title: Development of mucoadhesive microbeads using thiolated sodium alginate for intrapocket delivery of resveratrol.
abstract: 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 1h, compared to 2% for A microbeads. SEM micrographs showed a rough surface with drug precipitation. The formula maintained its %EE after 5h exposure to direct sunlight. A/TA 1:1 mucoadhesive Res microbeads could be exploited as a prolonged drug release devices for intrapocket application.
authors: Department of Pharmaceutical Sciences, Faculty of Pharmacy, Princess Nourah bint Abdulrahman University, Riyadh, Saudi Arabia; Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt. Electronic address: abeerkassem2002@gmail.com.
authors: Abeer Ahmed
authors: AA
authors: Kassem
authors: Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Pharos University in Alexandria, Alexandria, Egypt.
authors: Ragwa Mohamed
authors: RM
authors: Farid
authors: Department of Pharmaceutical Sciences, Faculty of Pharmacy, Beirut Arab University, Beirut, Lebanon; Department of Pharmaceutical chemistry, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
authors: Doaa Ahmed Elsayed
authors: DA
authors: Issa
authors: Department of Oral Medicine, Periodontology, Oral Diagnosis and Radiology, Faculty of Dentistry, Pharos University in Alexandria, Alexandria, Egypt.
authors: Doaa Said
authors: DS
authors: Khalil
authors: Department of Oral Medicine, Periodontology, Oral Diagnosis and Radiology, Faculty of Dentistry, Tanta University, Tanta, Egypt.
authors: Mona Yehia
authors: MY
authors: Abd-El-Razzak
authors: Department of Oral Medicine, Periodontology, Oral Diagnosis and Radiology, Faculty of Dentistry, Tanta University, Tanta, Egypt.
authors: Hussein Ibrahim
authors: HI
authors: Saudi
authors: Department of Oral Biology, Faculty of Dentistry, Tanta University, Tanta, Egypt.
authors: Heba Mohamed
authors: HM
authors: Eltokhey
authors: Department of Clinical Pathology, Faculty of Medicine, Tanta University, Tanta, Egypt.
authors: Enas Arafa
authors: EA
authors: El-Zamarany
mesh_terms: D000464:Alginates / Q000737:chemistry*; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage*; D002626:Chemistry, Pharmaceutical; D002645:Chickens; D016503:Drug Delivery Systems; D005079:Excipients; D005881:Gingiva; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D009092:Mucous Membrane / Q000187:drug effects*; D010316:Particle Size; D000077185:Resveratrol; D012995:Solubility; D013267:Stilbenes / Q000008:administration & dosage*; D013438:Sulfhydryl Compounds / Q000737:chemistry*; D013864:Thioglycolates; D014014:Tissue Adhesives
chemical_list: D000464:Alginates; D000975:Antioxidants; D005079:Excipients; D006603:Hexuronic Acids; D013267:Stilbenes; D013438:Sulfhydryl Compounds; D013864:Thioglycolates; D014014:Tissue Adhesives; C017487:2-mercaptoacetate; D020723:Glucuronic Acid; D000077185:Resveratrol
keywords: Alginate – thioglycolic acid conjugate; Ionotropic gelation; Periodontal; Polyphenol