Formulation, In Vitro Evaluation, and Toxicity Studies of A. vulgaris-co-AAm Carrier for Vildagliptin

Abstract

This study investigated the use of Artemisia vulgaris L. seed mucilage as a new excipient for sustained delivery of Vildagliptin. Copolymeric carrier of A. vulgaris seed mucilage-co-AAm was devised by using acrylamide (AAm) as a monomer, methylene-bis-acrylamide (MBA) as a crosslinker, and potassium persulfate (KPS) as an initiator through free radical polymerization. Different formulations of A. vulgaris-co-AAm were devised by varying contents of polymer, monomer, crosslinking agent, initiator, and reaction temperature. Copolymeric structures were characterized through XRD analysis, Fourier transform infrared (FTIR) spectroscopy, TGA and DSC analysis, and scanning electron microscopy. Porosity, gel fraction, and Vildagliptin loading capacity of copolymers were also established. Swelling and in vitro drug release studies were conducted. XRD evaluation showed the alteration of the crystalline structure of Vildagliptin into an amorphous form. FTIR analysis confirmed the successful grafting of AAm to A. vulgaris seed mucilage backbone. Porosity was increased with increasing polymer concentration and reaction temperature while it was decreased with an increasing amount of AAm, MBA, and KPS. Gel content was decreased with increasing polymer concentration and reaction temperature while it was increased with an increasing amount of AAm, MBA, and KPS. Acute oral toxicity of copolymeric network was done in animal models to evaluate the safety. Copolymers showed the same swelling behavior at all pH 1.2, 4.5, 6.8, and 7.4. Vildagliptin release from copolymer showed a cumulative trend by increasing polymer content and reaction temperature, while a declining trend was observed with increasing contents of monomer, crosslinking agent, and initiator. Sustained release of Vildagliptin was observed from copolymers and release followed the Korsmeyer-Peppas model. From the acute oral toxicity studies, it is evident that newly synthesized copolymeric carriers are potentially safe for eyes, skin, and vital organs.