Pluronic and Tetronic Copolymers with Polyglycolyzed Oils as Self-Emulsifying Drug Delivery Systems

Abstract

Abstract. The potential of poly(ethylene oxide)-poly(propylene oxide) block copolymers Pluronic® F127 (PF127) and Tetronic® 304 (T304), 904 (T904) and 1307 (T1307) as components of solid self-(micro) emulsifying dosage forms, S(M)EDDS, was evaluated. The dependence of the self-associative properties of Tetronics on pH explained the low ability of the micelles to solubilize griseofulvin at acid pH (sevenfold increase) compared to at alkaline pH (12-fold). Blends of polyglycolyzed glycerides (Labrasol, Labrafac CC, and Labrafil M 1944CS) with each copolymer at two different weight ratios (80:20 and 60:40) were prepared, diluted in water, and characterized in terms of globule size, appearance and griseofulvin solubility. The blends with Labrasol led to microemulsions that are able to increase drug solubility up to 30-fold. SMEDD hard gelatine capsules filled with griseofulvin and Labrasol or Labrasol/ copolymer 80:20 showed a remarkable increase in drug solubility and dissolution rate, particularly when T904, T1307 or PF127 was present in the blend. This effect was more remarkable when the volume of the dissolution medium was 200 ml (compared to 900 ml), which can be related to a higher stability of the microemulsion when there is a greater concentration of the copolymer and glyceride in the medium.

Photodynamic Effects of Zinc(II) Phthalocyanine‐Loaded Polymeric Micelles in Human Nasopharynx KB Carcinoma Cells

“…These results are in full agreement with previous studies and indicate that the size of the micellar core is the predominant parameter influencing the solubilization of Pc9 .…”

Induced micellization and micellar transitions in aqueous solutions of non-linear block copolymer Tetronic® T904

“…These copolymers play an important role in the withdrawing of water and are used in corrosion prevention in well service fluids. There have been very few studies on the surface activity [12,13], micellization, [14][15][16][17], solubilizing [15,17], emulsifying/demulsifying [11,12,[17][18][19], behavior of Tetronic Ò surfactants.…”

Dissolution Modulating Mechanism of Flurbiprofen Solid Dispersions: Characterization, Physical Stability and in vivo Performance: Formulation Considerations and optimization study

“…The dispersions were then ground with a mortar and pestle and sifted (Dispersion A). 7,8 Coprecipitation Method FLP and polymers were dissolved in dichloromethane (50 ml) and transferred to diethyl ether (100 ml) at 0°C while being gently stirred. The precipitates obtained were filtered using Whatman no.…”

“…The dried samples were milled and sifted to get coprecipitates (Dispersion B) (Method B). 7,8 Determination of Drug Content 10 mg of each solid dispersion were accurately weighed and dissolved in 10 ml of volumetric flask with pH 7.4, filtered and 1 ml of sample was diluted with double distilled water up to 10 ml and assayed spectrophotometrically for FLP at 247 nm using calibration curve based on standard solutions in double distilled water. Results are expressed both as the drug content (mg incorporated drug) and percent incorporation (actual amount of drug in solid dispersions Vs initially added amount).…”