Ikechukwu V. Onyishi

The aim of the study was to formulate colon targeted diclofenac sodium alginate beads. The beads were formulated by ionotropic gelation using sodium alginate as polymer, calcium carbonate as an internal cross linking agent and calcium chloride as an external cross linking agent. The optimized beads contained Neusilin and coated with Eudragit L100. The beads were analyzed in terms of, encapsulation efficiency (EE%), particle size and morphology. Swelling properties were studied in simulated gastric fluid (SGF, pH 1.2) and simulated intestinal fluid (SIF, pH 7.4). In vitro drug release was studied in SGF, pH 1.2, SIF, pH 6.8 and SIF, pH 7.4. The results show that the particle size of the beads ranged from 1.98 ± 0.40 to 2.80 ± 0.30 mm. The optimized batch containing Neusilin® had the highest EE% of 72 % significantly higher than other batches (p < 0.05). The degree of swelling of the beads was zero in SGF and about 90 % in SIF at 100 min. The results of the in vitro release showed that the beads had 0 % release in SGF, pH, 1.2 at 2 h, about 3 % in SIF, pH 6.8 at 4 h and 9 % drug release in SIF, pH 7.4 at 9 h. Therefore, sodium alginate beads could be used for colon delivery of diclofenac sodium. 

The aim of the work is to produce microcrystalline cellulose (MCC) from sugarcane bagasse (Saccarhum officinarum) and to characterise the MCC and compare with Avicel®. MCC was produced from α-cellulose produced by alkaline hydrolysis from sugarcane bagasse and bleached with sodium hypochlorite. The MCC were identified by BP (2009) method and characterised in terms of pH, moisture and ash content respectively. The physico-technical properties of MCC were studied including the particle size and flowability and compared with that of Avicel®. Also, the phytochemical properties of MCC were studied. The results of the phytochemical analysis of MCC from bagasse showed the presence of alkaloid in low concentration while, carbohydrates and glycosides were seen in very large concentrations, while flavonoids, saponin, tannin, resins, steroids, terpenoids, reducing sugars, proteins, fats and oil and acidic compounds were absent. MCC produced had a pH of 7 and moisture content of 7 % and exhibited mean particle diameter of 200.00 ± 0.05 µm. The results of the true density of the MCC showed that the differences in density between the MCC from bagasse and Avicel® were not significant (p < 0.05). The results of angle of repose, Carr’s index and Hausner’s quotient showed that the MCC from bagasse and Avicel® exhibited poor flow which could be improved by use of glidants. Therefore, MCC from bagasse could be used as diluents-binder in direct compression tableting and as diluents and or disintegrant in wet granulation tableting.

In view of the wide spread use of herbal formulations and its proven efficacy, there is need for standardization and quality control. Gongronema latifolium is widely used in the folk medicine in the treatment of diabetes, hence the need for an effective delivery system for this natural plant. The methanolic extract of Gongronema latifolium leaves (1, 3 and 5 %) were formulated into lipospheres by melt homogenization using lipid matrix consisting of mixture of goat fat and Phospholipon® 90H (1:2). The lipospheres were characterized by analyzing the encapsulation efficiency(EE), pH, particle size and morphology. The in vivo antidiabetic properties were studied in alloxan induced diabetic Wistar rats. The results showed spherical lipospheres within µm limit, stable pH over 30 days and EE% of 86, 89 and 90 % for batches A, B and C containing 1, 3 and 5 % Gongronema latifolium extract. Gongronema latifolium-loaded lipospheres (100 mg/kg) had 55.2 and 70.6 % reduction in blood glucose of the diabetic rats at 8 and 12 h respectively, while, the rats that received glibenclamide (0.2 mg/kg) had 38.4 and 53.4 % reduction in blood glucose at 8 and 12 h. Gongronema latifolium-loaded lipospheres had significantly higher antidiabetic properties than (p < 0.05) the reference drug at concentrations used.