Development and Characterization of Eudragit®-Based Electrospun Nanofibrous Mats and Their Formulation into Nanofiber Tablets for the Modified Release of Furosemide

Abstract

Furosemide, a chloride channel blocker ordinarily used as a high-ceiling or loop diuretic, is practically insoluble in water and dilute acids. Due to its acidic nature, furosemide is mostly absorbed in the stomach and in the upper small intestine. Efforts have focused on the development of sustained release systems of furosemide in order to improve the effectiveness of the drug, which exhibits poor aqueous solubility and poor permeability. Recently, electrospun nanofibrous drug delivery systems have emerged as promising alternative solid-dosage forms due to their advantages of high porosity, high surface to volume ratio, and high drug-loading efficacy. Herein, a number of nanofibrous mats composed of different types of Eudragit® polymers in various concentrations and combinations loaded with furosemide were designed, successfully electrospun, and characterized using SEM, FTIR, DSC, and TGA analyses. The nanofibrous nonwovens were formulated in nanofiber tablets and the release profile of furosemide from them was evaluated at pH 1.2 and 6.8 and compared to that of physical mixture matrix tablets of analogous composition as well as to that of a commercial formulation. It was found that the release of furosemide was compatible with the gastroretentive and slower intestinal release requirements with a well-defined absorption window, while some nanofiber formulations could act as furosemide carriers in emergency situations where a relatively fast onset of its action is required, as in the case of critically ill post-traumatic patients.

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“…50 All other ingredients including lyophilized GDD, HP-β-CyD and ES-100 show earlier change around 300 °C. [51][52][53][54] These results indicated that coaxial NFs effectively enhanced the thermal stability of encapsulated GDD.…”

Probing the Release of Bupropion and Naltrexone Hydrochloride Salts from Biopolymeric Matrices of Diverse Chemical Structures

“…The experiments were performed in two different aqueous media: for the first 2 h, 450 mL of 0.2 M HCl solution (pH 1.2) was used to simulate the stomach pH, and to that 450 mL of 0.14 M K 2 HPO 4 solution (pH 9) was then added, to have the required composition of the next phase, which simulates the enteric pH (pH 6.8, final volume 900 mL). [ 36 ].…”

Electrospinning for healthcare: recent advancements

“…This concept has been proven by Shen et al for the non-steroidal anti-inflammatory (NSAID) drug ketoprofen 28 and by Illangakoon and co-workers for the antispasmodic API mebeverine hydrochloride, 29 among other studies. 30,31 pH-sensitivity can also be imparted through the inclusion of a third component into the recipe: the incorporation of sodium bicarbonate has been shown to accelerate drug release in acidic conditions, giving fibres which could be used to target API release to the tumour microenvironment. 32 Thermo-responsive polymers can be included in the ES process, leading to fibres which can respond to temperature.…”