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Influence of the dissolution medium on the release of dehydroepiandrosterone from lipophilic suppositories

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Kasperek1 R., Galczynski K., Nalesniak M., Iwaniak K., Poleszak E.
Current Issues in Pharmacy and Medical Sciences
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2014
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vol. 27
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issue 1
46-50
EN
Suppositories with cocoa butter containing dehydroepiandrosterone (DHEA) without and with the addition of Span 80 and Tween 80 as surfactants with low and high HLB values were prepared. The physical properties and the drug content of all prepared suppositories were in accordance with the pharmacopoeial requirements. The release study tests in three dissolution media such as water, lactic acid solution at pH 4.2 and phosphate buffer at pH 7.4 were carried out. In acidic and alkalic media only about 10% and 27% of DHEA were released, respectively. The addition of Span 80 to the suppository mass did not improve the release process, but the addition of Tween 80 caused the increase in the amount of DHEA released in the acidic medium to about 35%. The data showed that rectal administration of suppositories with DHEA based on cocoa butter caused about 30% availability and after vaginal administration, only topical activity can be expected. By the addition of Tween 80 to the suppository mass availability of DHEA of about 35% from vaginal suppositories can be achieved.
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Neuroprotective effects of dehydroepiandrosterone (DHEA) in rat model of Alzheimer's disease

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Aly H. F., Metwally F. M., Ahmed H. H.
Acta Biochimica Polonica
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2011
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vol. 58
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issue 4
513-520
EN
The current study was undertaken to elucidate a possible neuroprotective role of dehydroepiandrosterone (DHEA) against the development of Alzheimer's disease in experimental rat model. Alzheimer's disease was produced in young female ovariectomized rats by intraperitoneal administration of AlCl3 (4.2 mg/kg body weight) daily for 12 weeks. Half of these animals also received orally DHEA (250 mg/kg body weight, three times weekly) for 18 weeks. Control groups of animals received either DHAE alone, or no DHEA, or were not ovariectomized. After such treatment the animals were analyzed for oxidative stress biomarkers such as hydrogen peroxide, nitric oxide and malondialdehyde, total antioxidant capacity, reduced glutathione, glutathione peroxidase, glutathione reductase, superoxide dismutase and catalase activities, antiapoptotic marker Bcl-2 and brain derived neurotrophic factor. Also brain cholinergic markers (acetylcholinesterase and acetylcholine) were determined. The results revealed significant increase in oxidative stress parameters associated with significant decrease in the antioxidant enzyme activities in Al-intoxicated ovariectomized rats. Significant depletion in brain Bcl-2 and brain-derived neurotrophic factor levels were also detected. Moreover, significant elevations in brain acetylcholinesterase activity accompanied with significant reduction in acetylcholine level were recorded. Significant amelioration in all investigated parameters was detected as a result of treatment of Al-intoxicated ovariectomized rats with DHEA. These results were confirmed by histological examination of brain sections. These results clearly indicate a neuroprotective effect of DHEA against Alzheimer's disease.
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