纳米医学与纳米技术杂志

抽象的

Design and Characterization of Nanocrystals of Lovastatin for Solubility and Dissolution Enhancement

Basavaraj K. Nanjwade, Ganesh K. Derkar, Hiren M. Bechra, Veerendra K. Nanjwade and F.V. Manvi

A major hurdle in pharmaceutical formulation is water insolubility of most of the drugs affecting stability and bioavailability of the drug, if the drug is also insoluble in organic medium, it is difficult to deliver the drug in a sufficiently bioavailable form and hence it is a great challenge to formulation researchers to overcome such difficulty. Although some approaches are available for enhancing the dissolution of poorly soluble drugs but has certain draw backs like low drug loading and large doses. However, a new solution to poorly water soluble drug candidates is now available i.e. nanonisation and it leads to much more soluble, more biologically available and safer dosage form of poorly soluble and poorly bioavailable drugs. In the present work, a nanocrystal of lovastatin was formulated by using simple precipitation method without using stabilizer or surfactant and it was found that formulation at 3 mM concentration of drug with the acetone and methanol as a solvent and at proper dilution (50 times) of drug solution with water, nanocrystals with less particle size is possible with slight change in crystallinity. It has also shown that, the drug has enhanced saturation solubility, increased dissolution rate and more bioavailable in biological fluid when drug formulated by using acetone and methanol as a solvent. Whereas drug formulation with acetonitrile has large particle size, less saturation solubility and low rate of dissolution.