聚胺化支链淀粉，一种新型的可生物降解的阳离子支链淀粉衍生物，用于粘膜药物传递。
Polyaminated pullulan, a new biodegradable and cationic pullulan derivative for mucosal drug delivery.
机构信息
Center for Chemistry and Biomedicine, Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Austria; Department of Industrial Pharmacy, University of Medicine and Pharmacy at Ho Chi Minh City, Viet Nam.
Center for Chemistry and Biomedicine, Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Austria.
出版信息
Carbohydr Polym. 2022 Apr 15;282:119143. doi: 10.1016/j.carbpol.2022.119143. Epub 2022 Jan 15.
AIM
To prepare new polycationic pullulan derivatives exhibiting highly mucoadhesive and sustained drug release properties.
METHODS
Hydroxy groups of pullulan were activated with mesyl chloride followed by conjugation with low-molecular weight polyamines. Pullulan-tris(2-aminoethyl)amine (Pul-TAEA) and pullulan-polyethyleneimine (Pul-PEI) were evaluated regarding swelling behaviour, mucoadhesive properties and potential to control drug release.
RESULTS
Pul-TAEA and Pul-PEI exhibited excellent swelling properties at pH 6.8 showing 240- and 370-fold increase in weight. Compared to unmodified pullulan, Pul-TAEA and Pul-PEI displayed 5- and 13.3-fold increased dynamic viscosity in mucus. Mucoadhesion studies of Pul-TAEA and Pul-PEI on intestinal mucosa showed a 6- and 37.8-fold increase in tensile strength, and a 72- and 120-fold increase in mucoadhesion time compared to unmodified pullulan, respectively. Due to additional ionic interactions between cationic groups on polyaminated pullulans and an anionic model drug, a sustained drug release was achieved.
CONCLUSIONS
Polyaminated pullulans are promising novel mucoadhesive excipients for mucosal drug delivery.
目的
制备具有高度黏膜黏附性和持续药物释放性能的新型聚阳离子普鲁兰衍生物。
方法
用氯甲磺酸活化普鲁兰的羟基，然后与低分子量聚胺缀合。对普鲁兰三（2-氨基乙基）胺（Pul-TAEA）和普鲁兰-聚乙烯亚胺（Pul-PEI）的溶胀行为、黏膜黏附性能和控制药物释放的潜力进行了评价。
结果
Pul-TAEA 和 Pul-PEI 在 pH 6.8 时表现出优异的溶胀性能，重量增加了 240-370 倍。与未修饰的普鲁兰相比，Pul-TAEA 和 Pul-PEI 在黏液中的动态粘度分别增加了 5-13.3 倍。Pul-TAEA 和 Pul-PEI 对肠黏膜的黏膜黏附研究表明，与未修饰的普鲁兰相比，拉伸强度分别增加了 6-37.8 倍，黏膜黏附时间分别增加了 72-120 倍。由于聚胺化普鲁兰上的阳离子基团与阴离子模型药物之间的额外离子相互作用，实现了药物的持续释放。
结论
聚胺化普鲁兰是一种有前途的新型黏膜给药黏附性赋形剂。
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