Solubility Enhancement of Lipophilic Drugs via Novel Vesicular System

Abstract

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 results obtained previously, a vesicular self-assembled carrier
was developed, optimized and evaluated with respect to the drug loading,
entrapment efficiency and in vitro drug 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 with a 3–5 fold higher solubility of drug than pure
drug. It was verified that in vitro drug release lasted more than 24 hours in the
case of controlled drug delivery. The optimized formulation was highly stable
under physiological conditions itself. Additionally, ex vivo permeation showed
more possibility of 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 vivo evaluation and clinical translational
approach to prove this system’s application in pharmaceuticals.