Synthesis of novel superdisintegrants for pharmaceutical tableting based on functionalized nanocellulose hydrogels

• Published in: International journal of biological macromolecules 2021-01, Vol.167, p.667-675
• Main Authors: Sheikhy, Shabnam, Safekordi, Ali Akbar, Ghorbani, Marjan, Adibkia, Khosro, Hamishehkar, Hamed
• Format: Article
• Language: English
• Subjects: Cellulose - analogs & derivatives; Cellulose - chemical synthesis; Cellulose - chemistry; Cellulose - ultrastructure; Chemistry; Chemistry Techniques, Synthetic; Chemistry, Pharmaceutical; Cross-Linking Reagents; Drug Carriers; Drug Delivery Systems; Drug Liberation; Hydrogel; Hydrogels - chemistry; Kinetics; Nanocrystalline cellulose; Nanoparticle; Nanoparticles - chemistry; Nanoparticles - ultrastructure; Pharmaceutical Preparations - chemistry; Solubility; Spectroscopy, Fourier Transform Infrared; Static Electricity; Superdisintegrant; Tablet; Tablets - chemistry
• ISSN: 0141-8130; 1879-0003
• DOI: 10.1016/j.ijbiomac.2020.11.173

Superdisintegrants have an important function in Fast dissolving tablets (FDT). It's believed that an increase in surface to the mass (size reduction) can enhance their performance. Due to the obligation of pharmaceutical excipients being in GRAS (generally recognized as safe) list, we've devoted our research to modify one of the routinely used and important natural polymer, cellulose, as superdisintegrant. Nanocrystalline cellulose (NCC) was extracted from microcrystalline cellulose (MCC) via the sulfuric acid hydrolysis process. NCC derivatives have been synthesized by Itaconic acid/Hydroxyethyl methacrylate (IA/HEMA) via maleic anhydride (MA) to acquire unique swellability properties in to achieve superabsorbent cellulose-based nano hydrogel with the cross-linking system. The disintegration performance of prepared tablets was compared with tablets composed of sodium starch glycolate (SSG) and MCC as positive and negative controls. The results show that the disintegration time of tablets formulated with synthesized modified NCC (m-NCC) decreased dramatically compared to other disintegrants. The dissolution analysis showed suitable condition for complete drug release in a shorter time. The in vitro cytotoxic experiments proved the biocompatibility of newly synthesized superdisintegrant. The dissolution Analysis findings suggest that our developed novel superdisintegrant paves the way for the formulation of fast dissolving tablets containing rapidly acting medicines such as zolpidem. •The following outcomes resulted from study:•Synthesis of nanocrystalline cellulose (NCC) from microcrystalline cellulose (MCC)•Modification of NCC as a novel superdisintegrant via cross-linking process•Faster disintegration of tablet made of NCC than those prepared by traditional one•Faster and complete drug release form tableting formulated by NCC