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

Abstract

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.

Quantification of Lovastatin Produced by Monascus purpureus

“…The defined production medium had the following composition (in g/L): dextrose, 29 The pH was adjusted to 6 [24]. A 500-mL Erlenmeyer flask containing 100 mL of sterile medium was inoculated with 10% (v/v) seed culture and incubated at 30 0 C for 15 days on a rotary shaker maintained at 120 rpm [18].…”

“…Hence, the quantification of the individual forms of lovastatin as well as hydrolyzed/metabolized products of lovastatin is necessary to determine the metabolic rate in controlled delivery systems. Several reports use the spectrophotometric method of quantification of in vitro and in vivo drug release characteristics [29][30][31][32][33][34][35]. A few studies have reported the controlled release characteristics of lovastatin in vitro by measuring lovastatin using UV-visible spectrophotometer and in vivo release characteristics of lovastatin measured by HPLC technique [29,36].…”

“…The phosphate alone appears to be a potential interfering component as observed from the present study. Several reports suggested spectrophotometric measurement for those in vitro and in vivo release characteristics of the drug [29][30][31][32][33][34][35]. Also, a few articles reported the release characteristics of the drug in vitro by UV-visible spectrophotometry and in vivo release characteristics using HPLC analysis, considering the competitive molecules in the serum [29,36].…”

Nanotextiles- A Broader Perspective

“…Based on the use of sub-units nanoparticles are systematically arranged [4]. In the field of textiles, nanotechnology has been used in synthesis of quantum dot [5,6] called semiconductor nanocrystals [7]. Dye molecules are used to make fibers.…”

Nanotechnology in Agriculture

“…Nanotechnology is based on the introduction of novel Nano-materials which can result in revolutionary new structures and devices using extremely biological sophisticated tools to precisely position molecule [16]. Nanoparticles technology has emerged as a strategy to tackle [17] developing new materials and selecting appropriate materials for each specific treatment, other factors need to be optimally selected in order to design better targeted Nano particles. These factors include the particles size, shape, sedimentation, drug encapsulation efficacy, desired drug release profiles, distribution in the body, circulation, and cost [18].…”