Abstract

Abstract Sildenafil citrate (SC) has proved to be an effective and inexpensive drug for the treatment of pulmonary arterial hypertension (PAH). This study aims to synthesize electrospun, submicron fiber scaffolds of poly(vinyl alcohol) (PVA) and poly(vinyl pyrrolidone) (PVP) loaded with SC for fast drug dissolution and its potential use in the treatment of PAH. These fiber scaffolds were prepared through the electrospinning technique. The chemical composition of the nanofibers was analyzed by Fourier transform infrared spectroscopy. Thermal stability was studied by thermogravimetric analysis and polymeric transitions by differential scattering calorimetry. Surface analysis of the nanofibers was studied by field emission scanning electron microscopy. The wetting and dissolution time of the scaffolds and drug release rate were studied as well. The drug-loaded PVP fibers showed better quality regarding size and homogeneity compared to drug-loaded PVA fibers. These fibers encapsulated approximately 2.5 mg/cm2 of the drug and achieved immediate controlled released rate, which is encouraging for further studies leading to an alternative treatment of PAH in children.

Highlights

  • Pulmonary arterial hypertension (PAH) is a common complication of congenital heart disease (CHD)

  • Dissolution of the fiber scaffolds was tested according to Li et al [11], where samples were submerged in a flask with 250 mL of distilled water at 37°C and measured as a function of time

  • A distinctive peak of the O–H stretch vibration in poly(vinyl alcohol) (PVA) can be observed at 3,400–3,200 cm−1; around 2,900 cm−1, a signal characteristic to alkyl C–H stretching is visible, and between 1,150 and 1,050 cm−1 a signal that corresponds to the C–O link can be observed

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Summary

Introduction

Pulmonary arterial hypertension (PAH) is a common complication of congenital heart disease (CHD) This condition is a progressive disorder characterized by high blood pressure in the pulmonary artery [1]. CHD is the most frequent birth defect, with a prevalence ranging from 6 to 8 per 1,000 live births This disease has high mortality and morbidity rates [2]. Several therapies are used to treat PAH; sildenafil citrate (SC) is one of the most cost-efficient treatments [3]. This drug inhibits phosphodiesterase 5 (PDE5) by blocking its catalytic site, which prevents the degradation of the cyclic guanosine monophosphate molecule, promoting vascular smooth muscle relaxation and increased blood flow, relieving the symptoms of PAH. SC was approved for PAH treatment in children by the Food and Drug Administration (FDA) and the European Medicines Agency in 2005 [4]

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