<p>Tadalafil-Loaded Limonene-Based Orodispersible Tablets: Formulation, in vitro Characterization and in vivo Appraisal of Gastroprotective Activity</p>

Abstract

Background Gastric ulcer is a prevalent disease with various etiologies, including non-steroidal anti-inflammatory drugs and alcohol consumption. This study aimed to explore the dual gastric protection effect of tadalafil and limonene as a self-nanoemulsifying system (SNES)-based orodispersible tablets. Methods Tadalafil-loaded limonene-based SNES was prepared, and the optimum formula was characterized in terms of particle size (PS), polydispersity index (PDI), and zeta potential (ZP) then loaded on various porous carriers to formulate lyophilized orodispersible tablets (ODTs). The ODTs were evaluated via determining hardness, friability, content uniformity, wetting, and disintegration time. The selected ODT was examined for its gastric ulcer protective effect against alcohol-induced ulcers in rat model. Ulcer score and ulcer index were computed for rats stomachs that were inspected macroscopically and histopathologically. Results The prepared SNES had droplet size of 104 nm, polydispersity index of 0.2, and zeta potential of −15.4 mV. From the different ODTs formulated, the formula with superior wetting time: 23.67 s, outstanding disintegration time: 28 s, accepted hardness value: 3.11 kg/cm 2 and friability: 0.6% was designated. A significant gastroprotective effect of the unloaded and tadalafil-loaded ODTs was recognized compared to the omeprazole pre-treated group. Moreover, the histopathological analysis displayed very mild inflammation in the limonene-based ODTs group and intact structure in the tadalafil-loaded pre-treated animals. Conclusion Limonene gastroprotective effect functioned along with tadalafil in the form of SNES-incorporated ODTs could serve as a promising revenue for better efficacy in gastric ulcer prevention.

Scalable flibanserin nanocrystal-based novel sublingual platform for female hypoactive sexual desire disorder: engineering, optimization adopting the desirability function approach and in vivo pharmacokinetic study

“…Wetting time is an important test for sublingual orodispersible tablets as it simulates the condition under the tongue with small saliva volume ranging from 1 to 5 mL (Rawas-Qalaji et al, 2006 ). It also gives an indication about the porosity of the tablets, and it was found to be correlated with the disintegration time (Mehanna et al, 2020 ). The wetting time of FLB-NCT4 was found to be 36 s, which is quite matching with the disintegration time result.…”

“…A tablet was carefully placed on the surface of the tissue paper and the time required for the dye to reach the upper surface of the tablet was recorded as the wetting time. The tablet was weighed again and percentage weight gain was determined (Mehanna et al, 2020 ).…”

Chemical composition, antidiabetic, anti-inflammatory, antioxidant and toxicityactivities, of the essential oil of <em>Fortunella margarita</em> peels

“…22 In another study on the characteristic odorous components in the essential oil from Fortunella japonica peel, limonene was the highest component, amounting to 93.73%. 23 Limonene is used to treat gastric disorders 24,25 and has an antiproliferative effect on cancer cells. 26 Antimicrobial, anti-inflammatory, sedative, and antilithic activities of limonene have also been reported.…”

Development and Evaluation of Cannabidiol Orodispersible Tablets Using a 23-Factorial Design

“…An advantage of this pharmaceutical formulation is related to the fact that no water intake is needed during administration [ 4 , 5 , 6 ]. In the past, the targeted populations for the OD formulations were pediatric and geriatric patients with Parkinson’s disease, schizophrenia, or gastroesophageal reflux, but recently, ODTs are used for a large category of patients due to their numerous advantages: do not necessitate chewing; disintegration takes place directly in the mouth; pleasant taste; increased stability compared to solutions, emulsions, and suspensions; can be manufactured as controlled released pharmaceutical formulations; high amounts of Active Pharmaceutical Ingredient (API) can be used; ability to confer the advantages of a liquid formulation in a solid form; the therapeutic effect occurs fast [ 7 , 8 , 9 , 10 , 11 ]. …”

“…10) of 3 min [1][2][3]. An advantage of this pharmaceutical formulation the therapeutic effect occurs fast [7][8][9][10][11].…”