Lipidated analogues of luteinizing hormone-releasing hormone (LHRH) reduce serum levels of follicle-stimulating hormone (FSH) after oral administration

Mansfeld, Friederike M. and Toth, Istvan (2012) Lipidated analogues of luteinizing hormone-releasing hormone (LHRH) reduce serum levels of follicle-stimulating hormone (FSH) after oral administration. International Journal of Pharmaceutics, 439 1-2: 216-222. doi:10.1016/j.ijpharm.2012.09.038


Author Mansfeld, Friederike M.
Toth, Istvan
Title Lipidated analogues of luteinizing hormone-releasing hormone (LHRH) reduce serum levels of follicle-stimulating hormone (FSH) after oral administration
Journal name International Journal of Pharmaceutics   Check publisher's open access policy
ISSN 0378-5173
1873-3476
Publication date 2012-09
Sub-type Article (original research)
DOI 10.1016/j.ijpharm.2012.09.038
Volume 439
Issue 1-2
Start page 216
End page 222
Total pages 7
Place of publication Amsterdam, Netherlands
Publisher Elsevier
Collection year 2013
Language eng
Abstract A diverse range of diseases involving the reproductive system are treated with luteinizinghormone-releasinghormone (LHRH) agonists which must be administered daily. Currently, an efficient oral delivery system is not available. Here, we show the facile inclusion of lipoamino acids into the peptide sequence of LHRH, rendering it more stable towards enzymatic degradation, as well as enhancing permeability across Caco-2 cell monolayers. Selected LHRH derivatives were tested in vivo by daily oral administration to rats. The size and weight of the sex organs remained unchanged and the levels of LH were stable over the course of the experiment. However, some of the lipidic peptides (3, 8 and 9) were able to reduce serum levels of follicle-stimulating hormone (FSH), an important finding towards the development of orally available LHRH agonists.
Keyword Luteinizing hormone-releasing hormone
Agonist
Oral peptide delivery
Lipoamino acid
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ
Additional Notes Available online: 26 September 2012. In Press, Uncorrected Proof.

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2013 Collection
School of Chemistry and Molecular Biosciences
School of Pharmacy Publications
 
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