下一代口腔黏附性辅料：预活化羧甲基纤维素。
Next generation of buccadhesive excipient: Preactivated carboxymethyl cellulose.
作者信息
Laffleur Flavia, Bacher Lukas, Vanicek Stefan, Menzel Claudia, Muhammad Ijaz
机构信息
Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Molecular Biosciences Innsbruck, University of Innsbruck, Austria.
Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Molecular Biosciences Innsbruck, University of Innsbruck, Austria.
出版信息
Int J Pharm. 2016 Mar 16;500(1-2):120-7. doi: 10.1016/j.ijpharm.2016.01.012. Epub 2016 Jan 7.
AIM
Assessment of preactivated carboxymethyl cellulose as potential excipient for buccal drug delivery.
METHODS
Firstly, carboxymethyl cellulose (CMC) and cysteine (SH) were covalently coupled via amide bond formation to obtain thiolated carboxymethyl cellulose (CMC-SH). Further, preactivated carboxymethyl cellulose (CMC-S-S-MNA) was obtained by preactivation with 2-mercaptonicotinic acid (MNA). Sulforhodamine 101 (SRH101) was used as a model drug for permeation study through buccal mucosa. CMC-S-S-MNA was evaluated with respect to mucoadhesive and permeation enhancing effect and cytotoxicity.
RESULTS
Thiolated carboxymethyl cellulose exhibited a total amount of 112.46 ± 0.46 thiol groups. CMC-S-S-MNA exhibited around 50% of preactivated thiol groups. The preactivated polymer showed no toxic effect. Furthermore, compared to unmodified CMC, CMC-S-S-MNA revealed 3.0-fold improved mucoadhesive properties according to the rotating cylinder method and 8.8-fold enhancement in mucoadhesiveness by tensile assay, respectively.
CONCLUSION
Preactivated carboxymethyl cellulose fulfills the requirements as potential excipient of being mucoadhesive and permeation enhancing for the buccal drug delivery.
目的
评估预活化羧甲基纤维素作为口腔给药潜在辅料的性能。
方法
首先，通过酰胺键形成将羧甲基纤维素（CMC）与半胱氨酸（SH）共价偶联，得到巯基化羧甲基纤维素（CMC-SH）。进一步地，用2-巯基烟酸（MNA）进行预活化，得到预活化羧甲基纤维素（CMC-S-S-MNA）。使用磺罗丹明101（SRH101）作为模型药物，用于口腔黏膜渗透研究。对CMC-S-S-MNA的黏膜黏附性、渗透促进作用及细胞毒性进行评估。
结果
巯基化羧甲基纤维素的巯基总量为112.46±0.46。CMC-S-S-MNA显示约50%的预活化巯基。预活化聚合物无毒性作用。此外，根据旋转圆筒法，与未修饰的CMC相比，CMC-S-S-MNA的黏膜黏附性能提高了3.0倍；通过拉伸试验，其黏膜黏附性增强了8.8倍。
结论
预活化羧甲基纤维素满足作为口腔给药潜在辅料的要求，具有黏膜黏附性和渗透促进作用。
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