Department of Pharmacy, Stamford University Bangladesh 51, Siddeswari Road, Dhaka-1217, Bangladesh.
Curr Drug Deliv. 2013 Dec;10(6):765-70. doi: 10.2174/15672018113109990054.
The objective of this study was to develop and evaluate mucoadhesive microsphere of diclofenac sodium with natural gums for sustained delivery. Guar gum and tragacanth were used along with sodium alginate as mucoadhesive polymers. Microspheres were formulated using orifice-ionic gelation method. Particle size, surface morphology, swelling study and drug entrapment efficiency of the prepared microspheres were determined. In vitro evaluation was carried out comprising of mucoadhesion and drug release study. The prepared microspheres were discrete and free flowing. Sodium alginate and natural gum, at a ratio of 1:0.25, showed good mucoadhesive property and they had high drug entrapment efficiencies. They also exhibited the best rate retarding effect among all the formulations. Drug entrapment efficiency of all the microspheres ranged from 80.42% to 91.67%. An inverse relationship was found between extent of crosslinking and drug release rate. Release rate was slow and extended in case of the formulations of 1:0.25 ratio (F1 and F3), releasing 68.36% and 70.56% drug respectively after 8 hours. Tragacanth-containing microspheres of F1 showed superiority over other formulations, with best mucoadhesive and rate retarding profile. The correlation value (r(2)) indicated that the drug release of all the formulations followed Higuchi's model. Overall, the results indicated that mucoadhesive microspheres containing natural gum can be promising in terms of prolonged delivery with good mucoadhesive action, targeting the absorption site to thrive oral drug delivery.
本研究旨在开发和评估载有双氯芬酸钠的具有天然胶的粘膜粘附性微球，用于持续释放。瓜尔胶和刺槐豆胶与海藻酸钠一起用作粘膜粘附性聚合物。采用孔-离子凝胶化法制备微球。测定了所制备的微球的粒径、表面形态、溶胀研究和药物包封效率。进行了体外评估，包括粘膜粘附性和药物释放研究。所制备的微球是离散的和自由流动的。海藻酸钠和天然胶（比例为 1:0.25）显示出良好的粘膜粘附性，并且具有高的药物包封效率。它们在所有配方中表现出最佳的延缓药物释放效果。所有微球的药物包封效率范围为 80.42%至 91.67%。交联程度与药物释放速率之间存在反比关系。在 1:0.25 比例的配方（F1 和 F3）中，释放速率较慢且延长，8 小时后分别释放 68.36%和 70.56%的药物。含刺槐豆胶的 F1 微球优于其他配方，具有最佳的粘膜粘附性和延缓药物释放效果。相关值（r(2)）表明，所有配方的药物释放均遵循 Higuchi 模型。总的来说，结果表明，含有天然胶的粘膜粘附性微球在延长药物释放时间、具有良好的粘膜粘附作用、靶向吸收部位方面具有良好的应用前景，可促进口服药物传递。
