GnRH antagonists have several clinical applications in prostate cancer, regulation of ovulation induction in females, breast cancer, male contraception and others. Antagonists differ from natural GnRH decapeptide in having five or more amino acid substitutions. Whereas most of antagonists are available as subcutaneous (SC) formula for injection, some are formulated as a depot formulation for sustained release (e.g. Cetrarelix, Degarelix). Systemic delivery of cetrorelix acetate by intratracheal route can be achieved using dry powder for inhalation of adhesive mixture when the powder deposition reaches stage four. Oral route for systemic delivery of peptide without its degradation can be achieved using gastrointestinal permeation enhancement technology GIPET® provided by acyline.
Current drug delivery. 2018 Feb 14 [Epub ahead of print]
Rawda Yaseen AlSheyyab, Bashar Mohammad Al-Taani, Rana Mohammad Obeidat, Motasem Mohammad Alsmadi, Rafeef Khalid Masaedeh, Raghda Nasry Sabat
Jordan University of science and technology - pharmaceutical technology, Irbid. Jordan.