Lipophilic drugs are potential drug candidates during drug development. However, due to the need for hazardous organic solvents for their solubilization, these drugs often fail to reach the pharmaceutical market, and in doing so highlight the importance of solvent free systems. Although transdermal drug delivery systems (TDDSs) are considered prospective safe drug delivery routes, a system involving lipophilic drugs in solvent free or powder form has not yet been described. Here, we report, for the first time, a novel approach for the delivery of every kind of lipophilic drug in powder form based on an innovative polymeric system (IPS). The phase transition of powder form of lipophilic drugs due to interior chemical bonds between drugs and biodegradable polymers and formation of nano-sized colloidal structures allowed the fabrication of dissolving microneedles (DMNs) to generate a powerful TDDS. We showed that IPS based DMN with powder capsaicin enhances the therapeutic effect for treatment of the rheumatic arthritis in a DBA/1 mouse model compared to a solvent-based system, indicating the promising potential of this new solvent-free platform for lipophilic drug delivery.
Bibliographical noteFunding Information:
This work was supported by the R&D program of MSIP/COMPA ( 2015K000201 , Development of minimal pain multi-micro lancets for one-touch-smart diagnostic sensor). We would like to specially thank Miroo Kim and Chang Yeol Lee for their suggestions during the entire research study. In addition, we would like to thank Inyoung Huh and YaeRang Lee for their work during animal experiments.
© 2015 Published by Elsevier B.V.
All Science Journal Classification (ASJC) codes
- Pharmaceutical Science