Solubility Enhancement of Lipophilic Drugs via Novel Vesicular System

Background: Pharmaceutical development of lipophilic drugs is deficient for poor aqueous solubility which causes decreased bioavailability and therapeutic efficiency.Objective:The aim of this study was to utilize a new vesicular system to increase solubility and bioavailability of poorly water-soluble drugs.Methodology: In order to enhance the solubility and release into the digestive tract of diacerein (DCT), phospholipid base, polyethylene glycol 400, and tween 80 were used to synthesize liquid proliposomes. Water has a low solubility for dialerase, but organic solvents make it soluble.Results: Based on previous results, a vesicular self-assembled carrier was developed, optimized and evaluated with respect to the drug loading, entrapment efficiency and in vitrodrug release. The formulation and particle size was prepared by modifying a thin film hydration method and a uniform distribution of nano sized particles was obtained by particle size analysis. Solubility studies resulted in a 3–5 fold higher solubility than pure drug. It was verified that in vitrodrug release lasted more than 24 h in the case of controlled drug delivery. Optimized formulation was highly stable under physiological conditions itself. Additionally, ex vivopermeation showed more possibilityof drug absorption and thus bioavailability. The study shows potential of vesicular carriers to resolve the solubility problem of lipophilic drugs. This approach, therefore, has opened doors towards new avenues for potentiating the therapeutic efficacy and patient compliance using novel approaches. Conclusion: This novel system proved to be effective and therefore future research should focus on this system’s in vivoevaluation and clinical translational approach to prove this system’s application in pharmaceuticals.