Abstract
The formation of nanoscale fibers from pH-sensitive polymers is a route which has been widely explored for targeted drug delivery. In particular, the Eudragit L100 and S100 families of polymers have received significant attention for this purpose. However, while in some cases it is shown that making drug-loaded Eudragit polymers effectively prevents drug release in low-pH media where the polymer is insoluble, this is not always the case, and other studies have reported significant amounts of drug release at acidic pHs. In this study, we sought to gain insight into the factors influencing the release of active ingredients from Eudragit S100 (ES100) fibers. A family of materials was prepared loaded with the model active ingredients (AIs) benzoic acid, 1-naphthoic acid, 1-naphthylamine, and 9-anthracene carboxylic acid. Analogous systems were prepared with an AI-loaded core and an ES100 sheath. The resultant fibers were smooth and cylindrical in the majority of cases, and X-ray diffraction and differential scanning calorimetry showed them to comprise amorphous solid dispersions. When AI release from the monolithic fibers was probed, it was found that there was significant release at pH 1 in all cases except with 9-anthracene carboxylic acid. Analysis of the results indicated that both the molecular weight of the AI and its acidity/basicity are important in controlling release, with lower molecular weight AIs and basic species released more quickly. The same release trends are seen with the core/shell fibers, but AI release at pH 1 is attenuated. The most significant change between the monolithic and core/shell systems was observed in the case of 1-naphthylamine. Mathematical equations were devised to connect molecular properties and AI release under acidic conditions.
Highlights
Electrospinning is a technique which has attracted great attention in the pharmaceutical technology field [1,2]
We show in this work that both the molecular weight and the acidity/basicity of an active ingredients (AIs) are crucial in determining the extent to which release occurs from Eudragit S100 fibers in acidic media
We report new insights into the factors governing the release of active ingredients (AIs) from electrospun Eudragit S100 (ES100) fibers
Summary
Electrospinning is a technique which has attracted great attention in the pharmaceutical technology field [1,2]. It most commonly involves the preparation of a polymer solution in a volatile solvent. This is loaded into a syringe and is slowly ejected through a narrow bore needle (the spinneret). In the simplest embodiment of the experiment, a single liquid is processed, but more advanced derivatives including coaxial electrospinning (which uses two needles nested concentrically one inside the other to process two liquids) and triaxial spinning (three needles, three solutions) have been reported. The use of coaxial spinnerets results in core/shell structures, and triaxial spinnerets give three-compartment architectures
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