Significant enhancement of antitumor activity and bioavailability of intracellular pH-sensitive polymeric micelles by folate conjugation

2006 ◽  
Vol 116 (2) ◽  
pp. e49-e50 ◽  
Author(s):  
Y. Bae ◽  
K. Kataoka
Keyword(s):  
Antitumor Activity ◽  
Intracellular Ph ◽  
Polymeric Micelles ◽  
Ph Sensitive ◽  
Significant Enhancement

Tissue Distribution and Systemic Toxicity Evaluation of Raloxifene Targeted Polymeric Micelles of Poly (Styrene-Maleic Acid)-Poly (Amide- Ether-Ester-Imide)-Poly (Ethylene Glycol) Loaded With Docetaxel in Breast Cancer Bearing Mice

2019 ◽  
Vol 14 (3) ◽  
pp. 280-291 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Farshid Hassanzadeh ◽  
Batool Hashemi-Beni ◽  
Mohsen Minaiyan ◽  
Saeedeh Enteshari
Keyword(s):  
Side Effects ◽  
Antitumor Activity ◽  
Ethylene Glycol ◽  
Tissue Distribution ◽  
Tumor Cells ◽  
Maleic Acid ◽  
Polymeric Micelles ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene ◽  
Ether Ester

Background: Due to the low water solubility of Docetaxel (DTX), it is formulated with ethanol and Tween 80 with lots of side effects. For this reason, special attention has been paid to formulate it in new drug nano-carriers. Objective: The goal of this study was to evaluate the safety, antitumor activity and tissue distribution of the novel synthesized Raloxifene (RA) targeted polymeric micelles. Methods: DTX-loaded RA-targeted polymeric micelles composed of poly(styrene-maleic acid)- poly(amide-ether-ester-imide)-poly(ethylene glycol) (SMA-PAEE-PEG) were prepared and their antitumor activity was studied in MC4-L2 tumor-bearing mice compared with non-targeted micelles and free DTX. Safety of the micelles was studied by Hematoxylin and Eosin (H&E) staining of tumors and major organs of the mice. The drug accumulation in the tumor and major organs was measured by HPLC method. Results: The results showed better tumor growth inhibition and increased survival of mice treated with DTX-loaded in targeted micelles compared to the non-targeted micelles and free DTX. Histopathological studies, H&E staining of tumors and immunohistochemical examination showed the potential of DTX-loaded RA-targeted micelles to inhibit tumor cells proliferation. The higher accumulation of the DTX in the tumor tissue after injection of the micelles compared to the free DTX may indicate the higher uptake of the targeted micelles by the G-Protein-Coupled Estrogen Receptors (GPER). Conclusion: The results indicate that RA-conjugated polymeric micelles may be a strong and effective drug delivery system for DTX therapy and uptake of the drug into tumor cells, and overcome the disadvantages and side effects of conventional DTX.

LONG TERM EFFECTS OF THYROID STIMULATING HORMONE AND INSULIN ON INTRACELLULAR pH IN FRTL-5 CELLS

1992 ◽  
Vol 133 (2) ◽  
pp. R9-R11
Author(s):  
A.M. Wood ◽  
S.P. Bidey ◽  
J. Soden ◽  
W.R. Robertson
Keyword(s):  
Intracellular Ph ◽  
Small Groups ◽  
Thyroid Stimulating Hormone ◽  
Ph Sensitive ◽  
Long Term Effects ◽  
Bicarbonate Ions ◽  
Chronic Effects ◽  
Petri Dishes ◽  
Presence And Absence

ABSTRACT We have studied the chronic effects of TSH (100μU/ml) and insulin (10μg/ml) on intracellular pH (pHi) in FRTL-5 cells using the pH sensitive probe 2′7-bis (2-carboxyethyl-5′-6′) carboxyfluorescein. FRTL-5 cells were cultured on Petri dishes either in the presence of 4H, ie. Coons F-12 containing cortisol (10nM), transferrin (0.5μg/ml), glycyl-histidyl lysine acetate (10ng/ml) and somatostatin (10μg/ml), or with 4H+insulin (5H), 4H+TSH, or 4H+TSH+insulin (6H). pHi was measured in small groups of cells by microspectrofluorimetry both in the presence and absence of bicarbonate ions after cells had been deprived of serum for at least a day. In

Intracellular pH-Sensitive PEG-block-Acetalated-Dextrans as Efficient Drug Delivery Platforms

2013 ◽  
Vol 5 (21) ◽  
pp. 10760-10766 ◽  
Author(s):  
Zhe Zhang ◽  
Xiaofei Chen ◽  
Li Chen ◽  
Shuangjiang Yu ◽  
Yue Cao ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Intracellular Ph ◽  
Ph Sensitive

Design and validation of a new ratiometric intracellular pH imaging probe using lanthanide-doped upconverting nanoparticles

2017 ◽  
Vol 46 (40) ◽  
pp. 13957-13965 ◽  
Author(s):  
Shuoren Du ◽  
Javier Hernández-Gil ◽  
Hao Dong ◽  
Xiaoyu Zheng ◽  
Guangming Lyu ◽  
...  
Keyword(s):  
Intracellular Ph ◽  
Quantitative Imaging ◽  
Living Cells ◽  
Ph Sensitive ◽  
Upconversion Nanoparticles ◽  
Imaging Probe ◽  
Ph Imaging ◽  
Ratiometric Probe ◽  
Subcellular Level

A ratiometric probe based on upconversion nanoparticles modified with a pH sensitive moiety for the quantitative imaging of pH at the subcellular level in living cells.

scholarly journals In vitro antitumor activity of methotrexate via pH-sensitive chitosan nanoparticles

Biomaterials ◽  
2013 ◽  
Vol 34 (11) ◽  
pp. 2758-2772 ◽  
Author(s):  
Daniele Rubert Nogueira ◽  
Lorena Tavano ◽  
Montserrat Mitjans ◽  
Lourdes Pérez ◽  
M. Rosa Infante ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Chitosan Nanoparticles ◽  
Ph Sensitive

Regulation of intracellular pH in proximal tubules of avian long-looped mammalian-type nephrons

1998 ◽  
Vol 274 (6) ◽  
pp. R1526-R1535 ◽  
Author(s):  
Olga H. Brokl ◽  
Christina L. Martinez ◽  
Apichai Shuprisha ◽  
Diane E. Abbott ◽  
William H. Dantzler
Keyword(s):  
Intracellular Ph ◽  
Ph Sensitive ◽  
Fluorescent Dye ◽  
Proximal Tubules ◽  
Acid Base ◽  
Rate Of Recovery

In nonperfused proximal tubules isolated from chicken long-looped mammalian-type nephrons, intracellular pH (pHi), measured with the pH-sensitive fluorescent dye 2′,7′-bis(2-carboxyethyl)-5(6)-carboxyfluorescein, was ∼7.3 under control conditions (HEPES-buffered medium with pH 7.4 at 37°C) and was reduced to ∼7.0 in response to NH4Cl pulse. The rate of recovery of pHi from this level to the resting level was 1) significantly reduced by the removal of Na+ from the bath, 2) significantly increased by the removal of Cl− from the bath, 3) unchanged by the removal of both Na+ and Cl− from the bath, 4) significantly reduced by the addition of either ethylisopropylamiloride or DIDS to the bath, 5) significantly increased by a high bath K+ concentration, and 6) unchanged by the addition of Ba2+ to the bath. These data suggest that both Na+-coupled and Cl−-coupled basolateral acid-base fluxes are involved in determining the rate of recovery of pHi after acidification. The most likely ones to be important in regulating pHi are a Na+/H+exchanger and a Na+-coupled Cl−/[Formula: see text]exchanger. In birds, long-looped mammalian-type nephrons resemble short-looped transitional nephrons but differ markedly from superficial loopless reptilian-type nephrons.

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