dc.contributor.author | Hayeshi, Rose | |
dc.contributor.author | Erasmus, Linné | |
dc.contributor.author | Scholtz, Liezl-Marie | |
dc.contributor.author | Venter, Kobus | |
dc.contributor.author | Bester, Cor | |
dc.contributor.author | Fick, Antoinette | |
dc.contributor.author | Leussa, Nyango-Nkeh Adrienne | |
dc.contributor.author | Grobler, Anne | |
dc.date.accessioned | 2019-09-13T10:57:32Z | |
dc.date.available | 2019-09-13T10:57:32Z | |
dc.date.issued | 2019 | |
dc.identifier.citation | Hayeshi, 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.issn | 1056-8719 | |
dc.identifier.issn | 1873-488X (Online) | |
dc.identifier.uri | http://hdl.handle.net/10394/33315 | |
dc.identifier.uri | https://www.sciencedirect.com/science/article/pii/S1056871919303260 | |
dc.identifier.uri | https://doi.org/10.1016/j.vascn.2019.106608 | |
dc.description.abstract | Goserelin 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 patients | en_US |
dc.language.iso | en | en_US |
dc.publisher | Elsevier | en_US |
dc.title | The effect of entrapment of a peptide in Pheroid® on pharmacokinetics and testosterone levels | en_US |
dc.type | Presentation | en_US |
dc.contributor.researchID | 11008857 - Grobler, Anne Frederica | |
dc.contributor.researchID | 26419904 - Hayeshi, Rose Khavogoi | |
dc.contributor.researchID | 23389907 - Erasmus, Linné | |
dc.contributor.researchID | 20969120 - Scholtz, Liezl-Marie | |
dc.contributor.researchID | 11680105 - Fick, Antoinette | |
dc.contributor.researchID | 10070095 - Bester, Cornelius Johannes Jacobus | |
dc.contributor.researchID | 30084504 - Leussa, Nyango-Nkeh Adrienne | |
dc.contributor.researchID | 29572983 - Venter, J.D. | |