Fabrication of Cationic Exchange Polystyrene Nanofibers for Drug Delivery

Purpose: To prepare polystyrene nanofiber ion exchangers (PSNIE) with surface cation exchange functionality using a new method based on electrospinning and also to optimize crosslinking and sulfonation reactions to obtain PSNIE with maximum ion exchange capacity (IEC).Method: The nanofibers were prepared from 15% w/v polystyrene solution in dimethylacetamide (DMAc) containing 0.025 %w/v tetrabutylammonium bromide (TBAB) using electrospinning technique, followed by crosslinking with sulfuric acid/formaldehyde in a ratio ranging from 100/0 to 50/50 v/v and sulfonation in sulfuric acid. Degree of crosslinking was determined as the amount of fibers that remained in dichloromethane. The morphology and diameter of the fibers were evaluated by scanning electron microscopy (SEM) while IEC of PSNIE was performed by salt splitting titration.Results: PSNIE crosslinked with a sulfuric acid/formaldehyde ratio of 90/10 with 0.1 %w/v silver sulfate for 10 min at 70°C and sulfonated in 98 % sulfuric acid with 0.2 %w/v silver sulfate as the catalyst at 100°C for 30 min showed a maximum IEC of 3.21 meq/g-dry-PSNIE. Increase in  sulfonation temperature caused the IEC of PSNIE to increase due to faster sulfonation. It was observed that the higher the temperature the faster the rate of sulfonation reaction. The diameter of the fibers after sulfonation was 404 ± 42 nm.Conclusion: These results indicate that PSNIE can be successfully prepared by electrospinning. Furthermore, cationic drug can be loaded onto the novel PSNIE for controlled release delivery.Keywords: Polystyrene, Ion exchange capacity, Nanofibers, Ion exchangers, Crosslinking, Sulfonation

Evaluation of some anionic exchange resins as potential tablet disintegrants

Purpose: To determine the potential of some anionic exchange resins as tablet disintegrants.Methods: Dowex1® x2, x4 and x8 resins (crosslinked copolymers of styrene and divinylbenzene with quaternary methyl amine functionality) were evaluated as disintegrant for dibasic calcium phosphate dihydrate tablets. The best resin providing the fastest disintegration and highest hardness of obtained tablets was selected for further investigation. The effect of resin concentration and compression force on the properties of tablets using the selected resin was investigated. In addition, the disintegrant efficacy of the selected resin in the tablet formulations containing either a basic drug, e.g., dextromethorphan hydrobromide (DMP), or an acidic drug, e.g., diclofenac sodium (DCN), was determined in comparison with sodium starch glycolate (SSG).Results: Dowex1®x2 resin exhibited the fastest disintegration (6.0 s) and the highest hardness (103.6 N) of obtained tablets. These disintegrating and tablet properties depended upon the resin concentration and compression force. For DMP, the resin provided faster disintegration and drug release (8.0 s and 100.4 % at 10 min) as compared with SSG (16.2 s and 98.9 % at 30 min). In contrast, the resin caused the depleted release of DCN (61.6 % at 120 min) in spite of providing the faster tablet disintegration (10.0 s) than SSG (15.5 s) due to the ionic binding of the drug and resin.Conclusion: The Dowex1®x2 resin was shown to be a potential disintegrant for the tablets of basic drugs.Keywords: Anionic exchange resin, Disintegrant, Dextromethorphan hydrobromide, Diclofenac sodium, Calcium phosphat

Effect of polysulfonate resins and direct compression fillers on multiple-unit sustained-release dextromethorphan resinate tablets

The purpose of this work was to investigate the effect of different polysulfonate resins and direct compression fillers on physical properties of multiple-unit sustained-release dextromethorphan (DMP) tablets. DMP resinates were formed by a complexation of DMP and strong cation exchange resins, Dowex 50 W and Amberlite IRP69. The tablets consisted of the DMP resinates and direct compression fillers, such as microcrystalline cellulose (MCC), dicalcium phosphate dihydrate (DCP), and spray-dried rice starch (SDRS). Physical properties of tablets, such as hardness, disintegration time, and in vitro release, were investigated. A good performance of the tablets was obtained when MCC or SDRS was used. The use of rod-like and plate-like particles of Amberlite IRP69 caused a statistical decrease in tablet hardness, whereas good tablet hardness was obtained when spherical particle of Dowex 50 W was used. The plastic deformation of the fillers, such as MCC and SDRS, caused a little change in the release of DMP. A higher release rate constant was found in the tablets containing DCP and Dowex 50 W, indicating the fracture of the resinates under compression, which was attributable to the fragmentation of DCP. However, the release of DMP from the tablets using Amberlite IRP69 was not significantly changed because of the higher degree of cross-linking of the resinates, which exhibited more resistance to deformation under compression. In conclusion, the properties of polysulfonate resin, such as particle shape and degree of cross-linking, and the deformation under compaction of fillers affect the physical properties and the drug release of the resinate tablets