Development of mucoadhesive microbeads using thiolated sodium alginate for intrapocket delivery of resveratrol

作者：Kassem Abeer Ahmed^*; Farid Ragwa Mohamed; Issa Doaa Ahmed Elsayed; Khalil Doaa Said; Abd El Razzak Mona Yehia; Saudi Hussein Ibrahim; Eltokhey Heba Mohamed; El zamarany Enas Arafa

来源：International Journal of Pharmaceutics, 2015, 487(1-2): 305-313.

DOI：10.1016/j.ijpharm.2015.04.010

• Polyphenol
• Ionotropic gelation
• Alginate - thioglycolic acid conjugate
• Periodontal

Resveratrol (Res), a polyphenolic phytoalexin, had shown a promising therapeutic efficacy towards treatment of periodontal disease in vitro. This work aims to develop Res microbeads with strong mucoadhesion using thiolated alginate (TA) for local treatment of periodontal pockets. TA was synthesized by conjugating sodium alginate (A) with thioglycolic acid. Product was evaluated by IR and DSC. Both A and A: TA Res microbeads with different ratios were prepared by ionotropic gelation method. Formulations were evaluated regarding their entrapment efficiency (%EE), swelling index (SI), in vitro drug release and kinetics. Selected formula was examined for its mucoadhesion by ex vivo wash-off method, surface morphology using scanning electron microscope (SEM) and stability against light. Clinical evaluation is running. Formation of TA was confirmed. % EE for all formulations ranged from 83.72 to 104.54%. Results revealed a significant lower SI for TA rich formulation (A/TA 1: 1) along with slower release rate and zero-order kinetics, in addition to powerful mucoadhesion; 26% remaining of microbeads after 1 h, compared to 2% for A microbeads. SEM micrographs showed a rough surface with drug precipitation. The formula maintained its % EE after 5 h exposure to direct sunlight. A/TA 1: 1 mucoadhesive Res microbeads could be exploited as a prolonged drug release devices for intrapocket application.

• 出版日期2015-6-20