依托泊苷鼻用黏附微球的性质考察及药动学研究

Properties and Pharmacokinetic Studies on Etoposide-Loaded Chitosan Microspheres for nasal Administration

目的通过对依托泊苷壳聚糖微球的黏附性、纤毛毒性及家兔体内药动学研究,评价其鼻腔给药的应用价值及作用。方法采用在体蟾蜍上颚纤毛评价微球的纤毛毒性,用纤毛输送速率考察黏膜黏附性;用HPLC测定不同剂型和不同给药方式家兔体内吸收情况。结果依托泊苷壳聚糖微球具有黏附性,无纤毛毒性;鼻腔给药后峰浓度(ρmax)为(85.99±3.52)μg·L-1,达峰时间(tmax)为(60.64±7.66)min。结论壳聚糖微球可以延长药物在鼻腔内的滞留时间,提高药物吸收,有很好的应用前景。

OBJECTIVE To investigate the mucoadhesive property, ciliotoxicity and pharmacokinetics for evaluaing the effects of etoposide-loaded chitosan microspheres for nasal administration, METHODS Mucoadhesive property and ciliotoxicity were evaluated with in situ toad palate model, High-performance Liquid Chromatograph was adopted for determining the concentration of etoposide in rabbit serum, RESULTS Chitosan microspheres had good mucoadhesive property and very low toxicity, after nasal administration, ρmax= （85.99± 3.52）μg·L^-1 and tmax （ 60. 64± 7. 66） min. CONCLUSION Chitosan microspheres could prolong the residence time of drug in the nasal cavity and increase the bioavailability of etoposide.