Eudragit® L100/N-trimethylchitosan chloride microspheres for oral insulin delivery.
Eudragit® L100/N-trimethylchitosan chloride microspheres for oral insulin delivery.
复制标题
Eudragit®L100/N-三甲基氯化物微球进行口服胰岛素递送。
DOI：
10.3390/molecules18066734
复制
发表时间：
2013-06-07
期刊：
影响因子：
--
通讯作者：
Steenekamp J
中科院分区：
文献类型：
--
作者：
Marais E;Hamman J;Plessis Ld;Lemmer R;Steenekamp J
蛋白质和肽类药物的有效口服给药仍然是科学研究中的一个活跃课题。在本研究中，用含有N-三甲基壳聚糖氯化物的Eudragit® L100制备基质型微球，以改善胰岛素通过细胞旁途径穿过肠上皮的渗透。最初根据析因设计（23）配制负载胰岛素的微球，并通过单一油包水乳化/蒸发方法制造。基于外部和内部形态，从初始制剂中选择两种微球制剂，用于进一步研究粒径、溶出行为和体外胰岛素在离体大鼠肠组织中的转运。最初的八种微球制剂表现出不同形状和内部结构的载药量范围为27.9-52.4%。两种选定的微球制剂的平均粒径分别为157.3 ± 31.74 µm和135.7 ± 41.05 µm，胰岛素释放的平均溶出时间值分别为34.47和42.63 min。两种选定微球制剂中胰岛素通过离体大鼠肠组织的体外转运分别是对照组（单独胰岛素）的10.67倍和9.68倍。因此，由含有N-三甲基壳聚糖氯化物的Eudragit® L100制备的微球递送系统是有效口服胰岛素递送的有希望的候选物。
Effective oral delivery of protein and peptide drugs remains an active topic in scientific research. In this study, matrix type microspheres were prepared with Eudragit® L100 containing N-trimethylchitosan chloride to improve the permeation of insulin across the intestinal epithelium via the paracellular pathway. Insulin loaded microspheres were initially formulated in accordance with a factorial design (23) and manufactured by means of a single water-in-oil emulsification/evaporation method. Based on external and internal morphology two microsphere formulations were selected from the initial formulations for further investigation in terms of particle size, dissolution behaviour and in vitro insulin transport across excised rat intestinal tissue. The initial eight microsphere formulations exhibited drug loading capacities ranging from 27.9–52.4% with different shapes and internal structures. The two selected microsphere formulations had average particle sizes of 157.3 ± 31.74 µm and 135.7 ± 41.05 µm, respectively, and mean dissolution time values for insulin release of 34.47 and 42.63 min, respectively. In vitro transport of insulin across excised rat intestinal tissue from the two selected microsphere formulations was 10.67–fold and 9.68–fold higher than the control group (insulin alone). The microsphere delivery system prepared from Eudragit® L100 containing N-trimethylchitosan chloride is therefore a promising candidate for effective oral insulin delivery.
登录
查看更多内容
影响因子：
10.8
作者：
Pauletti, GM;Gangwar, S;Borchardt, RT
通讯作者：
Borchardt, RT
影响因子：
2.9
作者：
Muzzarelli, RAA
通讯作者：
Muzzarelli, RAA
影响因子：
3.4
作者：
Snyman, D;Hamman, JH;Kotze, AF
通讯作者：
Kotze, AF
影响因子：
4.6
作者：
Kotzé, AF;Luessen, HL;Junginger, HE
通讯作者：
Junginger, HE
影响因子：
3.4
作者：
Hamman, JH;Schultz, CM;Kotzé, AF
通讯作者：
Kotzé, AF