Preparation of griseofulvin nanoparticles from water-dilutable microemulsions.
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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ABSTRACT: Nanosuspensions have attracted much interest of many scientists as a new approach to deliver poorly soluble drugs because of their process flexibility and special advantages such as improved oral bioavailability, high drug loading, targeting capabilities and so on. Recently, the manufacture processes of nanosuspensions have developed quickly, and some new methods have emerged, for example, controlled precipitation, emulsion method, microemulsion method and melt-emulsion method. Additionally, the post-process of nano-suspension has also gained great progresses to expand the utility of nanosuspensions, including solidification technique and surface modification technique. Moreover, the study on targeting delivery by nanosuspension following intravenous administration has become a hot topic of many researches. In the article, we will highlight new developments in the production of nanosuspensions and summarize the application of nanosuspensions via a variety of administration routes. In the end, we will overview the research and development prospectives of nanosuspensions.
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ABSTRACT: Most of the new chemical entities coming out from High-throughput screening in drug discovery process are failing due to their poor solubility in the water. Poorly water-soluble drugs show many problems in formulating them in conventional dosage forms. One of the critical problems associated with poorly soluble drugs is too low bioavailability. The problem is even more complex for drugs belonging to BCS CLASS II category, as they are poorly soluble in both aqueous and organic media, and for those drugs having a log P value of 2. There are number of formulation approaches to resolve the problems of low solubility and low bioavailability. These techniques for solubility enhancement have some limitations and hence have limited utility in solubility enhancement. Nanotechnology can be used to resolve the problems associated with these conventional approaches for solubility and bioavailability enhancement. Nanotechnology is defined as the science and engineering carried out in the nanoscale that is 10-9 meters. The present article describes the details about nanosuspensions. Nanosuspensions consist of the pure poorly water-soluble drug without any matrix material suspended in dispersion. The review article includes the methods of preparation with their advantages and disadvantages, characterization and evaluation parameters and pharmaceutical applications. A nanosuspension not only solves the problems of poor solubility and bioavailability but also alters the pharmacokinetics of drug and thus improves drug safety and efficacy.International Journal of Pharmaceutical Sciences and Research. 09/2010; 1(9-0975-8232):1-11.