Solubilization of tadalafil using a tartaric acid and chitosan-based multi-system

Solubilization studies of tadalafil (TDF) have recently improved the dissolution (%) using weak acids and bases in our group. However, the weak acid formulations have a low dissolution (%) of TDF as limitation. Thus, the purpose of this study was to improve the dissolution (%) of TDF over 90% in distilled water (DW) by weak acid-chitosan based multi-system.

Highlights

TDF-SD formulation with tartaric acid, polymer, and chitosan was successfully prepared using solvent evaporation method

SD11 formulation is improved the dissolution (%) of TDF compared to those of Cialis® in various dissolution media.

SD11 formulation is well maintained the stability (drug content, pre-dissolution (%), and crystallinity for 3 months.

The SD formulation (SD11: TDF, tartaric acid, chitosan, Aerosil®200, and PVP/VA S-630 in a 1:2:1:1:2 weight ratio) showed higher dissolution (%) of TDF by 5.0-, 6.0-, and 5.8-fold at 60 min than that of Cialis® in DW and pH 1.2 and pH 6.8 buffers, respectively. The physical properties of the SD11 formulation were changed. Moreover, the SD11 formulation maintained stability for 3 months. In conclusion, the solubilization of TDF using chitosan was successfully performed for the first time. Continue on solubilization of Tadalafil

Keywords and Materials: Tadalafil, Weak acid, Chitosan, Dissolution (%), Stability, Kolliphor® (P188®
and P407®), PEG6000, Kollidon® K12, Kolliphor® HS 15, polyvinyl
alcohol-polyethylene glycol graft-copolymer (Kollicoat® IR), polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®), and D-α-tocopherol polyethylene glycol 1000 succinate
(TPGS),  PVP/VA S-630, Aerosil®200, Chitosan, tartaric acid