Vaginal Absorption of a Potent Luteinizing Hormone-Releasing Hormone Analog (Leuprolide) in Rats I: Absorption by Various Routes and Absorption Enhancement

Okada, Hiroaki; Yamazaki, Iwao; Ogawa, Yasuaki; Hirai, Shinichiro; Takatsuka, Yuichi; Mima, Hiroyuki

doi:10.1002/jps.2600711214

Cited by 127 publications

(28 citation statements)

References 23 publications

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“…The absorption of GnRH by vaginal mucosa is influenced by the state of mucosa (Okada et al 1984), mucosal peptidase activity (Acartürk et al 2001), extender composition (Okada et al 1982), formulation of analogue (Padula 2005) and, probably, by semen (Vicente et al 2011). Additional research is needed to determine the effect of GnRH analogues on rabbit spermatozoa.…”

Section: Introductionmentioning

confidence: 99%

Motility, mitochondrial membrane potential and ATP content of rabbit spermatozoa stored in extender supplemented with GnRH analogue [des-Gly10, D-Ala6]-LH-RH ethylamide

Gogol¹,

Trzcińska²,

Bryła³

2014

Polish Journal of Veterinary Sciences

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The present study was aimed to determine the effect of GnRH analogue [des-Gly10, D-Ala6]-LH-RH ethylamide on the quality of rabbit spermatozoa stored at 17 o C for 3 days. Semen from 5 bucks (13 ejaculates) was used in the experiment. Ejaculates were divided and diluted at a 1:10 ratio with rabbit semen extender Galap (IMV, France) (Control) or with Galap extender supplemented with GnRH analogue [des-Gly10, D-Ala6]-LH-RH ethylamide (50 μg/ml) and stored for 3 days. Sperm motility parameters, mitochondrial membrane potential (MMP) and ATP content were assessed on each day of the experiment. Motility analysis was performed using a computer-assisted sperm analysis (CASA) system. The following sperm motility parameters were recorded: total motile spermatozoa, progressively motile spermatozoa, curvilinear velocity, straight-line velocity, average path velocity, linearity, straightness and amplitude of lateral head displacement. MMP was evaluated using JC-1 fluorescent dye. ATP content was assessed using a bioluminescence method. The addition of GnRH analogue [des-Gly10, D-Ala6]-LH-RH ethylamide to Galap extender did not affect any of the quality parameters studied. However, in both groups (Control and GnRH), significant changes in motility parameters (except straight-line velocity) and proportion of spermatozoa showing high MMP and ATP content were observed throughout 3 days of storage.

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Section: Introductionmentioning

confidence: 99%

Motility, mitochondrial membrane potential and ATP content of rabbit spermatozoa stored in extender supplemented with GnRH analogue [des-Gly10, D-Ala6]-LH-RH ethylamide

Gogol¹,

Trzcińska²,

Bryła³

2014

Polish Journal of Veterinary Sciences

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“…Similarly, rectal administration of an LH-RH analogue was more efficacious than nasal administration, but less so than Lv. or s.c. injections in rats (Okada et al, 1982). Consequently, it was determined that absorption by the rectal route is better than others.…”

Section: Absorption Of Peptides and Proteins And Effect Of Absorptionmentioning

confidence: 99%

“…The screening of promoters for the vaginal absorption of leuprolide has been carried out in diestrous rats (Okada et al, 1982). The absorption was facilitated markedly by polybasic carboxylic acids (citric, succinic, tartaric, and glycocholic acids).…”

Section: Absorption Enhancementmentioning

confidence: 99%

Rectal and Vaginal Absorption of Peptides and Proteins

Muranishi

Yamamoto

Okada

1993

Pharmaceutical Biotechnology

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“…The vaginal route is one that is also technically viable, as has been demonstrated for the LHRH analogue leoprolide (31). This route has not, however, been extensively studied, perhaps simply because it is only useful for therapies intended solely for females, and the number of these is limited.…”

Section: Rectal/vaginal Deliverymentioning

confidence: 99%

Drug delivery systems and routes of administration of peptide and protein drugs

Sanders¹

1990

Eur. J. Drug Metab. Pharmacokinet.

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The unique requirements of peptides and proteins in designing delivery systems, and the unprecedented recent growth in the field, has driven a great deal of research into novel means of drug delivery. The search for approaches that provide formulations that are stable, bioavailable, readily manufacturable, and acceptable to the patient, has led to major advances in development of nasal and controlled release technology. The field of parenteral solution technology has also seen some new demands made of it, and what was formerly a conventional area of formulation technology has made scientific advances to meet the needs of these compounds. At the same time, strides are being made in fundamental research in areas including oral delivery, transdermal delivery, and pulsatile and 'on demand' delivery of peptides and proteins.

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Vaginal Absorption of a Potent Luteinizing Hormone-Releasing Hormone Analog (Leuprolide) in Rats I: Absorption by Various Routes and Absorption Enhancement

Cited by 127 publications

References 23 publications

Motility, mitochondrial membrane potential and ATP content of rabbit spermatozoa stored in extender supplemented with GnRH analogue [des-Gly10, D-Ala6]-LH-RH ethylamide

Motility, mitochondrial membrane potential and ATP content of rabbit spermatozoa stored in extender supplemented with GnRH analogue [des-Gly10, D-Ala6]-LH-RH ethylamide

Rectal and Vaginal Absorption of Peptides and Proteins

Drug delivery systems and routes of administration of peptide and protein drugs

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