Development of Mucoadhesive Chitosan-Iodoacetamide Buccal Tablets for Local Delivery of Dextromethorphan

Yin Yin Myat, M. Vollrath, Nitjawan Sahatspan, T. Ngawhirunpat, Chaiyakarn Pornpitchanarong, Prasopchai Patrojanasophon
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Abstract

Abstract This study aimed to synthesize a chitosan (CHI) derivative, chitosan-iodoacetamide (CHI-IA), with enhanced mucoadhesive properties and develop buccal mucoadhesive tablets of CHI-IA for local delivery of dextromethorphan (DXT). Mucoadhesive CHI-IA was synthesized by a chemical reaction between CHI and iodoacetic acid (IA) in different weight ratios. The synthesized CHI-IA was characterized by Fourier-transformed infrared spectroscopy (FT-IR) and nuclear magnetic resonance spectroscopy (NMR) to confirm the chemical structure and assure successful synthesis. DXT was selected as the model drug to be incorporated into the matrix tablet to develop mucoadhesive buccal cough relief tablets. The mucoadhesive strength of the CHI-IA tablets was determined by a texture analyzer. Moreover, the drug content and the release characteristics of DXT from the mucoadhesive tablets were evaluated. The FT-IR and NMR spectra of CHI-IA indicated the conjugation of IA on the structure of CHI. The CHI-IA tablets exhibited a 4-time increase in mucoadhesion force compared with that of unmodified CHI. Moreover, a gradual release of DXT from the tablets was observed, and the release kinetics best fit with the Higuchi model (R2 = 0.9912). Therefore, the CHI-IA could be applied as the mucoadhesive carrier system for drug delivery. Keywords: Chitosan, Iodoacetic acid, Mucoadhesive, Buccal tablets, Dextromethorphan
右美沙芬局部给药黏附壳聚糖-碘乙酰胺口腔片的研制
摘要本研究旨在合成壳聚糖(CHI)衍生物壳聚糖-碘乙酰胺(CHI- ia),增强其黏附性能,并开发用于局部给药右美沙芬(DXT)的CHI- ia口腔黏附片。以不同质量比的碘乙酸为原料,通过化学反应合成了黏合剂CHI-IA。利用傅里叶变换红外光谱(FT-IR)和核磁共振光谱(NMR)对合成的CHI-IA进行了表征,确定了其化学结构,确保了成功合成。以DXT为模型药,掺入基质片,研制黏附型口腔止咳片。用质构仪测定了CHI-IA片的粘接强度。此外,还对该黏附片的药物含量和释放特性进行了评价。CHI-IA的红外光谱和核磁共振光谱表明了IA对CHI结构的共轭作用。与未加修饰的CHI- ia片相比,CHI- ia片的黏附力提高了4倍。释药动力学符合Higuchi模型(R2 = 0.9912)。因此,CHI-IA可以作为一种黏附的药物传递载体系统。关键词:壳聚糖,碘乙酸,黏合剂,口腔片,右美沙芬
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