Chitosan nanoparticles loaded with insulin (IN-CS-NPs) were prepared using ionic gelation method using sodium tripolyphophate as a crosslinker. Later the nanoparticles (NPs) were dispersed in buccal films. The physicochemical properties and the morphology of the nanoparticles were characterized. The stability and release of insulin from the NPs were investigated. Buccal films were prepared separately and their properties such as the weight, thickness, pH, and mucoadhesiveness were investigated. The best film was used to disperse IN-CS-NPs and the loaded film was characterized. The nanoparticles size, polydispersity index, zeta potential, entrapment efficacy, and the loading capacity were 325.07 ± 1.32 nm, 0.38 ± 0.03 and 8.41 ± 0.80 mV, and 73.27 and 18.03%, respectively. The weight and thickness of the loaded film with IN-CS-NPs were 23.0 ± 3.0 mg and 0.32 ± 0.04 mm, respectively and the mucoadhesive force was 2.3 ± 0.2 N. The drug was stable in the NPs and in the films for three months, and its release was controlled by the film and the nanoparticles. Finally, the films loaded with IN-CS-NPs were studied in vivo and were compared to the commercially available insulin. The films prepared in this work were found to decrease glucose level significantly in diabetic rats.
Keywords: Chitosan; TPP; buccal film; insulin; ionic gelation; nanoparticles.