A review of poloxamer 407 pharmaceutical and pharmacological characteristics.
Poloxamer 407 copolymer (ethylene oxide and propylene oxide blocks) shows thermoreversible properties, which is of the utmost interest in optimising drug formulation (fluid state at room temperature facilitating administration and gel state above sol-gel transition temperature at body temperature promoting prolonged release of pharmacological agents). Pharmaceutical evaluation consists in determining the rheological behaviour (flow curve or oscillatory studies), sol-gel transition temperature, in vitro drug release using either synthetic or physiological membrane and (bio)adhesion characteristics. Poloxamer 407 formulations led to enhanced solubilisation of poorly water-soluble drugs and prolonged release profile for many galenic applications (e.g., oral, rectal, topical, ophthalmic, nasal and injectable preparations) but did not clearly show any relevant advantages when used alone. Combination with other excipients like Poloxamer 188 or mucoadhesive polymers promotes Poloxamer 407 action by optimising sol-gel transition temperature or increasing bioadhesive properties. Inclusion of liposomes or micro(nano)particles in Poloxamer 407 formulations offers interesting prospects, as well. Besides these promising data, Poloxamer 407 has been held responsible for lipidic profile alteration and possible renal toxicity, which compromises its development for parenteral applications. In addition, new findings have demonstrated immuno-modulation and cytotoxicity-promoting properties of Poloxamer 407 revealing significant pharmacological interest and, hence, human trials are in progress to specify these potential applications.
Dumortier
Gilles
G
Laboratoire de Galénique, UPRES EA 2498, Faculté des Sciences Pharmaceutiques et Biologiques (Université Paris 5), 4, Avenue de l'Observatoire, 75270, Paris Cedex 06, France. gilles.dumortier@univ-paris5.fr
Grossiord
Jean Louis
JL
Agnely
Florence
F
Chaumeil
Jean Claude
JC
D000818:Animals; D049109:Cell Proliferation / Q000187:drug effects; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D002627:Chemistry, Physical; D005079:Excipients / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D006801:Humans; D007155:Immunologic Factors / Q000494:pharmacology; D020442:Poloxamer / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D013816:Thermodynamics
D005079:Excipients; D007155:Immunologic Factors; D020442:Poloxamer