Intestinal transit of bioadhesive microspheres in an in situ loop in the rat—A comparative study with copolymers and blends based on poly(acrylic acid)
Intestinal transit of bioadhesive microspheres in an in situ loop in the rat—A comparative study with copolymers and blends based on poly(acrylic acid)
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DOI：
10.1016/0168-3659(90)90074-4
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发表时间：
1990-07
影响因子：
10.8
通讯作者：
C. Lehr;J. Bouwstra;J. Tukker;H. Junginger
中科院分区：
文献类型：
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作者：
C. Lehr;J. Bouwstra;J. Tukker;H. Junginger
通过测定将涂覆聚合物的玻璃板从猪肠黏膜上分离所需的力，筛选了两种商用的丙烯酸共聚物Carbomer(Carbopol®934P)和PolyCarophl(Carbopol®EX-55树脂)以及与Eudradit®RL 100的混合物的粘附性。采用悬浮聚合法制备了聚甲基丙烯酸羟乙酯(PHEMA)微球，并在空气悬浮法中包覆了候选粘附性聚合物。采用大鼠慢性离体回肠回肠模型，研究微球的肠道转运。通过记录微球在灌流肠段内的平均滞留时间来评价该潜在给药系统的生物黏附性能。与卡波姆相比，聚碳酸酯在体外表现出显著的粘附性。在模型中，卡波姆涂层微球的滞留时间与未涂层的对照组相当，而聚碳酸酯涂层微球最初表现出显著的生物粘附性。
Two commercially available copolymers of acrylic acid, Carbomer (Carbopol®934P) and Polycarbophil (Carbopol®EX-55 resin), and blends with Eudragit®RL 100 were screened for their mucoadhesive properties by determining the force needed to detach a polymer coated glass plate from porcine intestinal mucosain vitro. Microspheres of poly(2-hydroxyethyl methacrylate) (PHEMA) were synthesized by suspension polymerization and coated with candidate mucoadhesive polymers in an air-suspension process. A chronically isolated ileal loop model in the rat was used in order to study the intestinal transit of the microspheres. Bioadhesive properties of this potential drug delivery system were evaluated by recording the mean residence time of the microspheres when injected into thein situperfused gut segment. Polycarbophil showed significantly improved mucoadhesive propertiesin vitroin comparison to Carbomer. In thein situmodel, the residence time of Carbomer-coated microspheres was comparable to the non-coated controls, whereas Polycarbophil-coated spheres initially showed a marked bioadhesion.