Spray-dried chitosan/ethylcellulose microspheres for nasal drug delivery: swelling study and evaluation of in vitro drug release properties.
The aim of this study was to develop spray-dried chitosan-based microspheres, suitable for nasal delivery of loratadine, and to evaluate their potential of modifying loratadine release. The microspheres were composed with ethylcellulose (EC) and chitosan (CM) in two different weight ratios, 1:2 and 1:3. One-phase systems (dispersions) and two-phase systems (emulsions and suspensions) were subjected to spray-drying, resulting in conventional and composed microspheres, respectively. The microspheres were evaluated with respect to the yield, particle size, encapsulation efficiency, physical state of the drug in the polymer matrix, swelling properties and in vitro drug release profile. It was shown that particle size, swelling ability and loratadine release from spray-dried microspheres were significantly affected by the polymeric composition and feed concentration in spray-drying process. Emulsifying method to produce composed EC/CM microspheres resulted in improved loratadine entrapment and moderate swelling, when compared to conventional chitosan microspheres. It seems like better formation of EC cores and chitosan coating were obtained when higher feed concentration and ultrasonic homogenization were employed in the preparation of emulsion systems and when EC to CM weight ratio was 1:3.
Martinac
A
A
Department of Pharmaceutics, Faculty of Pharmacy and Biochemistry, University of Zagreb, Croatia.
Filipović-Grcić
J
J
Perissutti
B
B
Voinovich
D
D
Pavelić
Z
Z
D000042:Absorption; D000281:Administration, Intranasal; D001672:Biocompatible Materials; D002152:Calorimetry, Differential Scanning / Q000379:methods; D002482:Cellulose / Q000031:analogs & derivatives*; D048271:Chitosan; D003692:Delayed-Action Preparations; D004339:Drug Compounding / Q000379:methods; D039563:Histamine H1 Antagonists, Non-Sedating / Q000008:administration & dosage; D006801:Humans; D017336:Loratadine / Q000008:administration & dosage; D008863:Microspheres; D017817:Nasal Lavage Fluid; D010316:Particle Size; D012597:Sclerosing Solutions
D001672:Biocompatible Materials; D003692:Delayed-Action Preparations; D039563:Histamine H1 Antagonists, Non-Sedating; D012597:Sclerosing Solutions; D017336:Loratadine; C013517:ethyl cellulose; D002482:Cellulose; D048271:Chitosan