Histological changes in the ovary and uterus of rat after injectable contraceptive therapy.
TL;DR: The whole morphological alteration in the ovary after DMPA therapy appeared to be the atresia of the follicular apparatus with degeneration of the growing follicles.
About: This article is published in Contraception.The article was published on 1988-05-01. It has received 19 citations till now. The article focuses on the topics: Follicular phase & Ovary.
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TL;DR: Findings suggest that M PA treatment leads to long-lasting cognitive impairments in the rodent, even in the absence of circulating MPA in animals given prior MPA treatment, which may relate to the GABAergic system.
Abstract: Rationale
The synthetic progestin medroxyprogesterone acetate (MPA), widely used in hormone therapy (HT) and as the contraceptive Depo Provera, is implicated in detrimental cognitive effects in women. Recent evidence in aged ovariectomized (Ovx) rodents shows that short-term MPA treatment impairs cognition and alters the GABAergic system.
51 citations
Cites background or methods from "Histological changes in the ovary a..."
...This regimen of MPA treatment was selected based on previously established anti-ovulatory effects (Bhowmik and Mukherjea 1988) in order to mimic the biological action of Depo Provera taken by women (Depo Provera Prescribing Information 2006)....
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...Although it has previously been shown by Bhowmik and Mukherjea (1988) that weekly injections of 3.5 mg of MPA are sufficient to halt ovulation for at least 7 days, we confirmed this in a pilot study with animals, not included in Visible Platform behavioral testing, at 3 months of age and of the…...
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TL;DR: Encapsulation of ethinylestradiol in ultraflexible liposomes modified the pharmacodynamics and pharmacokinetics of the contraceptive agent, resulting in a marked improvement in bioavailability and optimized therapy.
Abstract: This study aimed to develop ultraflexible liposomes as an alternative to the oral route, which would enhance the bioavailability and reduce the toxicity of ethinylestradiol. Ultraflexible liposomes of ethinylestradiol using an optimized concentration of surfactants were prepared and characterized in vitro. The effect of surfactant type under non-occlusive conditions on transdermal permeability was assessed. A histopathological study was performed to assess the action of ethinylestradiol on the uterus and ovaries. The pharmacokinetics of free ethinylestradiol (following single oral administration and one day of application to the skin), ultraflexible liposomal ethinylestradiol and non-flexible liposomal ethinylestradiol were studied in female Sprague-Dawley rats. Insignificant differences in size between the ultraflexible liposomal formulations containing optimized concentrations of different surfactants were observed. Ultraflexible liposomes can penetrate through pores much smaller than their own diameter. The transdermal permeability of lipophilic surfactant was greater than that of hydrophilic surfactant. The release of ethinylestradiol from the proposed formulation through rat skin was found to be constant. The histopathological study showed that the ultraflexible liposomal transdermal drug delivery system for ethinylestradiol provided effective contraception by follicular cell lysis, depletion of zona granulosa and ova, and by increasing the uterine mucosal and endometrial proliferation. Encapsulation of ethinylestradiol in ultraflexible liposomes modified the pharmacodynamics and pharmacokinetics of the contraceptive agent, resulting in a marked improvement in bioavailability and optimized therapy.
29 citations
Cites background from "Histological changes in the ovary a..."
...The high flux rate has been attributed to naturally occurring transdermal osmotic gradients (Bhowmik & Mukherjea 1988)....
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...The morphological changes produced by the direct action on the uterine endometrium of the rats were recorded (Bhowmik & Mukherjea 1988; Thompson 1990)....
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TL;DR: In normal mammary gland of female rats: progestin action depends on estrogen presence and MPA does not revert estrogen-dependent proliferation, but it magnifies estradiol effect.
22 citations
14 Aug 2018
TL;DR: In this article, the authors provided more information on normal anatomy, histology, physiology, and endocrinology of Reproductive System and Mammary Gland, and discussed compound-related effects on the reproductive system can be pivotal in pharmaceutical development.
Abstract: This chapter provides more information on normal anatomy, histology, physiology, and endocrinology of Reproductive System and Mammary Gland. Compound-related effects on the reproductive system can be pivotal in pharmaceutical development. It considers the male and female reproductive systems together with the mammary gland as many basic concepts track across these organ systems. Embryological development of the reproductive tract is broadly similar species but there are detailed differences, particularly in the timing of events. The development of xenobiotic-induced endometrial hyperplasia in rodents has been reported in numerous studies of animals exposed in utero, prepubertally, or after ovariectomy. Postnatal testicular development varies among species, just as the timing of puberty varies. The term "puberty" denotes the time period encompassing hormonal changes, development of sexually dimorphic traits, and the achievement of fertility. Considerable confusion exists regarding the terminology of sexual maturation.
17 citations
TL;DR: These results confirm the potential of these mucoadhesive vaginal tablets to enhance P4 efficacy and avoid the side effects associated with IM injection.
Abstract: Objective: To develop mucoadhesive tablets for the vaginal delivery of progesterone (P4) to overcome its low oral bioavailability resulting from drug hydrophobicity and extensive hepatic metabolism.Methods: The tablets were prepared using mixtures of P4/Pluronic® F-127 solid dispersion and different mucoadhesive polymers. The tablets physical properties, swelling index, mucoadhesion and drug release kinetics were evaluated. P4 pharmacokinetic and pharmacodynamic properties were evaluated in female rabbits and compared with vaginal micronized P4 tablets and intramuscular (IM) P4 injection, respectively.Results: The tablets had satisfactory physical properties and their swelling, in vitro mucoadhesion force and ex vivo mucoadhesion time were dependent on tablet composition. Highest swelling index and mucoadhesion time were detected for tablets containing 20% chitosan-10% alginate mixture. Most tablets exhibited burst release (∼25%) during the first 2 h but sustained the drug release for ∼48 h. In vi...
12 citations
Cites background from "Histological changes in the ovary a..."
...Further, the uterus in rabbits administrated F12 tablets showed atrophy of epithelium of endometrial glands, probably due to local effect of high P4 concentration (Figure S1, Supporting information) [57]....
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References
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TL;DR: It is indicated that medroxyprogesterone acetate administered in this dosage acts as a contraceptive by inhibiting release of LH.
32 citations
TL;DR: Intramuscular injections of an oily suspension of 200 mg of norethisterone enanthate were given to 130 young fertile healthy women at 3-month intervals; most were treated for more than a year with the average 17.6 months.
30 citations
TL;DR: The contraceptive efficacy and menstrual abnormalities of long-acting medroxyprogesterone acetate, injected intramuscularly at doses of 150 mg every 3 months for 1 year, were studied in 14 women, finding the chief advantage is the infrequent need for injection.
25 citations
Journal Article•
TL;DR: There was no change in the endometrial or cytological picture after several years of treatment and at no time was evidence of hyperestrogenic alteration found.
23 citations
TL;DR: It is possible that map suppresses the synthesis or the release of luteinizing hormone (lh) from the pituitary gland and thus prevents the production of sufficient endogenous oestrogen to cause implantation.
Abstract: Intact, female Holtzman rats were treated daily with medroxyprogesterone acetate (map; Provera) in corn oil, beginning on the day of insemination. This caused delay of implantation in 14% (0\m=.\5mg/day) to 100% (2\m=.\4mg/day) of the animals tested. It is possible that map suppresses the synthesis or the release of luteinizing hormone (lh) from the pituitary gland and thus prevents the production of sufficient endogenous oestrogen to cause implantation. Implantation was achieved in 'delayed' rats by simultaneous administration of 1 \g=m\gof oestrone with the dose of map they had been receiving. The viability of foetuses in such animals varied inversely with the dose of map the mothers had received.
16 citations