Preparation of Zolmitriptan water-soluble carboxylation chitosan microspheres for nasal delivery by emulsification solvent evaporation method and its characteristics evaluation
- Author:
Chao-Qun YU
1
Author Information
- Publication Type:Journal Article
- Keywords: Carboxylation chitosan; Emulsification solvent evaporation technique; Microspheres; Zolmitriptan
- From: Chinese Pharmaceutical Journal 2013;48(10):800-804
- CountryChina
- Language:Chinese
- Abstract: OBJECTIVE: To prepare microspheres for nasal delivery by emulsification solvent evaporation technique using water-soluble carboxylation chitosan as the drug carrier, thus to avoid using stimulatory and toxic aldehydes crosslinkers and acid solvent which are used by the traditional method. METHODS: Zolmitriptan (ZT) was used as the model drug to prepare the carboxylation chitosan microspheres. The prescription and technology were optimized to prepare the microspheres. The yield, particle sizes, appearance, drug loading, encapsulation efficiency and drug release of the microspheres were evaluated. RESULTS: The microspheres prepared by the optimized method were spherical, smooth, and free flowing. The particle sizes of the microspheres were well-distributed and the mean particle size was (21.4±10.1)μm. The drug loading was 5.67% and the encapsulation efficiency was 62.4%. The in vitro release study of the microspheres showed that the drug was sustainedly released and could be released for about 85% in 8 h. CONCLUSION: It is feasible to prepare carboxylation chitosan microspheres for nasal administration by emulsification solvent evaporation method, avoiding the use of aldehydes crosslinkers and acid solvent.