Vardenafil Oral Dispersible Films (ODFs) with Advanced Dissolution, Palatability, and Bioavailability

Abstract

Oral, quick response, and on demand, also known as a spontaneous oral treatment for erectile dysfunction, is highly needed by both patients and physicians. Vardenafil is selective (fewer side effects) and more effective in difficult-to-treat conditions than sildenafil. This study aims at fostering the dual objectives of using biomolecules such as artificial sweetening agents to solubilize and mask the bitterness of vardenafil loaded on biodegradable polymeric materials (PVA, MC, SA, and PVP K30) to fabricate oral, fast-dissolving films (vardenafil ODFs) in the mouth without the need for water to ingest the dosage form. Furthermore, coprecipitated-dispersed mixtures of vardenafil and three sweeteners (sorbitol, acesulfame K, and sucralose) were prepared and characterized using FTIR, DSC, and solubility studies. Moreover, eight different vardenafil ODFs were prepared using the solvent-casting method. Modified gustatory sensation test, in vitro disintegration, and release studies were performed. In addition, the optimized ODF (F8) was compared with the commercial film-coated tablets pharmacokinetically (relative bioavailability, onset, and duration of actions were estimated). The results indicated that the three sweetening agents had comparable solubilizing capacity. However, both sucralose- and acesulfame K-based ODFs have a more enhanced sweet and palatable taste than sorbitol-sweetened ODF. The SA- and PVP K30-based ODFs showed significantly faster disintegration times and release rates than MC. In conclusion, PVA has good film-forming properties, but a higher ratio of PVA adversely affected the disintegration and release characteristics. The % relative bioavailability for ODF was 126.5%, with a superior absorption rate constant (Ka) of 1.2-fold. The Cmax and estimated Tmax were compared to conventional film-coated tablets.

Vardenafil-Loaded Bilosomal Mucoadhesive Sponge for Buccal Delivery: Optimization, Characterization, and In Vivo Evaluation

“…Thermal properties of VDF, SPC, CHOL, SDC, and optimized VDF-loaded bilosomal formulation were recorded utilizing differential scanning calorimeter ( Figure 5 ). The pure vardenafil (VDF) thermogram exhibited a broad endothermic peak from 50–100 °C, corresponding to water loss, and another characteristic endothermic peak at 118 °C, corresponding to VDF melting [ 34 ]. The SPC thermogram showed an endothermic peak at 167 °C.…”

Orodispersible Films—Current State of the Art, Limitations, Advances and Future Perspectives

“…Another critical issue is the bitter taste of many APIs since the dosage form is in direct contact with the oral mucosa. The taste masking effect of APIs may be achieved through a variety of methods and technologies, such as the simple addition of flavour and sweetener combinations [ 72 , 73 ] or more complex systems such as drug complexation with ion exchange resins [ 74 ] or cyclodextrins [ 75 ].…”

Rizatriptan-Loaded Oral Fast Dissolving Films: Design and Characterizations

“…The components PUL (X 1 ), MTX (X 2 ), and PG (X 3 ) had a substantial effect on the response TS (Y 3 ). Based on the findings of the ANOVA, a statistical model was developed to outline a workable relationship between the dependent and independent variables.The response Y 3 (TS, MPa) model produced a final equation regarding coded factors and responses, as shown in Equation (9).…”

“…In recent decades, many studies have demonstrated that oral dispersible films (ODFs) as drug delivery systems (DDS) can provide a rapid onset of therapeutic effects and maximize drug bioavailability. ODFs are conventionally made by solvent casting method (SCM) or hot-melt extrusion (HME) using hydrophilic polymers [9]. Europe has already commercialized RIZAPORT ® ODFs prepared by SCM.…”

“…ODFs acceptability as a drug carrier is further supported by its rapid onset of action, patient adherence, portability, and avoidance of hepatic metabolism [10]. ODFs are flexible, transportable, and effortless to ingest, lowering the danger of choking compared to orally disintegrating tablets (ODTs) [9]. However, ODFs possess significant restrictions owing to compositional variations that might lead to poor mechanical qualities, such as exterior blistering, substrate detaching issues, irregular creases, or fractures.…”