title: Leuprolide acetate: pharmaceutical use and delivery potentials.
abstract: BACKGROUND
  Thanks to recent advances in biotechnology, the use of peptides and proteins as drugs has become a concrete clinical reality, and consequently an interesting challenge has emerged for non-parenteral drug delivery. Leuprolide is a synthetic nonapeptide agonist to the luteinizing hormone-releasing hormone (LH-RH) receptor with principal clinical applications for prostate cancer. Although a large number of formulations available, they mainly consist in depot subcutaneous injections or implantable devices. Both of these routes of administration present multiple limitations considering the large clinical applications of this active substance.
  
  
  METHODS
  The objective of this review is to critically discuss the formulations currently available on the market for leuprolide optimization and to consider how drug delivery plays an important role in improving the bioavailability of this compound.
  
  
  CONCLUSIONS
  Due to its physicochemical properties and its economical market, leuprolide is an interesting candidate for drug delivery to improve the efficacy of existing treatments, dose adjustments, and patient compliance and safety.
authors.affiliation: Univ Paris Sud, UMR CNRS 8612, IFR 141, Faculté de Pharmacie, Châtenay-Malabry, France. d.teutonico@lacdr.leidenuniv.nl
authors.forename: Donato
authors.initials: D
authors.lastname: Teutonico
authors.forename: Silvia
authors.initials: S
authors.lastname: Montanari
authors.forename: Gilles
authors.initials: G
authors.lastname: Ponchel
mesh_terms: D000279:Administration, Cutaneous; D000281:Administration, Intranasal; D000284:Administration, Oral; D000286:Administration, Sublingual; D000595:Amino Acid Sequence; D018931:Antineoplastic Agents, Hormonal / Q000008:administration & dosage / Q000737:chemistry; D001943:Breast Neoplasms / Q000188:drug therapy; D002626:Chemistry, Pharmaceutical; D004715:Endometriosis / Q000188:drug therapy; D005260:Female; D005831:Genital Diseases, Female / Q000188:drug therapy*; D007987:Gonadotropin-Releasing Hormone / Q000819:agonists; D006801:Humans; D007263:Infusions, Parenteral; D007279:Injections, Subcutaneous; D016729:Leuprolide / Q000008:administration & dosage* / Q000737:chemistry; D008297:Male; D011471:Prostatic Neoplasms / Q000188:drug therapy*; D011629:Puberty, Precocious / Q000188:drug therapy; D011966:Receptors, LHRH / Q000819:agonists
chemical_list: D018931:Antineoplastic Agents, Hormonal; D011966:Receptors, LHRH; D007987:Gonadotropin-Releasing Hormone; D016729:Leuprolide