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.


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  (ERA 2012 Listed)    (ERA 2010 Rank A)   Check publisher's open access policy
Publication date 2012-09
Sub-type Article
DOI 10.1016/j.ijpharm.2012.09.038
Volume number 439
Issue number 1-2
ISSN 0378-5173
1873-3476
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.

 
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Created: Fri, 05 Oct 2012, 13:22:40 EST by Mrs Louise Nimwegen on behalf of School of Chemistry & Molecular Biosciences