽  
Regression Analyses ◽  
South Wales ◽  
Fertilizer Requirement

Linear regression analyses were used to evaluate the usefulness of a number of measures of the available soil nitrogen in accounting for the variability in wheat yields under field conditions in southern New South Wales. Single soil tests, such as total mineral nitrogen in the surface sample (0-10 cm depth), could account for only 38 and 18.5 per cent of the variation in yield at flowering and harvest respectively. However, the Use of bilinear regression involving boiling water soluble nitrogen in the surface horizon and nitrate-nitrogen in the sub-soil (10-30 cm depth) accounted for 64 and 36 per cent of the variation in yield at flowering and harvest respectively. The use of these tests to predict the nitrogen fertilizer requirement of wheat will necessitate the measure ment of climatic, cultural and edaphic factors as well as response to nitrogen fertilizer.

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