Improved Release of a Drug with Poor Water Solubility by Using Electrospun Water-Soluble Polymers as Carriers

Abstract

In an attempt to improve the solubility of valsartan, a BCS II drug, fibers containing the drug were prepared from three water-soluble polymers, hydroxypropyl-methyl-cellulose (HPMC), polyvinyl-pyrrolidone (PVP), and polyvinyl-alcohol (PVA). Fiber spinning technology was optimized for each polymer separately. The polymers contained 20 wt% of the active component. The drug was homogenously distributed within the fibers in the amorphous form. The presence of the drug interfered with the spinning process only slightly, the diameters of the fibers were in the same range as without the drug for the HPMC and the PVA fibers, while it doubled in PVP. The incorporation of the drug into the fibers increased its solubility in all cases compared to that of the neat drug. The solubility of the drug itself depends very much on pH and this sensitivity remained the same in the HPMC and PVP fibers; the release of the drug is dominated by the dissolution behavior of valsartan itself. On the other hand, solubility and the rate of release were practically independent of pH in the PVA fibers. The different behavior is explained by the rate of the dissolution of the respective polymer, which is larger for HPMC and PVP, and smaller for PVA than the dissolution rate of the drug. The larger extent of release compared to neat valsartan can be explained by the lack of crystallinity of the drug, its better dispersion, and the larger surface area of the fibers. Considering all facts, the preparation of electrospun devices from valsartan and water-soluble polymers is beneficial, and the use of PVA is more advantageous than that of the other two polymers.

Recent Advances in Amorphous Solid Dispersions: Preformulation, Formulation Strategies, Technological Advancements and Characterization

“…Consequently, the existing technologies prevailed to spray-dryers and hot melt extruders, making them viable for ASD commercial manufacturing [ 10 ]. Additionally, the developments in the manufacturing arena helped to identify the impact of process variables over critical quality attributes (CQA’s) of ASDs and also led to the development of novel manufacturing processes like Kinetisol ® dispersing (KSD) [ 29 ], selective laser sintering (SLS) [ 30 ] and fused deposition modeling (FDM) 3D printing [ 31 ], electronanospinning, and others [ 32 ]. It is worth mentioning the recent advancements in preformulation space, which aimed to understand the interactions between the formulation components at a molecular level [ 33 ]; this was possible through analytical techniques and molecular simulation predictions using in-silico tools [ 34 ].…”

Levocetirizine-Loaded Electrospun Fibers from Water-Soluble Polymers: Encapsulation and Drug Release

“…PVA is a crystalline polymer, while the other two are amorphous. The physical structure of the polymers also influences their dissolution, and in a previous study, PVA was shown to dissolve slower than the other two polymers, thus determining the rate of release and its dependence on pH [ 43 ]. Although Jahangir et al [ 41 ] found that strong interactions do not form between Levo and the three polymers used in this study, based on the chemical structure of the components, some doubts might be raised about that claim.…”

“…Drugs are often added to formulations with a complete disregard for interactions and solubility. Similarly, the solubility of an active component in a solvent or a solvent mixture might be limited, just as in the case of BCS II drugs [ 34 , 43 ].…”

“…Accordingly, the technology must be optimized in order to obtain fibers of good quality. Our optimization started from the parameter set determined in a previous study [ 43 ], but it had to be modified somewhat because of the use of a new apparatus and the effect of the different drugs on the technology. The most important parameters optimized were the polymer concentration of the solution as well as the voltage, feeding rate and collector distance.…”

Bioactive Materials Based on Hydroxypropyl Methylcellulose and Silver Nanoparticles: Structural-Morphological Characterization and Antimicrobial Testing

“…To obtain a better dispersion and fixation/catching of AgNPs in the HPMC matrix, the poly(N-vinylpyrrolidone) (PVP) has attracted considerable attention because it acts not only as a stabilizing agent but also has an impact on the control of the reduction rate of the silver ions and the aggregation process of silver atoms [ 41 , 42 ]. It is known to have excellent chemical and physical properties that make it a good material as additive or coating to other materials, including HPMC [ 43 , 44 , 45 , 46 ]. Thus, the utilization of PVP as a stabilizer facilitates the binding of the metal, leading to the improvement of the biomedical properties.…”