Drug Res (Stuttg) 2018; 68(12): 673-679
DOI: 10.1055/a-0586-8406
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Preparation and Properties of 5-Fluorouracil-Loaded Chitosan Microspheres for the Intranasal Administration

Wanqing Li*
1   School of Preclinical Medicine, Beijing University of Chinese Medicine Beijing, China
,
Hongyuan Ba
2   Academy of Sports Medicine and Physiotherapy, Beijing Sport University Beijing, China
,
Peng Huang
2   Academy of Sports Medicine and Physiotherapy, Beijing Sport University Beijing, China
,
Aiping Zheng
3   State Key Laboratory of Toxicology and Medical Countermeasures, Department of Pharmaceutics, Institute of Pharmacology and Toxicology of Academy of Military Medical Sciences, Beijing, China
,
Xi Yang
3   State Key Laboratory of Toxicology and Medical Countermeasures, Department of Pharmaceutics, Institute of Pharmacology and Toxicology of Academy of Military Medical Sciences, Beijing, China
› Author Affiliations
Further Information

Publication History

received 05 September 2017

accepted 05 March 2018

Publication Date:
02 July 2018 (online)

Abstract

Objective To study the preparation technique of 5-fluorouracil and the release characteristic of 5-fluorouracil-loaded chitosan microspheres for the intranasal administration.

Methods 5-fluorouracil-loaded chitosan microspheres were prepared by emulsion chemical cross-link technique. The orthogonal experimental design was used to optimize the preparation procedure. Dynamic dialysis method was applied to determine the release characteristic of microspheres in vitro and its influencing factors. Swelling behavior was expressed by swelling ratio. The degree of mucoadhesion was investigated by determining the mucociliary transport rate(MTR) of the microparticle across a frog palate.

Results Microspheres with a good shape and narrow size distribution were prepared. The average diameter was 43±4 μm. The drug loading was (38.5±1.0) %. The entrapment efficiency was (79.0±1.8) %. The drug release profile in vitro could be described by Higuichi eqution as Q=0.1035t1/2+0.0284 (r=0.9965). Chitosan had good mucoadhesive property and caused a significant reduction in MTR(P<0.01).

Conclusion The optimized technique has a good reproducibility and a high entrapment efficiency, so it could be used to prepare 5-fluorouracil-loaded chitosan microspheres for the intranasal administration.Chitosan is a good material for nasal preparation and has prospective development in the pharmaceutical field.

* Wanqing Li mainly contributed to the study


 
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