Okunlola Adenike, Odeku Oluwatoyin A, Lamprecht Alf, Oyagbemi Ademola A, Oridupa Olayinka A, Aina Oluwasanmi O
Department of Pharmaceutics & Industrial Pharmacy, University of Ibadan, Ibadan, Nigeria.
Department of Pharmaceutics & Industrial Pharmacy, University of Ibadan, Ibadan, Nigeria; Laboratory of Pharmaceutical Technology, Institute of Pharmacy, Rheinische Friedrich-Wilhelms University, Bonn, Germany.
Int J Biol Macromol. 2015 Aug;79:226-34. doi: 10.1016/j.ijbiomac.2015.04.062. Epub 2015 May 2.
Cissus gum has been employed as polymer with sodium alginate in the formulation of diclofenac microbeads and the in vivo mucoprotective properties of the polymer in anti-inflammatory therapy assessed in rats with carrageenan-induced paw edema in comparison to diclofenac powder and commercial diclofenac tablet. A full 2(3) factorial experimental design has been used to investigate the influence of concentration of cissus gum (X1); concentration of calcium acetate (X2) and stirring speed (X3) on properties of the microbeads. Optimized small discrete microbeads with size of 1.22±0.10 mm, entrapment efficiency of 84.6% and t80 of 15.2±3.5 h were obtained at ratio of cissus gum:alginate (1:1), low concentration of calcium acetate (5% w/v) and high stirring speed (400 rpm). In vivo studies showed that the ranking of percent inhibition of inflammation after 3h was diclofenac powder>commercial tablet=cissus>alginate. Histological damage score and parietal cell density were lower while crypt depth and mucosal width were significantly higher (p<0.05) in the groups administered with the diclofenac microbeads than those administered with diclofenac powder and commercial tablet, suggesting the mucoprotective property of the gum. Thus, cissus gum could be suitable as polymer in the formulation of non-steroidal anti-inflammatory drugs ensuring sustained release while reducing gastric side effects.
西苏斯胶已被用作与海藻酸钠的聚合物，用于制备双氯芬酸微珠，并在角叉菜胶诱导的爪肿胀大鼠中评估该聚合物在抗炎治疗中的体内粘膜保护特性，与双氯芬酸粉末和市售双氯芬酸片剂进行比较。采用全2(3)析因实验设计来研究西苏斯胶浓度(X1)、醋酸钙浓度(X2)和搅拌速度(X3)对微珠性质的影响。在西苏斯胶:海藻酸盐比例为1:1、醋酸钙浓度低(5% w/v)和搅拌速度高(400 rpm)的条件下，获得了尺寸为1.22±0.10 mm、包封率为84.6%、t80为15.2±3.5 h的优化小离散微珠。体内研究表明，3小时后炎症抑制百分比的排名为双氯芬酸粉末>市售片剂=西苏斯胶>海藻酸盐。与给予双氯芬酸粉末和市售片剂的组相比，给予双氯芬酸微珠的组的组织学损伤评分和壁细胞密度较低，而隐窝深度和粘膜宽度显著较高(p<0.05)，表明该胶具有粘膜保护特性。因此，西苏斯胶可适合作为聚合物用于非甾体抗炎药的制剂中，确保持续释放同时减少胃部副作用。
