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dc.contributor.authorHayeshi, Rose
dc.contributor.authorErasmus, Linné
dc.contributor.authorScholtz, Liezl-Marie
dc.contributor.authorVenter, Kobus
dc.contributor.authorBester, Cor
dc.contributor.authorFick, Antoinette
dc.contributor.authorLeussa, Nyango-Nkeh Adrienne
dc.contributor.authorGrobler, Anne
dc.date.accessioned2019-09-13T10:57:32Z
dc.date.available2019-09-13T10:57:32Z
dc.date.issued2019
dc.identifier.citationHayeshi, R. et al. 2019. The effect of entrapment of a peptide in Pheroid® on pharmacokinetics and testosterone levels. Drug Safety Africa 2018 Conference, 20-22 Nov 2018, Potchefstroom, South Africa. Journal of pharmacological and toxicological methods, 98: Abstract no 017. [https://doi.org/10.1016/j.vascn.2019.106608]en_US
dc.identifier.issn1056-8719
dc.identifier.issn1873-488X (Online)
dc.identifier.urihttp://hdl.handle.net/10394/33315
dc.identifier.urihttps://www.sciencedirect.com/science/article/pii/S1056871919303260
dc.identifier.urihttps://doi.org/10.1016/j.vascn.2019.106608
dc.description.abstractGoserelin is a peptide drug that suppresses levels of testosterone and oestradiol [1]. The current formulation is presented in a sustained-release depot with several approved indications such as treatment of endometriosis, prostate cancer and breast cancer. The depots are placed subcutaneously with a large bore needle, hence there is a need for less invasive administration. An oral formulation in a drug delivery system such as Pheroid® would offer ease of administration to the patient, improved bioavailability as well as reduced manufacturing costs [2]. Therefore, the aim of this study was to determine the effect of entrapment of goserelin in Pheroid® on the pharmacokinetics (PK) of goserelin as well as the pharmacodynamic (PD) effects, in mice. Goserelin was entrapped in Pheroid® and characte- rized in terms of size, zeta potential and morphology. Male Balb/c mice, 6–8 weeks old were administered goserelin subcutaneously and goserelin entrapped in Pheroid® orally. At selected time points, mice were euthanised, blood collected and analysed for goserelin and testosterone levels by LCMS/MS to determine the PK and PD effects respectively. The size and zeta potential of Pheroid® remained in the expected ranges suggesting that entrapment of goserelin had no effect on Pheroid® vesicle size and stability. Confocal imaging showed satisfactory quality of the Pheroid® and goserelin did not have any effect on the Pheroid® structure. Entrapment of goserelin in Pheroid led to detectable levels of goserelin in plasma of the mice and a corresponding decrease in testosterone levels. The results suggest that Pheroid® may improve the oral bioavailability of goserelin and could be a potential strategy for an oral formulation which would be less invasive for patientsen_US
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.titleThe effect of entrapment of a peptide in Pheroid® on pharmacokinetics and testosterone levelsen_US
dc.typePresentationen_US
dc.contributor.researchID11008857 - Grobler, Anne Frederica
dc.contributor.researchID26419904 - Hayeshi, Rose Khavogoi
dc.contributor.researchID23389907 - Erasmus, Linné
dc.contributor.researchID20969120 - Scholtz, Liezl-Marie
dc.contributor.researchID11680105 - Fick, Antoinette
dc.contributor.researchID10070095 - Bester, Cornelius Johannes Jacobus
dc.contributor.researchID30084504 - Leussa, Nyango-Nkeh Adrienne
dc.contributor.researchID29572983 - Venter, J.D.


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