The effect of water-soluble polymers, PEG and PVP, on the solubilisation of griseofulvin in aqueous micellar solutions of Pluronic F127.

The purpose of this study was to investigate the possibility of enhancing the solubilisation capacity of micellar solutions of Pluronic F127 for the poorly water-soluble drug griseofulvin by co-formulating with a water-soluble polymer. The effect of the addition of the polyethylene glycols PEG6000 and 35000, and the poly(vinylpyrrolidone)s PVP K30 and K90, on the solubilisation capacity of 1wt% solutions of Pluronic F127 was related to the effect of these additives on particle size as determined by dynamic light scattering measurements. The addition of PEG35000 to 1wt% F127 solutions significantly increased the solubility capacity expressed in terms of unit weight of F127; PVP K90 had a smaller effect but no enhancement was noted following the addition of PEG6000 or PVP K30.

The effect of polymeric additives on the solubilisation of a poorly-soluble drug in micellar solutions of Pluronic F127.

The solubilisation of griseofulvin in 1wt% aqueous micellar solutions of Pluronic F127 at 37°C has been modified by adding polyethylene glycol PEG 35000 or poly(vinylpyrrolidone) PVP K30. The solubilisation capacity expressed in terms of unit weight of F127 is increased by the addition of 0.5wt% PEG 35000 to a value approaching double that of a 2.

Solubilisation of griseofulvin, quercetin and rutin in micellar formulations of triblock copolymers E62P39E62 and E137S18E137.

The solubilisation of two poorly soluble flavonoids, quercetin and rutin, in micellar solutions of mixtures of a block copolymer of ethylene oxide and styrene oxide (E(137)S(18)E(137)) with one of ethylene oxide and propylene oxide (E(62)P(39)E(62)) has been studied at 25 and 37 degrees C. Solubilisation capacities were higher than those for the model poorly water-soluble drug griseofulvin and comparable with published values for the solubilisation of rutin by beta-cyclodextrin.

Solubilisation of griseofulvin in aqueous micellar solutions of diblock copolymers of ethylene oxide and 1,2-butylene oxide with lengthy B-blocks.

The influence of hydrophobic-block length on solubilisation capacity was examined for micelles of E(m)B(n) copolymers (E=oxyethylene, B=oxybutylene, subscripts denote number-average block lengths in repeat units) with B-block lengths in the range of 30-76 and with E-blocks of sufficient length to ensure the formation of spherical micelles. Griseofulvin was used as a model poorly-water-soluble drug known to be almost exclusively solubilised in the micellar core. Combination of solubilisation data with those of a previous study has shown that the amount of drug solubilised per gram of hydrophobe is essentially independent of B-block length when this exceeds about 15 B units, suggesting that core size is not a major influence on solubilisation.

Diblock copolymers of ethylene oxide and 1,2-butylene oxide in aqueous solution: formation of unimolecular micelles.

The dependence of log(cmc) on hydrophobic block length n was examined for E(m)B(n) copolymers (E=oxyethylene, B=oxybutylene, subscripts denote number-average block lengths in repeat units) with n in the range 30-76. Combination with published data for E(m)B(n) diblock copolymers with shorter E-blocks shows two changes of slope in the log(cmc)-n plot corresponding to the onset of unimolecular micelle formation at n approximately 12 and completion of this process at n approximately 30. The results are discussed with reference to published data for E(m)L(n) and E(m)CL(n) (L from d,L-lactide; CL from epsilon-caprolactone) copolymers, which show similar behaviour.