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首页> 外文期刊>Acta Pharmacologica Sinica >Permeation-enhancing effects of chitosan formulations on recombinant hirudin-2 by nasal delivery in vitro and in vivo
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Permeation-enhancing effects of chitosan formulations on recombinant hirudin-2 by nasal delivery in vitro and in vivo

机译：壳聚糖制剂通过体外和体内鼻腔输送对重组水rud素2的渗透增强作用

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Aim: To investigate the enhancing effects of chitosan with or without enhancers on nasal recombinant hirudin-2 (rHV2) delivery in vitro and in vivo, and to evaluate the ciliotoxicity of these formulations. Methods: The permeation-enhancing effect of various chitosan formulations was estimated by using the permeation coefficient of fluorescein isothiocyanate recombinant hirudin-2 (FTTC-rHV2) across the excited rabbit nasal epithelium in vitro. The effect was further evaluated by measuring the blood concentration level after nasal absorption of FITC-rHV2 in rats. The mucosal ciliotoxicity of different formulations was evaluated with an in situ toad palate model. Results: Chitosan at a concentration of 0.5% with or without various enhancers significantly increased the permeability coefficient (P) and relative bioavailability (Fr) of FITC-rHV2 compared with the blank control. The addition of 1% sodium dodecylsulfate, 5% Brij35,5% Tween 80,1.5% menthol, 1% glycyrrhizic acid monoammonium salt (GAM) or 4% Azone into the 0.5% chitosan solution resulted in a further increase in absorption (P < 0.05) compared with 0.5% chitosan alone. But co-administration of chitosan with 5% hydroxyl-propyl-beta-cyclodextrin (HP-β-CD), 5% lecithin or 0.1% ethylenediamine tetraacetic acid (EDTA) was not more effective than using the 0.5% chitosan solution alone. Chitosan alone and with 5% HP-β-CD, 0.1% EDTA, 1% GAM or 5%Tween80 was relatively less ciliotoxic. Conclusion: Chitosan with or without some enhancers was able to effectively promote the nasal absorption of recombinant hirudin, while not resulting in severe mucosal ciliotoxicity. A chitosan formulation system would be a useful approach for the nasal delivery of recombinant hirudin.
机译：目的：研究壳聚糖在有或没有增强剂的情况下对体内和体外经鼻重组水rud素2（rHV2）递送的增强作用，并评估这些制剂的纤毛毒性。方法：利用异硫氰酸荧光素重组水rud素-2（FTTC-rHV2）在体外兴奋兔鼻上皮的渗透系数，评估各种壳聚糖制剂的渗透增强作用。通过测量大鼠鼻腔吸收FITC-rHV2后的血药浓度水平，进一步评估了该作用。用原位蟾蜍pa模型评价不同制剂的粘膜纤毛毒性。结果：与空白对照组相比，在有或没有各种增强剂的情况下，浓度为0.5％的壳聚糖可显着提高FITC-rHV2的渗透系数（P）和相对生物利用度（Fr）。在0.5％的脱乙酰壳多糖溶液中添加1％的十二烷基硫酸钠，5％的Brij35、5％的Tween 80.1.5％薄荷醇，1％的甘草酸一铵盐（GAM）或4％的Azone导致吸收进一步增加（P < 0.05），而单独使用0.5％的壳聚糖。但是，将壳聚糖与5％羟丙基-β-环糊精（HP-β-CD），5％卵磷脂或0.1％乙二胺四乙酸（EDTA）并用比单独使用0.5％壳聚糖溶液更有效。单独的壳聚糖和5％HP-β-CD，0.1％EDTA，1％GAM或5％Tween80的纤溶性相对较低。结论：含或不含某些增强剂的壳聚糖能够有效促进重组水rud素的鼻吸收，而不会引起严重的粘膜纤毛毒性。壳聚糖制剂系统将是鼻内递送重组水rud素的有用方法。

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