INFILTRATION AND TISSUE CONCENTRATION OF INTRAVESICALLY INSTILLED (2^|^Prime;R)-4^|^prime;-O-TETRAHYDROPYRANYLADRIAMYCIN OR ADRIAMYCIN IN RAT BLADDER TUMOR INDUCED BY BBN

Abstract

Rats with bladder tumor induced by BBN were treated by intravesical instillation of 0.8 mg of (2"R)-4'-O-tetrahydropyranyladriamycin (THP) (9 rats) or adriamycin (ADM) (8 rats) dissolved in 0.2 ml of distilled water. Thirty minutes later, the bladder was removed surgically. Rats without the tumor received the same treatment of THP (8 rats) or ADM (9 rats). THP and ADM infiltrations to the normal bladder tissue and the tumor were estimated by the use of the photonic microscope system, since both drugs were known to emit characteristic fluorescence. It was found that infiltration of THP to the tumor tissue was more prominent in amounts and deeper than that of ADM, while smaller amounts of THP infiltrated into the normal mucosa compared to ADM. The fact might explain the clinical finding that THP instilled intravesically in half a concentration of ADM showed the same effect on the tumor as ADM. Subsequently, tissue concentrations of THP and ADM were estimated by high performance liquid chromatography. Either THP or ADM was instilled intravesically for 30 minutes to 6 rats with bladder tumor. Similarly, either THP or ADM was instilled in 5 rats without the tumors. Contrary to the result of the photonic microscope system, the tissue concentration of THP was not different from that of ADM not only in the tumor tissues but also in the normal bladder ones. Furthermore, the tissue concentration of both drugs in the normal bladder was higher than that in the bladder tumor.(ABSTRACT TRUNCATED AT 250 WORDS)

Diagnosing the Location of Carcinoma in situ (CIS) of the Urinary Bladder Using Pirarubicin Hydrochloride

“…Their results show that, compared to ADM, THP was more likely to transfer to tumor tissue, but was less likely to transfer to normal tissue [5] .…”

“…Masuda et al [5] injected 0.2 ml of 4 mg/ml THP or ADM into the urinary bladder of BBN rats, and measured the levels of these drugs in the urinary bladder 30 min after injection using an image analyzer based on the fl uorescence of the two drugs. Their results show that, compared to ADM, THP was more likely to transfer to tumor tissue, but was less likely to transfer to normal tissue [5] .…”

“…Because THP is selectively absorbed by bladder tumor cells [2][3][4][5] , and has a pigment, we think that THP may be useful in diagnosing the location of bladder CIS macroscopically.…”

Improved Detection of Nonmuscle Invasive Urothelial Carcinoma of the Bladder Using Pirarubicin Endoscopy: A Prospective, Single-Center Preliminary Study

“…THP is quickly and selectively absorbed by tumor cells, 22 and fluorescence intensity is proportional to the level of uptake. In previous studies, THP was absorbed within 3 to 4 minutes, reaching peak absorption in 30 minutes, but retention of THP in the bladder for 5 to 15 minutes using intravesical chemotherapy appears to be a better technique.…”