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 ◽  
...  

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.

2006 ◽  
Vol 319 (1-2) ◽  
pp. 130-138 ◽  
Author(s):  
D KIM ◽  
Y JEONG ◽  
C CHOI ◽  
S ROH ◽  
S KANG ◽  
...  

2009 ◽  
Vol 27 (15_suppl) ◽  
pp. 2570-2570 ◽  
Author(s):  
D. Hess ◽  
S. Boehm ◽  
A. Delmonte ◽  
E. Gallerani ◽  
P. Barbieri ◽  
...  

2570 Background: Namitecan is a new water-soluble camptothecin analogue which showed high antitumor activity in preclinical models. Aim of this trial was to determine safety, PK profile and activity in adult patients with advanced solid tumors. Methods: The dose escalation started at 2.5 mg i.v. on days 1 and 8 of a 21 day cycle (D1, D8 Q21D) and increased according to 3+3 cohort design depending on the observed toxicity. Dose limiting toxicity (DLT) definitions were: ANC <0.5x109/L for >5 days; PLT ≥ Grade 3 (CTC V3); grade ≥2 liver/renal toxicity not recovered by D22; any non-hematologic toxicity ≥ Grade 3; D8 dose skipping due to toxicity. Maximum tolerated dose (MTD) and recommended dose (RD) were the primary end-points. Blood and urine samples were collected at cycle 1 for PK evaluation. Results: 31 pts (11 endometrial ca., 5 CRC, 5 ovarian ca., 2 NSCLC, 8 other) have been included, with 6 dose levels evaluated (2.5; 5; 10; 15; 17.5 and 20 mg). 17.5 mg was introduced later when 2/7 DLTs at 20 mg were observed (ANC G4>5days, one with D8 skipping). At 17.5mg 2/4 pts experienced DLTs (ANC G4; D8 skipped). Uncomplicated neutropenia and thrombocytopenia were the most relevant G3/4 hematological toxicities. Other toxicities were mild or moderate asthenia, fatigue and alopecia. The MTD was defined at 17.5 mg and the RD was 15 mg. Stable disease ≥ 6 cycles was recorded in 6 pts (2 stable diseases ≥ 10 cycles). PK was linear and data suggest an entero-hepatic recirculation. No metabolites were found in plasma and the product resulted poorly excreted into urine. Conclusions: The MTD and RD of D1, D8 Q21D schedule have been identified. The study will continue with the evaluation of MTD and RD of a single administration per cycle (D1 Q21D), to optimize the schedule of treatment. [Table: see text]


2020 ◽  
Vol 10 ◽  
pp. 184798042091726 ◽  
Author(s):  
Hyo-Sun Kim ◽  
Song-Hee Lee ◽  
Chae-Jung Eun ◽  
Jeseung Yoo ◽  
Young-Soo Seo

We have developed stable chitosan colloids over a wide pH range without cross-linkers or gelling agents. The colloid was prepared using chitosan nanoparticle obtained from pulverization of bulk chitosan powder, followed by surface treatment using small amount of ascorbic acid (AA) and polyglycerol monostearate (PGMS) in water. Chitosan nanoparticles were well dispersed in a diluted AA solution due to the protonation of the chitosan chain on the surface. And then, the addition of PGMS led them to exhibit highly stable dispersion even in alkali conditions and 50 °C. The hydrodynamic diameter of the colloid was monitored using dynamic light scattering and the real image of the colloid was obtained using cryo-electron microscope measurement. This chitosan colloid will be useful for developing food ingredients or drug carrier templates that should be stable over a wide pH range.


Polymers ◽  
2018 ◽  
Vol 10 (11) ◽  
pp. 1226 ◽  
Author(s):  
Kuo-Yu Chen ◽  
Si-Ying Zeng

Various amounts of 2-((acryloyloxy)ethyl)trimethylammonium chloride were grafted onto chitosan (CS) via redox polymerization method to obtain water-soluble quaternized CS (QCS). The QCS nanoparticles loaded with bovine serum albumin (BSA) were then produced by ionic gelation with tripolyphosphate (TPP) and further covalently cross-linked with genipin. The formation of QCS nanoparticles was optimized as a function of monomer grafting yield, QCS/TPP weight ratio, and QCS/genipin weight ratio by Box-Behnken design and response surface methodology. The results showed that QCS nanoparticles prepared with a grafting yield of 50%, QCS/TPP weight ratio of 7.67, and QCS/genipin weight ratio of 60 had a particle size of 193.68 ± 44.92 nm, polydispersity of 0.232, zeta potential of +23.97 mV and BSA encapsulation efficiency of 46.37 ± 2.89%, which were close to the predicted values from mathematical models. In vitro drug release studies at pH 1.2 and pH 7.4 exhibited that the release rate of BSA was significantly decreased and the release period was significantly prolonged after QCS nanoparticles cross-linking with genipin. Therefore, QCS nanoparticles cross-linked with TPP/genipin dual cross-linkers may be a promising protein drug carrier for a prolonged and sustained delivery.


2013 ◽  
Vol 796 ◽  
pp. 92-97 ◽  
Author(s):  
Cheng Wang ◽  
Hong Lin ◽  
Yu Yue Chen ◽  
Yan Hua Lu

Due to the advantages of both the chitosan and the nanomaterial, chitosan nanoparticle has a broad application in a lot of fields, such as medicine carrier, food process, cosmetics and agriculture protect. And there also appears a lot of research about chitosan nanoparticle in textile finishing in recent years. In former research, steady state chitosan nanoparticles were prepared by ionotropic gelation method in dispersion system. In this paper, in order to confirm the preparation of low molecular weight chitosan nanoparticle, it was also characterized by Fourier Transform Infrared (FT-IR) Spectrometry, X-ray diffraction (XRD) and Transmission Electron Microscope (TEM). Focusing on the application value, chitosan nanoparticles dispersion solution were used as one kind of textile finishing agent to modifyB.morisilk fabrics in order to realize the functionalization of silk fabrics. The wrinkle resistance and bacteria repellency of silk fabrics were tested in the paper. The results showed that chitosan nanoparticles were successfully prepared and confirmed accrording to the XRD, FT-IR and TEM tests. In addition, compared with the ordinaryB. morisilk fabric and theB. morisilk fabric treated with chitosan accordingly, theB. morisilk fabrics treated with chitosan nanoparticle dispersion system had better wrinkle resistance and bacteria repellency.


2006 ◽  
Vol 14 (1) ◽  
pp. 66-72 ◽  
Author(s):  
Dong-Gon Kim ◽  
Changyong Choi ◽  
Young-Il Jeong ◽  
Mi-Kyeong Jang ◽  
Jae-Woon Nah ◽  
...  

2013 ◽  
Vol 13 (3) ◽  
Author(s):  
Netty Widyastuti ◽  
Teguh Baruji ◽  
Henky Isnawan ◽  
Priyo Wahyudi ◽  
Donowati Donowati

Beta glucan is a polysaccharide compound, generally not soluble inwater and resistant to acid. Beta glucan is used as an immunomodulator (enhancing the immune system) in mammals is usually a beta-glucan soluble in water, easily absorbed and has a low molecular weight. Several example of beta-glucan such as cellulose (β-1 ,4-glucan), lentinan (β-1 0.6-glucan) and (β-1 ,3-glucan), pleuran (β-1, 6 and β-1 ,3-glucan) are isolated from species of fungi Basidiomycota include mushrooms (Pleurotus ostreatus) and shiitake (Lentinus edodes).The purpose of thisresearch activity is to obtain beta-glucan compound that can be dissolved in water and in alkali derived from fungi Basidiomycota, i.e, Oyster mushrooms (Pleurotus ostreatus) and shiitake (Lentinus edodes). The result of beta-glucan compared to characterize the resulting beta glucan that is molecular structure . The difference of beta glucan extraction is based on the differences in solubility of beta-glucan. Beta glucan could be water soluble and insoluble water.


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