Enhancement of transdermal delivery of progesterone using medium-chain mono and diglycerides as skin penetration enhancers.

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  • Author(s): Lopes LB;Lopes LB; Murphy N; Nornoo A
  • Source:
    Pharmaceutical development and technology [Pharm Dev Technol] 2009; Vol. 14 (5), pp. 524-9.
  • Publication Type:
    Journal Article; Research Support, Non-U.S. Gov't
  • Language:
    English
  • Additional Information
    • Source:
      Publisher: Informa Healthcare Country of Publication: England NLM ID: 9610932 Publication Model: Print Cited Medium: Internet ISSN: 1097-9867 (Electronic) Linking ISSN: 10837450 NLM ISO Abbreviation: Pharm Dev Technol Subsets: MEDLINE
    • Publication Information:
      Publication: London : Informa Healthcare
      Original Publication: Monticello, NY : Marcel Dekker, c1996-
    • Subject Terms:
      Glycerides/*pharmacology ; Monoglycerides/*pharmacology ; Progesterone/*administration & dosage ; Skin/*metabolism ; Skin Absorption/*drug effects; Administration, Cutaneous ; Animals ; Cell Survival/drug effects ; Mice ; Propylene Glycol ; Skin/drug effects ; Swine ; Swiss 3T3 Cells
    • Abstract:
      We evaluated whether medium-chain mono and diglycerides (MCG) can be utilized to optimize the transdermal delivery of progesterone (PGT). MCG was studied at 10-70% (w/w) in propylene glycol (a polar solvent) or Myvacet oil (nonpolar solvent); PGT was used at 1% (w/w). The topical (to the skin) and transdermal (across the skin) delivery of PGT were evaluated in vitro using porcine ear skin. When incorporated in propylene glycol, MCG at 10% enhanced the topical and transdermal delivery of PGT by 2.5- and 7-fold, respectively. At 20-50%, topical delivery was further enhanced while transdermal delivery gradually returned towards baseline. At 70%, MCG enhanced neither the delivery to viable skin nor the transdermal delivery of PGT. Similar concentration-dependent effects were observed when MCG was incorporated in Myvacet oil, but their magnitudes were 2- to 3-fold smaller. The relative safety of MCG was assessed in cultured fibroblasts and compared to propylene glycol (regarded as safe) and sodium lauryl sulfate (moderate-to-severe irritant). Both MCG and propylene glycol were substantially less cytotoxic than sodium lauryl sulfate. We conclude that formulations containing 10% MCG in propylene glycol may be a simple and safe method to improve the transdermal delivery of progesterone and promote its use in hormone replacement therapy.
    • Accession Number:
      0 (Glycerides)
      0 (Monoglycerides)
      4G7DS2Q64Y (Progesterone)
      6DC9Q167V3 (Propylene Glycol)
    • Publication Date:
      Date Created: 20090626 Date Completed: 20091117 Latest Revision: 20131121
    • Publication Date:
      20240829
    • Accession Number:
      10.1080/10837450902814180
    • Accession Number:
      19552564