Design and physico-mechanical evaluation of fast-dissolving valsartan polymeric drug delivery system by electrospinning method

Objective(s): Chronic hypertension is a pervasive morbidity and the leading risk factor for cardiovascular diseases. Valsartan, as an antihypertensive drug, has low solubility and bioavailability. The application of orodispersible films of valsartan is suggested to improve its bioavailability. With this dosage form, the drug dissolves rapidly in saliva and is absorbed readily without the need for water. Materials and Methods: For this purpose, valsartan with polyvinylpyrrolidone (PVPK۹۰) polymer were exposed to the electrospinning technique to construct orodispersible nanofilms. The optimum obtained nanofiber, selected by Design-Expert software, was evaluated in terms of mechanical strength for evaluation of the flexibility and fragility of the nanofibers. The drug content, wettability, and disintegration tests, as well as the release assessment of the nanofibers, were performed followed by DSC, FTIR, and XRD assays.Results: The uniform nanofibers’ diameter increased with the increase of the polymer concentration. The tensile test verified a stress reduction at the yield point as the polymer concentration increased. Then, the ۴۹۲ nm nanofiber with above ۹۰% drug encapsulation, containing ۸% polymer and ۱۸% valsartan made below ۹ kV, was selected. The wetting time was less than ۳۰ sec and over ۹۰% of the drug was released in less than ۲ min. The XRD and DSC studies also confirmed higher valsartan solubility due to the construction alternations in nanofibers. The FTIR examination indicated the chemical bonding between the drug and the polymer.Conclusion: The selected nanofibers of valsartan present the essential drug feature and acceptable drug release for further investigations.

Keywords:

Hypertension , Nanofiber , Polymers , Polyvinylpyrrolidone , Valsartan