Spray-dried chitosan ethylcellulose microspheres for nasal drug delivery: Swelling study and evaluation of in vitro drug release properties

• Published in: Journal of microencapsulation Vol. 22; no. 5; pp. 549 - 561
• Main Authors: Martinac, A., Filipovi -Gr i, J., Perissutti, B., Voinovich, D., Paveli, .
• Format: Journal Article
• Language: English
• Published: Colchester Informa UK Ltd 01.08.2005; Taylor & Francis; Informa
• Subjects: Absorption; Administration, Intranasal; Biocompatible Materials; Biological and medical sciences; Calorimetry, Differential Scanning - methods; Cellulose - analogs & derivatives; Chitosan; Delayed-Action Preparations; Drug Compounding - methods; drug release profile; ethylcellulose; General pharmacology; Histamine H1 Antagonists, Non-Sedating - administration & dosage; Humans; Loratadine - administration & dosage; Medical sciences; Microspheres; nasal delivery; Nasal Lavage Fluid; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Sclerosing Solutions; swelling properties; Drug; Evaluation; Microsphere; Pharmaceutical technology; Swelling; microspheres; Vehicle(excipient); swelling properties; Intranasal administration; nasal delivery; In vitro; drug release profile; Microparticle; Chitosan; Release; Ethylcellulose
• ISSN: 0265-2048; 1464-5246
• DOI: 10.1080/02652040500098960

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.