Development of oil-in-water (o/w) nanoemulsion formulations for spontaneous transdermal delivery of ciprofloxacin

Nanoemulsions have attracted attention in delivery of therapeutically active agents since most of the new chemical entities are hydrophobic in nature and the delivery of poor water soluble drugs is a challenge. This study was carried out to adopt nanoemulsion as a means of entrapping ciprofloxacin in the oil phase of the emulsion for transdermal drug delivery. Nanoemulsions were formulated as oil in water (O/W) type and prepared by self-mild mechanical nanoemulsification method. The formulation consisted of Sandbox (Huracrepitan) and Sesame seed (Sesamumindicum) as the organic phase of the emulsion, Polyethylene (20) sorbitanmonooleate (Tween 80) and Polyethylene (20) sorbitanmonolaurate (Tween 20) as the surfactants and Polyehtylene glycol (PEG 400) as co-surfactant. The formulations were tested and characterized. Ciprofloxacin (0.075 g) was incorporated into the oil phase of the most stable nanoemulsion formulation prior emulsification and tested on Escherichia coli. Transdermal application was done on male Wister rats (R) followed by biopsification. The result showed the zones of inhibition of HCa3+Ciprofloxacin (Ciprofloxacin-loaded, Huracrpitan oil based nanoemulsion) and SSA3+Ciprofloxacin (Ciprofloxacin-loaded, Sesame oil based nanoemulsion) to be 26.00 and 25.00 mm respectively. The HPLC results showed that, out of 75000 µg of ciprofloxacin loaded in the oil phases of HCa3 and SSA3 formulations, 6.0076 (R2), 0.4112 (R3) and 6.7241 µg (R6) were absorbed in HCa3 while 1.9519 (R1), 1.2631 (R4) and 2.1801 µg (R5) were absorbed in SSA3. The SEM images revealed an encapsulation with globule size diameter of 94 and 63 nm respectively. The findings of this work showed that sandbox and Sesame seedoil based nanoemulsions are effective for transdermal drug delivery

Antidiarrhoeal Activities of Ethanolic Extract of Aristolochia ringens Stem Bark in Castor Oil-Induced Diarrhoeal Albino Rats

The antidiarrhoeal potentials of ethanolic extract of Aristolochia ringens stem back was evaluated in castor oil-induced diarrhoeal rats. The A. ringens stem back ethanolic extract was, in addition, screened for its phytoconstituents. Thirty albino rats of 150-180 g were randomized into six groups of five animals each for each of the three experiments and all administration were oral. Rats in groups I and II were administered 1.0 ml distilled water and 1% DMSO (Vehicle) respectively, while those in group III were administered 2.5 mg/kg b.wt loperamide hydrochloride as reference drug. Rats in groups IV, V and VI were administered 25, 50, and 100 mg/kg b.wt. ethanolic extract of A. ringens stem bark. The castor oil-induced diarrhoeal model was used, the weight and volume of the intestinal content was determined by enteropooling method and the intestinal motility was determined using activated charcoal method. The small intestine of the rats was also assessed for histopathological changes. The extract significantly and dose-dependently reduced the number of diarrhoeal faeces, the volume of intestinal accumulation and the distance moved by the fed charcoal in treated rats compared to the untreated diarrhoeal group (group II). The percentage inhibitions exhibited by the extract at 50 and 100 mg/kg body weight were significantly higher than that of the reference drug. Furthermore, the photomicrograph of the intestine of the extract treated rats showed intact intestinal architecture. Hence, ethanolic extract of Aristolochia ringens stem bark may contain phytochemicals with better antidiarrhoeal potentials which can be explored in the development of more viable antidiarrhoeal agents. Keywords: Aristolochia ringens, Antidiarrhoeal agents, Intestinal motility,  Intestinal accumulation

Development of oil-in-water (o/w) nanoemulsion formulations for spontaneous transdermal delivery of ciprofloxacin

Nanoemulsions have attracted attention in delivery of therapeutically active agents since most of the new chemical entities are hydrophobic in nature and the delivery of poor water soluble drugs is a challenge. This study was carried out to adopt nanoemulsion as a means of entrapping ciprofloxacin in the oil phase of the emulsion for transdermal drug delivery. Nanoemulsions were formulated as oil in water (O/W) type and prepared by self-mild mechanical nanoemulsification method. The formulation consisted of Sandbox (Huracrepitan) and Sesame seed (Sesamumindicum) as the organic phase of the emulsion, Polyethylene (20) sorbitanmonooleate (Tween 80) and Polyethylene (20) sorbitanmonolaurate (Tween 20) as the surfactants and Polyehtylene glycol (PEG 400) as co-surfactant. The formulations were tested and characterized. Ciprofloxacin (0.075 g) was incorporated into the oil phase of the most stable nanoemulsion formulation prior emulsification and tested on Escherichia coli. Transdermal application was done on male Wister rats (R) followed by biopsification. The result showed the zones of inhibition of HCa3+Ciprofloxacin (Ciprofloxacin-loaded, Huracrpitan oil based nanoemulsion) and SSA3+Ciprofloxacin (Ciprofloxacin-loaded, Sesame oil based nanoemulsion) to be 26.00 and 25.00 mm respectively. The HPLC results showed that, out of 75000 µg of ciprofloxacin loaded in the oil phases of HCa3 and SSA3 formulations, 6.0076 (R2), 0.4112 (R3) and 6.7241 µg (R6) were absorbed in HCa3 while 1.9519 (R1), 1.2631 (R4) and 2.1801 µg (R5) were absorbed in SSA3. The SEM images revealed an encapsulation with globule size diameter of 94 and 63 nm respectively. The findings of this work showed that sandbox and Sesame seedoil based nanoemulsions are effective for transdermal drug delivery

Phytochemical constituents and antidiarrhoeal effects of the aqueous extract of Terminalia superba leaves on Wistar rats

The aqueous extract of Terminalia superba leaves was subjected to phytochemical screening. Antidiarrhoeal property of the extract was determined at 50, 100 and 150 mg/kg body weight in castor oil-induced diarrhoeal Wistar rats. Phytochemical screening revealed the presence of saponins, cardenolides, triterpenes, flavonoids, steroids, phenolics and tannins, whereas alkaloids, anthraquinones and phlobatanins were not detected. The time of induction of diarrhoea was significantly (P < 0.05) prolonged at all the doses of the extract. The frequency of stooling and feacal parameters (total number of feaces and number of wet feaces), intestinal fluid accumulation (enteropooling) and the weight of intestinal content were significantly reduced. The data in the present study indicate that the aqueous extract of T. superba leaves possessed antidiarrhoeal properties. Key words: Phytochemicals, Terminalia superba, aqueous extract, diarrhoea, rats

Antidiarrheal activity of aqueous leaf extract of Ceratotheca sesamoides in rats

The antidiarrheal effects of the aqueous leaf extract of C. sesamoides at 25, 50 and 100 mg/kg body weight was evaluated in female rats using gastrointestinal transit, diarrhea and enteropooling induced by castor oil models. The extract was positive for alkaloids, saponins, flavonoids and phenolics. The 25 mg/kg body weight of the extract significantly (p<0.05) prolonged the onset time of diarrhea, decreased the fecal parameters (number, water content, fresh weight, total number of wet feaces) with no episode in the animals treated with 50 and 100 mg/kg body weight. The activity of small intestine Na+-K+ ATPase increased (p<0.05) while the nitric oxide, volume and mass of intestinal fluid as well as the distance travelled by the charcoal meal decreased. The patterns of changes were similar to the reference drugs. Overall, the antidiarrheal activity of the aqueous leaf extract of Ceratotheca sesamoides may be due to alkaloids, phenolics, flavonoids and saponins present in the extract

Evaluation of hypoglycemic and toxicological effects of leaf extracts of Morinda lucida in hyperglycemic albino rats

The aqueous and 50% methanolic extracts of leaf of Morinda lucida were investigated for their phytochemical constituents, hypoglycemic and toxicological effects in alloxan-induced hyperglycemia in rats. In addition, the possible acute toxicological effects of the extracts were also studied for seven days.The results revealed the presence of alkaloids, cardenolides, flavonoids, glycosides, saponins and steroids in the aqueous extract while 50% methanolic extract contained anthraquinones in addition to those found in aqueous extract. Phenolics and tannins were not detected in both extracts while anthraquinones was not detected in aqueous extract. The extracts significantly (P<0.05) lowered the blood glucose level in the alloxan-induced hyperglycemia in rats. However, the aqueous extract was more effective than the 50% methanolic extract, though they may possibly be toxic at the doses used because marker enzymes (ALP, AST and ALT) were secreted into the sera of these extracts-treated rats. The acute intra-peritoneal toxicity study of the extracts at the limit doses of 500-1500 mg/kg body weight revealed toxicity of the extracts, most especially at relatively high concentrations for seven days. Keywords: Leaf extracts, Morinda lucida, blood glucose level and toxicological effects