NGHIÊN CỨU ĐIỀU CHẾ MICROEMULGEL CHỨA DIOSMIN VÀ QUERCETIN

Abstract

Diosmin and quercetin are active ingredients, possess anti-inflammatory effects, stabilize blood vessels, and could be the potential API  for transdermal formulations for the treatment of varicose veins. Both diosmin and quercetin have poor water solubility. This study aimed at developing a microemulgel dosage form containing diosmin and quercetin (DQE). The solubility of diosmin and quercetin in excipients was investigated by using the saturation method to select excipients of microemulsion. The phase diagram was constructed using the water titration method. Active ingredients were loaded into selected microemulsion formulations and evaluated for organoleptic, pH, viscosity, and particle size. The physical stability of microemulsion containing diosmin and quercetin (DQM) was evaluated through 6 thermal cycles, each cycle consisted of 2 phases: 4 ± 1^oC for 48 hours and 45 ± 1^oC for 48 hours and high-speed centrifugation at 10000 rpm for 30 minutes. DQE was prepared from DQM and investigated in combination with different gelling excipients (HPMC, Sepinov Derm, Sepimax Zen). The properties of DQE were evaluated including: organoleptic, pH, viscosity, and thinness. The selected DQM had a droplet size of 165.6 ± 2.0 nm (PDI=0.267) and was resistant to thermal and centrifugation tests. The chosen DQE consisted of Plurol oleique CC479: Cremophor RH 40: Transcutol P: Water: Sepinov Derm with the ratios of 15%: 16.67%: 8.33%: 60%: 0.1% (kl/kl), respectively. The contents of diosmin and quercetin in DQE were 0.005% and 0.01% (w/w), respectively. DQE had a pH of 3.95 and possessed the pseudoplastic non-Newtonian rheological properties. The study has successfully developed a DQE formulation containing 0.005% diosmin and 0.01% quercetin. The results could be useful for the development of a transdermal dosage form to support the treatment of varicose veins.