Formulation of Convenient, Easily Scalable, and Efficient Granisetron HCl Intranasal Droppable Gels

Abstract

Deacetylated gellan gum and two sodium alginate polymer types were used each at three concentrations in the suitable range for their sol-gel transition. The prepared nine droppable gels were evaluated in vitro, ex vivo through sheep nasal mucosa, as well as in vivo in comparison to drug solution given intravenously and orally at the same dose. The prepared formulas gelled instantaneously in simulated nasal fluid and the obtained gels sustained their shear thinning and thixotropic behavior up to 48 h. Polymer type and concentration had significant effects on the apparent viscosities and the in vitro release profile of granisetron from the prepared gels. The drug release data best fitted a modified Higuchi equation with initial burst and followed Fickian diffusion mechanism. A 0.5% gellan-gum-based formula sustained the in vitro drug release up to 3 h and enhanced the drug permeation without need for an enhancer. The histopatholgical study revealed the safety of the tested formula. Intranasal delivery recorded double the drug bioavailabilty in comparison to the oral route. It had an absolute bioavailability of 0.6539 and the maximum plasma drug concentration reached after 1.5 h. The developed formula could be promising for the management of chemotherapy-induced nausea and vomiting regarding its improved bioavailability, patient acceptability, and ease of production.

Novel reverse electrodialysis-driven iontophoretic system for topical and transdermal delivery of poorly permeable therapeutic agents

“…In vitro skin permeation parameters were calculated by plotting the cumulative amount of drug permeated through the skin per unit area versus time. The slope of the linear portion in the plot was calculated as the flux (μg/h/cm 2 ) (Ibrahim et al., 2015 ; Salah et al., 2017 ). The lag time was calculated by extrapolating the linear portion to the X-axis of the plot (Rao et al., 2015 ; Salah et al., 2017 ).…”

Newest Drugs for Chronic Unexplained Nausea and Vomiting

“…Responses were similar in diabetic versus idiopathic gastroparesis and among those with delayed versus no documented delay in gastric emptying. Recently, an intranasal granisetron product was developed which may provide another means of drug delivery (22). …”

Development and Evaluation of a Novel Intranasal Spray for the Delivery of Amantadine

“…To achieve this goal, the use of intelligent polymer based systems have now become more commonplace in this field and particularly the use of responsive systems which may respond to the nasal cavity temperature [13][14][15][16][17][18][19][20][21][22] or pH [23][24][25][26][27] have increased amongst researchers. Furthermore, the use of mucoadhesive polymers 4,[27][28][29][30][31][32][33] to enhance the adhesion of the formulations onto the nasal mucosa has further demonstrated the ability to prolong contact time with the mucosa and hence increase bioavailability 10,15,18,23,[34][35][36] .…”