Formulation Development and Evaluation of Gastroresistant Microparticles of Diosmin for the Treatment of Chronic Venous Insufficiency (CVI)

Abstract

Diosmin exhibits antioxidant and anti-inflammatory activities, improves venous tone and is used for the treatment of chronic venous insufficiency. In this research, Gastroresistant microparticles of diosmin were prepared by a spray-drying process using cellulose acetate phthalate (CAP) as enteric polymer and a series of enhancers of dissolution rate, such as sodium carboxymethylcellulose (NaCMC), sodium lauryl sulphate and Tween 80. The raw materials were characterized by DSC. The prepared microparticles were analyzed by DSC and scanning electron microscopy. In-vitro dissolution tests were carried out using a pH-change method to find out the influence of formulative parameters on the drug release from microparticles. The presence of a combination of CAP and enhancers in the formulations produced microparticles with good resistance at low pH of the gastric fluid and complete flavanoid release in the simulated intestinal environment. The spraydrying technique and the process conditions selected for microparticles were able to give satisfactory encapsulation efficiency, production yield, microparticles morphology and a complete drug release in the intestine