Article

Preparation of griseofulvin nanoparticles from water-dilutable microemulsions.

Dipartimento di Scienza e Tecnologia del Farmaco, via P Giuria 9, Torino 10125, Italy.
International Journal of Pharmaceutics (impact factor: 3.35). 04/2003; 254(2):235-42. DOI:10.1016/S0378-5173(03)00029-2 pp.235-42
Source: PubMed

ABSTRACT Nanoparticles of griseofulvin, a model drug with poor solubility and low bioavailability, were prepared from water dilutable microemulsions by the solvent diffusion technique. Solvent-in-water microemulsion formulations containing water, butyl lactate, lecithin, taurodeoxycholate sodium salt (TDC) or dipotassium glycyrrhizinate (KG), 1,2-propanediol or ethanol were used. The formation of macroscopically homogeneous, stable, fluid, optically transparent, isotropic solutions (microemulsions) was investigated by constructing pseudo-ternary phase diagrams. In the presence of TDC or KG, microemulsion systems that remained transparent on water dilution could be obtained. The displacement of butyl lactate, with an excess of water, from the internal phase of the microemulsions containing the drug into the external phase, lead to successful fabrication of drug nanosuspensions. Nanoparticle size was dependent on microemulsion composition: using KG, griseofulvin nanoparticles below 100 nm with low polydispersity and an increased dissolution rate were obtained.

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Keywords

1,2-propanediol
 
butyl lactate
 
drug nanosuspensions
 
external phase
 
griseofulvin nanoparticles
 
increased dissolution rate
 
internal phase
 
isotropic solutions
 
microemulsion composition
 
microemulsions
 
Nanoparticle size
 
Nanoparticles
 
poor solubility
 
pseudo-ternary phase diagrams
 
solvent diffusion technique
 
Solvent-in-water microemulsion formulations
 
stable
 
taurodeoxycholate sodium salt
 
water dilutable microemulsions
 
water dilution