Low dissolution rates of poorly soluble drugs are the factor afflicting their bioavailability. The aim of this study is to prepare a centrifugal spinning-based formulation of a poorly soluble drug, oxcarbazepine, for the improvement of dissolution rate and hence quick action. Sucrose-based microfibers of oxcarbazepine were prepared by a centrifugal melt spinning technique using a cotton candy machine. The prepared microfibers were characterized using Scanning electron microscopy (SEM), PXRD, Differential Scanning Calorimetry (DSC) and FTIR. The optimum formulation was molded into tablets and tested for in vitro drug release and in vivo pharmacokinetic studies using rabbits as test animals. The results indicated that the centrifugal spinning rapidly produced dissolving microfibers (diameter are <10 µm and dissolve in few seconds). In these fibers, ~20% oxcarbazepine was loaded, and both the yield and drug loading efficiency were improved by incorporating polyvinypyrolidine (PVP) in the formulations. The dissolution studies have revealed >90% of the drug was dissolved in just 2 min as compared with drug alone that shows only 15% dissolution at this time interval. XRD and DSC analyses have shown the amorphous state of the drug in the fibers while the FTIR analysis showed chemical stability of oxcarbazepine in the fibers. In vivo studies have revealed a 2 h reduction in tmax of drug in the rabbits treated with microfibers as compared with controlled group which was given pure oxcarbazepine. The study concludes the potential of the centrifugal spinning technique for the production of drug loaded fibers that can significantly enhance the dissolution rates of poorly soluble drugs and thus produce formulations for quick action of such drugs. Furthermore, the sucrose-based formulation can enhance the palatability with the intention of attracting pediatric patients.
Fused deposition modeling (FDM) based threedimensional printing (3DP) is amongst a recently used methods intended for the preparation of customized medicine (1). Dose customization involves; tailoring the medical treatment based on the individual characteristics, needs and preferences of each patient (2). This approach can improve the safety profile of drugs by lowering the risk of overdosing (particularly for drugs prescribed at lower doses), hence adverse reactions (3). FDM is an additive manufacturing technique (4) which constructs a 3D object directly from computer-aided design (CAD) data, utilizing a thermoplastic material (such as PVA and PLA, etc.) in the form of filament extruded through printing head of 3D printer in a layer by layer fashion (5). The classical approach for drug loading in commercially available PVA or PLA filaments is the impregnation or solvent diffusion (6). The method involves soaking the filament in the saturated alcoholic solution of a drug at room temperature (7). The preparations reported so far have shown a meager drug loading i.e. (< 2% w/w) by this method. In one such study, fluorescein sodium was loaded in PVA filament. Although the printed tablets were mechanically strong with low friability, they exhibited a drug content of <1% (6). Similarly, 3D printing of 4-aminosalicylic acid (4-ASA) and 5-aminosalicylic acid (5-ASA) tablets also revealed almost similar extent of drug loading (8). The impregnation method has also been tried for 3D printing of pred
Aim: The study explores the material properties of two different grades of prefabricated polyvinyl alcohol filaments in terms of drug-loading capacity and printability. Materials & methods: Loratadine was loaded into these filaments or their scaffolds by impregnation and they were evaluated for physical and mechanical properties, drug content and printability. Results: The Type I (Pc) filament, being more flexible, showed approximately 100-times higher drug loading compared with the Type II (Pm) filament. However, the diameter of the Pc filament increased by 35% with decreased mechanical strength on soaking in drug solution, which made it unsuitable for 3D printing. On the other hand, the Pm filament was tougher and showed a meager amount of drug loading (<1 mg per 0.5 g) but remained mechanically stronger with good printability. Conclusion: Therapeutic doses of low-dose drug can be loaded efficiently in printed scaffolds of Pc filament.
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