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PubMed1986

[A new superselective balloon catheter--all-silicone catheter with a floppy tip].

We have introduced concept of "chemical" embolization and have tried to develop a new agent which would enable us to embolize the lesion with one-shot injection. Such an agent must be able to occlude diffusely the lesion distal to the catheter. This has made it mandatory to develop a new catheter which can be introduced into the vessel as close to the lesion as possible with fewer risks of clot formation and/or vessel damage. A new superselective balloon catheter for angiography and infusion of liquid embolizing materials has been developed. This catheter consists of a proximal relatively stiff silicone catheter, a short distal thin-walled flexible silicone catheter and silicone balloon. These three silicone components are connected by silicone adhesives. The distal catheter allows us to catheterize fine arteries such as lenticulostriates, while the proximal catheter assures easy manipulation. This balloon catheter can be used for superselective angiography and infusion of liquid embolizing materials. It has been used on nine patients; one with a dural arterio-venous malformation (AVM), four with meningiomas, and four with brain and spinal cord AVMs. In the case of dural AVM and meningiomas, it was possible to easily introduce into the middle meningeal artery distal to the foramen spinosum. In addition, in one of the cases of meningioma, we were able to catheterize one of the main feeding pedicles beyond the pterion. Chemical embolization was carried out in 5 cases with good results. In the case of brain and spinal cord AVM, useful information was obtained from the superselective angiography.(ABSTRACT TRUNCATED AT 250 WORDS)

Angiography↗
PubMed1992

Lipid-independent therapeutic properties of transdermal 17 B-estradiol on cardiovascular diseases.

A low dose of transdermally administered 17 B-estradiol promptly improved a severe, treatment-unresponsive, cardiac arrhythmia initiated after the menopause in a woman with type-II familial hyperlipoproteinemia. The same treatment normalized the hypertension initiated after ovariectomy, in a woman who was only poorly controlled by anti-hypertensive drugs. These two cases are the first clear report of cardiovascular therapeutic properties of transdermal estradiol via mechanisms independent of lipoprotein modifications.

Administration, Cutaneous↗
PubMed1994

Recruitment with high physiological doses of estradiol preceding chemotherapy: flow cytometric and therapeutic results in women with locally advanced breast cancers--a Southwest Oncology Group study.

One theoretical method of increasing chemotherapeutic efficacy in breast cancer is to temporarily increase the number of tumor cells in cycle through hormonal recruitment prior to initiation of chemotherapy. In an effort to determine when and if this could be reliably accomplished, 50 women with locally advanced and/or metastatic breast cancer with known estrogen receptor (ER) status were entered into a serial breast biopsy study designed to measure increases in S-phase fraction (SPF) and proliferative index (PI; S + G2 + M) following administration of a high physiological dose of estrogen via estradiol vaginal suppositories prior to chemotherapy. Blood levels of estradiol were maintained in a range (0.5-5 nM) known to increase SPF in vitro. Compliance with suppository administration was monitored by serial blood sampling. Tumors were sampled at 0, 24, 48, 72, and/or 96 h. Thirty-one ER-positive and 9 ER-negative women had evaluable baseline biopsies and at least 1 subsequent biopsy. An increase was seen for SPF in 20 (69%) and for PI in 23 (79%) of 29 ER-positive patients at 48 h after estrogen initiation (95% confidence intervals, 49-85% for SPF and 60-92% for PI); similar increases were seen at 72 h. Median baseline SPF and PI values in ER-positive patients for whom increases were noted at 48 h were 6.2 and 8.5%, respectively. The median relative increases in these patients were 170 and 100%, respectively, at 48 h. The increases observed at 24 h in 4 (SPF) and 6 (PI) of the 9 ER-negative patients could have occurred by chance alone. Twenty-five of the 28 locally advanced (T4 and/or N2-3) patients achieved a complete response during combined modality treatment (estradiol-chemotherapy, mastectomy, and radiation). At a minimum follow-up time of 42 months, estimated 5-year progression-free and overall survivals are 30 and 49%, respectively, with a median time to progression of 35 months. Twenty-two women had metastatic disease (19 also had locally advanced disease). Thirteen had a complete or partial response, with a median duration of 12 months. Median progression-free and over-all survival times for all metastatic patients are 4 and 17 months, respectively. Estimated 5-year survival for metastatic disease patients is 27%. A high physiological dose of estrogen administered to patients with locally advanced ER-positive tumors can reliably increase the tumor SPF and PI within 48 h.(ABSTRACT TRUNCATED AT 400 WORDS)

Breast Neoplasms↗
PubMed1984

Estriol modifies the absorption of estrone and estradiol in castrated rhesus monkeys: a new therapeutic approach for the use of natural estrogens in the menopause?

In order to study the effects of estriol (E3) on estradiol (E2) and estrone (E1) absorption in the rhesus monkey the following study was performed. Chronically ovariectomized animals were divided in four groups of five each according to the treatment protocol (1) E1: 0.7 mg (2) E1: 0.7 mg + E3: 0.135 mg (3) E2: 0.3 mg, (4) E2: 0.3 mg + E3: 0.135 mg (5) E1: 0.7 mg + E2: 0.3 mg and (6) E1: 0.7 mg + E2: 0.3 mg + E3: 0.135 mg. Monkeys received daily drug administration (DA) for 10 consecutive days. Serum E1, E2 and E3 were determined by RIA on a daily basis. In addition, during the first day of treatment blood samples were obtained at hourly intervals. Results were analyzed by comparing the areas under the curve (Integral tests). The data shows that during treatment serum concentrations of E1 and E2 in groups 1, 3 and 5 were significantly higher than in groups 2, 4 and 6 (2-4-fold greater). Serum levels of E1 and E2 rose 5-fold from baseline in animals from group 1 within 1 h, while they increased only 2-fold in those from group 2 at 3-6 h after DA. Similarly, serum levels of E1 and E2 increased 30- and 10-fold respectively 1 h after DA in group 3, while they rose 12- and 5-fold respectively 4 h after DA in animals of group 4. Estriol levels were similar in animals from group 2 and 4 throughout the study (250 +/- 80 pg/ml). It may be concluded therefore that the oral administration of estriol diminishes the absorption of both E1 and E2 and alters their bioavailability, perhaps modulating their biological activity.

Absorption↗
PubMed2000

Visualization of percutaneous 3H-estradiol and 3H-norethindrone acetate transport across human epidermis as a function of time.

Developing transdermal therapeutic systems for estradiol and norethindrone acetate raised questions about the steroids penetration pathway across and retention in the skin. This paper describes the distribution of 3H-estradiol and 3H-norethindrone acetate in human stratum corneum after topical application to dermatomed skin in vitro. The study involved (a) permeation experiments to determine the steroid flux, (b) autoradiographical visualization of the steroid distribution in the same skin samples, and (c) a correlation between flux and skin distribution in time. On correlating the steroid flux with intraepidermal steroid distribution, it was concluded that both permeants were bound in the skin tissue. The steroids were preferentially located in or close to the intercellular lipids of the stratum corneum, indicating that both transport and binding occurred via this domain of the stratum corneum. This study demonstrated the importance of correlating drug flux with intraepidermal drug distribution as a function of time.

Administration, Cutaneous↗
PubMed2002

Therapeutic effect of in vivo sustained estradiol release from poly (lactide-co-glycolide) microspheres on bone mineral density of osteoporosis rats.

Poly (lactide-co-glycolide or PLGA) microspheres containing 0.3% (w/w) of estradiol were prepared by a solvent evaporation method. These PLGA microspheres had a wide particle distribution between 0.5 and more than 100 microm. The average size was 76 microm. Physicochemical properties of the microspheres were characterized by X-ray diffraction patterns, FT-IR spectra and DSC. In vitro estradiol release was maintained at a constant rate from these PLGA microspheres for 1 month. The loaded drug was totally recovered in the collection buffer within this time period. In vivo experiments were performed on Wistar rats that had received ovariectomy. These rats were fed with a vitamin D-deficient and Ca-deficient diet. The combination of ovariectomy and diet induced osteoporosis. PLGA microspheres containing either 50, 100, or 200 microg estradiol were injected into these rats. The plasma estradiol in each rat was monitored for 50 days. These in vivo drug release patterns were found to be different from the one obtained from in vitro release. The Ca-AUC was not significant different among various dosages administered. However, bone mineral density for rats after the injection of estradiol loaded microspheres was higher than that obtained for the control. This suggested that all estradiol microspheres administration induced bone generation in osteoporosis rats.

Animals↗
PubMed1991

Suppression of ovarian estradiol secretion by a single injection of antide in cynomolgus monkeys during the early follicular phase: immediate, sustained, and reversible actions.

We examined the effects of the GnRH antagonist antide on ovarian estrogen secretion after a single administration in intact cycling cynomolgus monkeys (n = 5/group) during the early follicular phase. Antide treatment on menstrual cycle day 2 resulted in a dose-dependent increase in menstrual cycle lengths (mean +/- SEM) to 38 +/- 3, 49 +/- 8, and 96 +/- 15 days for 3.0, 10.0, and 30.0 mg/kg antide, respectively, in association with inhibition of folliculogenesis and suppression of estradiol concentrations to therapeutic levels. Subsequent resumption of apparently normal ovulatory menstrual cycles occurred in all 15 individuals. In addition, all four monkeys from the group treated with 30 mg/kg antide that were available for subsequent matings became pregnant and had normal babies. Thus, no irreversible consequences or adverse effects of antide on reproductive function in these primates was observed. No allergic or other adverse reactions were found locally or systemically in these primates, even at the highest dose of antide. To the extent that this primate model is a paradigm for clinical therapeutics, a single treatment of antide (30 mg/kg) provides sustained inhibition of ovarian estradiol secretion for about 2 months, thus demonstrating the feasibility of using antide for clinical management of steroid-dependent conditions.

Animals↗
PubMed1981

Cytoplasmic progesterone and estradiol receptors in normal, hyperplastic, and carcinomatous endometria: therapeutic implications.

This study was designed to determine whether the presence of progesterone receptors (PR) and/or estradiol receptors (ER) could be used to predict progestin responsiveness of recurrent or advanced endometrial cancers. We have demonstrated the presence of physicochemically similar cytoplasmic progesterone and estradiol receptors in normal, hyperplastic, and carcinomatous endometria. All normal endometria contained both PR and ER. Seventy-three percent of endometrial hyperplasias were PR(+) and 93% were ER(+). A decreasing concentration of progesterone receptor activity was observed with increasing tumor anaplasia [grade 1, 84% PR(+); grade 2, 55% PR(+); grade 3, 22% PR(+)] and in irradiated tumors. A statistically significant (p less than 0.001) relationship has been demonstrated between the presence of specific cytoplasmic PR and response to progestin therapy in recurrent or advanced endometrial adenocarcinomas. Thus, we conclude that a PR assay may be used to help select the most appropriate therapy for patients with recurrent or advanced endometrial adenocarcinoma.

Adenocarcinoma↗
PubMed1989

Human early pregnancy factor and early pregnancy associated protein before and after therapeutic abortion in comparison with beta-hCG, estradiol, progesterone and 17-hydroxyprogesterone.

Serum activities and concentrations, respectively, of early pregnancy factor (EPF), early pregnancy associated protein (EPAP), beta-hCG, estradiol, progesterone and 17-hydroxyprogesterone were estimated in 20 healthy primigravidae within the tenth to twelfth completed gestational week before and after therapeutic abortion. EPF, beta-hCG and estradiol markedly decreased after termination of pregnancy, whereas progesterone and 17-hydroxyprogesterone concentrations moderately fell. EPAP showed no significant alterations in a 24 hours period. Because of its possible role as immunosuppressive substance and its short half-life EPF may be a promising immunobiomarker for disturbances in early pregnancy.

17-alpha-Hydroxyprogesterone↗
PubMed1987

[A transdermal therapeutic system for hormonal therapy of climacteric deficiency pictures. A multicenter study].

In an open study 112 women with menopausal symptoms were treated with a transdermal therapeutic system delivering estradiol at a rate of 25, 50 or 100 micrograms per day resp. The study, which was to measure the therapeutic efficacy and systemic and local tolerability, lasted 3 months. At the end of the treatment period 46% of the women were completely free of symptoms and a further 46% very much improved. In 64% the hot flushes disappeared entirely and in the remaining women their frequency and intensity, with a few exceptions, were markedly diminished. Nocturnal bouts of sweating were completely prevented in 67% of those complaining of this symptom. Pollakiuria improved in 93%. Before commencement of the therapy 24 patients felt unwell; during the study only two. The proportion of women who felt well or very well rose from 36% to 83%. The systemic tolerability was rated good or excellent by 97% of patients and in no case was it rated poor. Blood pressure and body weight were not affected. The local tolerability was considered good or very good by 80% of the women; it was poor in 5 cases (4.6%) and only in one case did it lead to discontinuation of the therapy. Ninety percent of the participants wanted to continue treatment beyond the duration of the study.

Administration, Cutaneous↗
PubMed2004

The therapeutic effects of a progesterone-releasing intravaginal device (PRID) with attached estradiol capsule on ovarian quiescence and cystic ovarian disease in postpartum dairy cows.

The objective of this study was to evaluate the effects of a progesterone-releasing intravaginal device (PRID) containing an estradiol benzoate capsule on ovarian dysfunction, including ovarian quiescence, follicular cyst (FC) and luteal cyst or cystic corpus luteum (LC/CCL), in postpartum dairy cows. These ovarian dysfunctions were examined by palpation per rectum relative to plasma progesterone status. The results of clinical examination and hormone assay determined ovarian quiescence in 13 cows, FC in 15 cows and LC/CCL in 7 cows. These cows were treated with PRID for 12 d and then clinical examination was performed. After PRID removal, the proportion of cows exhibiting estrous signs within 7 d and confirmed formation of CL within 7-14 d (markedly effective) were 69.2 % (n=9) for ovarian quiescence, 46.7 % (n=7) for FC, and 28.6 % (2 cows) for LC/CCL. Two cows (15.4 %) in ovarian quiescence, 5 cows (33.3%) with FC and 4 cows (57.1 %) with LC/CCL did not exhibit estrous signs but were recognized as having formed CL within 12-16 d after removal of PRID (effective). These results suggest that treatments of PRID with estradiol benzoate for 12 d have therapeutic efficacy on ovarian dysfunction including ovarian quiescence, FC and LC/CCL in postpartum dairy cows.

Animals↗
PubMed1999

Effects of ovariectomy, 192 IgG-saporin-induced cortical cholinergic deafferentation, and administration of estradiol on sustained attention performance in rats.

Female ovariectomized (OVX) and sham-OVX rats were trained in a task designed to assess sustained attention. After achieving asymptotic performance, OVX rats did not exhibit the impairment in performance over blocks of trials (i.e., the vigilance decrement) observed in sham-OVX rats. Furthermore, OVX rats' performance over blocks of trials was unaffected by the normally detrimental effects of a visual distractor. 192 IgG-saporin-induced lesions of basal forebrain cholinergic neurons resulted in similar impairments in the performance of OVX and sham-OVX rats. The acute, but not chronic, administration of 17beta-estradiol attenuated the lesion-induced decrease in the relative number of hits to longest signals exclusively in rats with intact ovaries. These findings indicate that the variables contributing to the potential therapeutic effects of estradiol remain poorly understood.

Animals↗
PubMed2004

Modulation of survival in osteoblasts from postmenopausal women.

Osteoblast survival is one of the determinants of postmenopausal osteoporosis development. Recent data from animal experiments suggest that cytokines, in particular Fas ligand (FasL), contribute to postmenopausal osteoporosis. We now address the effect of Fas activation in postmenopausal osteoblast survival and the potential modulatory effect of estrogen and raloxifene analog (LY117018). The expression of Fas mRNA, Fas protein, and the sensitivity to Fas-induced apoptosis were studied in primary cultures of human osteoblasts from postmenopausal women and in osteoblastic MG-63 cells. Human postmenopausal osteoblasts constitutively expressed Fas receptors in the cell surface. TNFalpha increased the expression of Fas mRNA and cell surface Fas expression. Neither estradiol nor raloxifene analog prevented this increase in Fas expression. In addition, activation of Fas receptor resulted in apoptosis of postmenopausal osteoblasts. While TNFalpha did not induce human osteoblast apoptosis, it did increase the lethal effect of Fas activation. Therapeutic concentrations of estradiol or raloxifene analog did not modulate lethal cytokine-induced apoptosis. Both postmenopausal osteoblasts and MG-63 cells express FasL. FasL expression was not modulated by TNFalpha. In conclusion, estrogen and raloxifene analog do not appear to affect the sensitivity of postmenopausal osteoblasts to Fas-mediated apoptosis.

Aged↗
PubMed1996

Comparative bioavailability study of an once-a-week matrix versus a twice-a-week reservoir transdermal estradiol delivery systems in postmenopausal women.

An open-label, randomised, crossover study was conducted with in healthy postmenopausal women to compare the relative bioavailability of a matrix transdermal estradiol delivery system worn for 7 consecutive days, versus a reservoir transdermal patch worn for 4 days followed by its immediate replacement by another patch worn for further 3 consecutive days. There was a minimum 7-day washout period between the two study periods. Both systems were labelled to release approximately 50 micrograms/day of estradiol. Twenty-six subjects were evaluated with regard to estradiol serum levels. Blood samples were taken immediately before and at regular intervals until 192 h after the initiation of each study treatment (patch application) and assayed for estradiol. There was no difference between the patches with regard to Cmax. Based on the relative bioavailability, one matrix patch proved to be bioequivalent to two reservoir patches worn consecutively for 7 days. These results demonstrate the ability of one matrix patch to deliver consistent therapeutic levels of estradiol over a 7-day period.

Administration, Cutaneous↗
PubMed2000

Post-injury ex vivo model to investigate effects and toxicity of pharmacological treatment in rings of rabbit aortic vessels.

Animal experiments are widely accepted in arteriosclerosis research. The aim of the present study was to establish an organ culture model (rings of rabbit aortic vessels) to investigate inhibitory estrogen effects on post injury neointima formation in the vessel wall and to examine whether these effects are cytotoxic. Estrogens are used for secondary prevention of atherosclerosis in postmenopausal women (estrogen replacement therapy/ERT). Phytoestrogens as well as the ovarian 17 beta-estradiol have been demonstrated to inhibit proliferation and migration of vascular smooth muscle cells which are key events in atherogenesis and restenosis after coronary angioplasty. In situ endothelial denudation of the thoracic and abdominal aorta was performed in female rabbits by a 3F Fogarty catheter. Segments of 5 mm were randomized in groups of n = 12 and held in culture. 17 beta-estradiol, Genistein and Daidzein were applied in concentrations of 20 microM, 30 microM, and 40 microM. Groups without estrogen treatment served as controls. The segments were investigated after 21 days. Afterwards, 3 further groups (n = 12) were held with the lowest concentrations of 17 beta-estradiol or the two phytoestrogens having been evaluated to inhibit the neointima formation significantly. After 21 days of treatment these sections were held in medium only for another 7 days to proof whether these segments were still able to proliferate. A denuded control group was held in medium only over 28 days. Compared to controls, 30 microM 17 beta-estradiol, 20 microM Genistein, and 40 microM Daidzein inhibited neointima formation significantly over 21 days. After another 7 days of cultivation in medium only the amount of neointima formation was comparable to that of non-estrogen-treated controls after 21 days. We therefore suggest that the demonstrated inhibitory effect is not explained by toxicity. In conclusion, by the use of this organ culture model it was possible to demonstrate non-toxic post injury effects of different estrogens in the vasculature. Because 24 aortic segments could be taken from one aortic vessel, the number of animals that would have been necessary for an experiment (8 to 10 per group for statistical reasons) could be markedly reduced. The results are of clinical interest because phytoestrogens and 17 beta-estradiol may offer therapeutic options for patients after coronary angioplasty regarding the process of restenosis. Because phytoestrogens do not affect the reproductive system they can also be used in men.

Animals↗