title: Nasal polysaccharides-glucose regulator microparticles: optimization, tolerability and antidiabetic activity in rats.
abstract: The aim of the present study was to load the post-prandial glucose regulator, repaglinide (REP), on spray dried mucoadhesive microparticles (MPs) comprising anionic polysaccharides. The formulation parameters of the polysaccharides-REP spray dried powders (SDP) namely, polysaccharide type and drug to polymer (D/P) ratio, were optimized for % release after 5 min (R%5 min) and time required for 80% release (T80%). The suitability of the selected formulae for nasal application was evaluated by ex vivo mucoadhesion, in vitro cytocompatability and tolerability studies. A pharmacodynamic study in diabetic rats was conducted. Results showed that both polysaccharide type and amount greatly influenced the chosen responses. REP was highly incorporated in mucoadhesive MPs with proven safety on the rat nasal mucosa. The selected REP loaded powders exhibited a significant two to threefold increase in total decrease in blood glucose compared to the nasal and intravenous solutions.
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Egypt.
authors.forename: Enas
authors.initials: E
authors.lastname: Elmowafy
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Egypt. Electronic address: rihabosman@pharma.asu.edu.eg.
authors.forename: Rihab
authors.initials: R
authors.lastname: Osman
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Egypt.
authors.forename: Abd El-Hameed A
authors.initials: Ael-H
authors.lastname: El-Shamy
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Egypt.
authors.forename: Gehanne A S
authors.initials: GA
authors.lastname: Awad
mesh_terms: D000281:Administration, Intranasal; D000818:Animals; D001786:Blood Glucose / Q000187:drug effects; D002219:Carbamates / Q000008:administration & dosage / Q000627:therapeutic use; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy; D016503:Drug Delivery Systems / Q000379:methods; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000627:therapeutic use*; D008297:Male; D009297:Nasal Mucosa; D010880:Piperidines / Q000008:administration & dosage / Q000627:therapeutic use; D051381:Rats
chemical_list: D001786:Blood Glucose; D002219:Carbamates; D007004:Hypoglycemic Agents; D010880:Piperidines; C072379:repaglinide
keywords: Antidiabetic; Insufflator; Microparticles; Nasal powder; Polysaccharides; Spray drying