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    Development of ibuprofen microspheres using acetylated plantain starches as polymer for sustained release
    (Springer Publications, 2018) Okunlola, A.; Ghomorai, T.
    Ibuprofen has a short half-life (1–3 h) and istypically administered 3–4 times daily with subsequent adverse side effects. A good approach to reduce these effects is the preparation of sustained-release formulations of ibuprofen. Acetylated starches form water-insoluble, acid-resistant films that can substantially retard drug release. Ibuprofen microspheres were prepared using acetylated plantain starch as sustained-release polymer. Starch obtained from unripe plantain (Musa Paradisiaca normalis) were acetylated using acetic anhydride with pyridine (degrees of substitution, DS 1.5 ± 0.05 and 2.20 ± 0.10). The starches were characterized using morphology, crystallinity, swelling, density and flow properties. Ibuprofen microspheres were prepared by quasi-emulsion solvent diffusion method, using acetylated plantain starches DS 1.5 and 2.20 in comparison to Eudragit S100. Full 32 factorial experimental design was performed with polymer type (X1), polymer: drug ratio (X2) as independent factors; microsphere size, entrapment, and quantity of drug released in 12 h (Q12) were dependent variables. The data from in vitro drug release were fitted to various kinetic models. Acetylation resulted in larger starch aggregates with disruption in crystalline order. Ibuprofen microspheres were spherical with size 5.50 ± 4.00–129.90 ± 12.97μm. Drug entrapment was 43.92 ± 4.00–79.91 ± 6.15%. Values of Q12 ranged from 20.10 ± 0.55 to 54.00 ± 5.71%. Interaction between variables X1 and X2 had positive effects on size and entrapment. Drug release fitted zero order, first order and Baker-Lonsdale kinetic models. Acetylated starch of plantain with DS 2.20 was suitable as a polymer at polymer:drug ratio 4:1 for the formulation of ibuprofen microspheres with prolonged drug release.
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    Formulation of floating metronidazole microspheres using cassava starch (manihot esculenta) as polymer
    (Springer Publications, 2017) Odeku, O. A; Aderogba, A. A.; Ajala, T. O.; Akin-Ajani, O. D.; Okunlola, A
    " Floating gastroretentive microspheres have been used to prolong the gastric residence time after oral administration and improve the local effect of metronidazole in the stomach in the treatment of peptic ulcer caused by Helicobacter pylori. In the present study, cassava starch, obtained from the tubers of Manihot esculenta has been pregelatinized and used as polymer in combination with sodium alginate for the formulation of floating gastroretentive metronidazole microspheres. Metronidazole microspheres were prepared by ionic gelation method using pregelatinized cassava starch and sodium alginate at different concentrations as polymers and calcium chloride (2% w/v) as chelating agent. Sodium bicarbonate (2% w/w) was used as gas releasing agent. Microspheres were characterized using the particle size, swelling index, floating lag time (FLT), total floating time and drug release properties. Spherical discrete microspheres with size ranging from 1.52 to 2.23 mm were obtained with FLT of less than 5min and drug entrapment efficiency of 42–60% w/w. The microsphere maintained buoyancy for over 19h and the microspheres provided controlled release of metronidazolefor up to 18h. Drug release from the microspheres, swelling index and buoyancy depended on the concentration of cassava starch in the polymer blend. Formulations containing high concentration of cassava starch showing shorter floating lag time and faster drug release. Thus, buoyancy and rate of drug release appeared to be modulated by the concentration of cassava starch in the polymer blend. The results showed that pregelatinized cassava could be useful in the formulation of floating gastroretentive metronidazole microspheres "