A Review of Poloxamer 407 Pharmaceutical and Pharmacological Characteristics

Abstract

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.

Enhancement of intratumoral cyclophosphamide pharmacokinetics and antitumor activity in a P450 2B11-based cancer gene therapy model

“…This biocompatible polymer dissolves in aqueous solution at 4 1C, but rapidly forms a gel upon shifting the temperature to 37 1C and can be used to effect slow release of lipophilic drugs and other small molecules as well as large particles such as viruses. 23,33,46 Overall exposure of the tumor mass to 4-OH-CPA was increased 3.9-fold by i.t. CPA delivery via the slow release polymer, as indicated by AUC, and antitumor activity was correspondingly enhanced, as indicated by early onset and more extensive tumor regression.…”

Development of a Nanocrystalline Paclitaxel Formulation for Hipec Treatment

“…In addition, these surfactants are known to increase the solubility of low soluble drugs, and have cytotoxicity-promoting properties as they interact with multi-drug resistance cancer tumors, resulting in drastic sensitization of these tumors to the cytostatic drugs (16)(17)(18). A wet milling cycle during 24 h did not yield nanocrystalline PTX when Pluronic F68 ® was used as stabilizer (independent of the PTX/stabilizer ratio) ( Table I).…”

Double-Layered Matrix of Shellac Wax-Lutrol in Controlled Dual Drug Release

“…S and L are moldable materials; therefore, they can be fabricated into a tablet using a molding technique by melting and cooling. The hydrophilic polymer can tune up the drug release profile of a waxy matrix because it can create pores and channels on the wax matrix to allow the penetration of dissolution medium (6,17). The addition of L to modulate the drug release of monolithic S tablet has been reported previously (7) which the sustainable drug release was obtained.…”