geoscience.net logo
+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

Biodistribution and bioactivity of tetra-pegylated meta-tetra(hydroxyphenyl)chlorin compared to native meta-tetra(hydroxyphenyl)chlorin in a rat liver tumor model


, : Biodistribution and bioactivity of tetra-pegylated meta-tetra(hydroxyphenyl)chlorin compared to native meta-tetra(hydroxyphenyl)chlorin in a rat liver tumor model. Photochemistry and Photobiology 71(2): 211-217

It has been proposed that the construction of a photosensitizer-polymer conjugate would lead to an increased selective retention of the drug in tumor tissue resulting in an enhancement of selective tumor destruction by light in photodynamic therapy. In this study the kinetics of a tetra-pegylated derivative of meta-tetra(hydroxyphenyl)chlorin (mTHPC-PEG) were compared with those of native meta-tetra(hydroxyphenyl)chlorin (mTHPC) in a rat liver tumor model. In addition, the time course of bioactivity of both drugs was studied in normal liver tissue. Pegylation of mTHPC resulted in a two-fold increase in the plasma half-life time, a five-fold decrease in liver uptake and an increase in the tumor selectivity at early time intervals after drug administration. However, although mTHPC concentrations in liver decrease rapidly with time, mTHPC-PEG liver concentrations increased as a function of time. This led to a loss of tumor selectivity at all but the earliest time points, whereas with mTHPC tumor selectivity increased with time. For both drugs the time course of bioactivity in the liver parallels drug concentration levels with extensive necrosis after irradiation of mTHPC-PEG-sensitized liver tissue up to drug-light intervals of 120 h. It is concluded that on balance mTHPC-PEG does not appear to show any benefits over native mTHPC for the treatment of liver tumors, as normal liver tissue accumulates the compound. However, pegylation is a potentially promising strategy with an increase in tumor selectivity and reduced liver uptake if accumulation in the liver can be prevented.

US$19.90

PMID: 10687396

DOI: 10.1562/0031-8655(2000)0710211babotp2.0.co2


Other references

Alaluusua, S., 2010: Aetiology of Molar-Incisor Hypomineralisation: A systematic review. This was to review and assess the studies on aetiology of Molar-Incisor Hypomineralisation (MIH) or, as a proxy, of demarcated opacities in permanent first molars and to consider the potential factors involved with findings obtained in animal expe...

Anonymous, 2005: Update: West Nile virus activity--United States, 2005. This report summarizes West Nile virus (WNV) surveillance data reported to CDC through ArboNET as of 3 a.m. Mountain Daylight Time, August 30, 2005.

Fersini, A., 1967: Raspberries: a crop yielding lasting profits. Environmental requirements, varieties, propagation, soil preparation, planting, training, cultural practices, harvesting, and control of pests and diseases.

Herisset, A., 1947: Addition to the note: Une. In reply to criticisms by Blaringhem (cf. Abst. 2924) the author states that he claims no more than that the castor oil plant variety under discussion has remained stable for five years. The procedure described for inactivating ricin is declared t...

Thornton P.S.; Alter C.A.; O'neill J.A.; Baker L.; Stanley C.A., 1992: Octreotide therapy in hyperinsulinism. Pediatric Research 31(4 PART 2): 189A

Obermayer, H., 1922: Beitrage zur Kenntnis der Litoralfauna des Vier-waldstattersees. Revue d'Hydrobiol Aarau, 2: 3-111

Petrick, L.; Destaillats, H.; Zouev, I.; Sabach, S.; Dubowski, Y., 2010: Sorption, desorption, and surface oxidative fate of nicotine. Nicotine dynamics in an indoor environment can be greatly affected by building parameters (e.g. relative humidity (RH), air exchange rate (AER), and presence of ozone), as well as surface parameters (e.g. surface area (SA) and polarity). To better...

Swaminath, D.; Sivakumar, P.; Parker, A.; Funderburk, M.; Magers, B.D., 2015: Building A Dashboard For A Cardiovascular Center Of Excellence. Physician Leadership Journal 2(1): 40-46

Cook, D.G.; Butt, J.A., 1953: Hysterosalpingography studies following ectopic pregnancy. American Journal of Obstetrics and Gynecology 66(3): 626-636

Nair, V.M.G.; Kuntz, J.E., 1963: A Wound susceptibility of Bur Oaks to artificial inoculation by Ceratocystis fagacearum. Bur oak (Quercus macrocarpa) proved susceptible to inoculation with C. fagacearum for 18 hr. after wounding in hot, dry weather and 24 hr.