Background: Malaria is a serious global health problem affecting people in developing countries. The increasing resistance of plasmodium parasite to currently used antimalarial drugs has made the search for more efficacious drugs urgent.

Aim: To screen the methanol aerial parts extract and fractions of Vernonia cinerea for antiplasmodial activity in Plasmodium berghei infected mice.

Methods; Phytochemical evaluation and oral acute toxicity studies were carried out using standard protocols on both the extract and fractions of Vernonia cinerea. The suppressive, curative and prophylactic models were used to evaluate the antiplasmodial effect of the extract while curative model was used to evaluate fractions of Vernonia cinerea at doses of 250, 500 and 1000 mg/kg in Plasmodium berghei infected mice.

Results: There were presence of phytochemicals such as carbohydrates, flavonoids, saponins, tannins, alkaloids, steroids and triterpenes and cardiac glycosides in the extract and its fractions. The oral median lethal dose of the extract and fractions were estimated to be ˃ 5000 mg/kg. The extract produced a significant decrease in parasitaemia levels at p<0.05 when compared to negative control in the curative model. And, hexane fraction produced a dose dependent decrease in parasitaemia clearance than ethyl acetate, butanol and aqueous fractions.

Conclusions: This study suggests that methanol aerial parts extract of V. cinerea possess antiplasmodial activity that could be due to the phytoconstituents found present in the plant. The hexane fraction showed a better curative activity than other fractions.

The root of Entada africana L was extracted with methanol, ethyl acetate and hexane. The extracts obtained were then screened for antibacterial activity against six wound isolates; Staphylococcus aureus, Streptococcus pyogenes, Proteus mirabilis, Pseudomonas florescence, Klebsiella pneumonia and Escherichia coli. The results of this study showed that the methanol root extract of Entada africana produced the highest antibacterial activity, active on four out of the six organisms tested while that of hexane and ethyl acetate were only active on three organisms. Also, ethyl acetate extract produced a mild inhibition on P. florescence at 100mg/ml. The best inhibitory potential produced by the methanol extract was observed on S. aureus with minimum inhibitory concentration (MIC) value of 1.5 mg/ml, followed by Streptococcus pyogenes and Klebsiella pneumonia both with values of 6.25 mg/ml. Proteus mirabilis, P. florescence and E. coli were not inhibited by the methanol extract. The root of E. africana showed strong antibacterial property on some common wound infectious bacteria, thus justifies the traditional use of E. africana in the treatment of wounds and skin infections.

Development of drugs remain an incredibly important factor in human existence. While the world seems to face shortage of medicines because of increasingly new diseases, scientists in pharmaceutical industries and academic researchers are busy looking for new strategies of discovering and developing either entirely new drugs (new chemical entities) or new drugs from existing compounds.

This paper reviews how changing the route of administration of an already approved drug can be used to incrementally optimize an old drug, giving benefits like increased solubility and permeability, by-passing first pass effect, decreased cost, increased patient compliance to treatment, etc. Additionally, this paper summarizes the 505(b)(2) program which is the new drug application pathway for the approval of such new drug.

The approach employed in this review was studying information from literatures, company and government websites, and examples from official books.

Results show that although changing a drug’s route of administration is possible and encouraged, there are important tests for filing any modification in routes of administration, either clinical or non-clinical. Also presented are examples of drug products that have seen such changes.

In conclusion, incrementally modifying drugs through changing route of administration has been seen to potentiate the use and value of important medicines, and their importance in a large population of patients cannot be overemphasized.

This study aims to evaluate the potential of cross-linked Acacia seyal gum as a matrix former in sustained-release salbutamol sulphate tablet formulation prepared by direct compression method. Tablets were formulated with constant quantity of salbutamol sulphate (8 mg), while the matrix material varied between 30, 40 and 50 percent (%), resulting in formulations T1, T2 and T3 containing EG; T4, T5 and T6 containing CG and; T7, T8 and T9 containing Hydroxypropyl methylcellulose (HPMC). Tablets were evaluated for weight, diameter, thickness, friability, crushing strength, tensile strength, disintegration time, and drug content, all falling within acceptable B.P standards for sustained-release tablets with weight between 131 – 325 mg. Drug release was studied in 0.1 N HCl (pH 1.0) for 2 h then phosphate buffer (pH 6.8) for 6 h. Cumulative percent drug released calculated showed the time for 50 % drug release (T_50%) being longer for the CG matrices. Formulation T4 (30 % CG proportion) showed release of 78.78 % at the 8^th h, the closest to the theoretical release of 66.66 %. Based on this and the results of the statistical analysis of variance (p < 0.05), T4 was selected as the optimum formulation in this study to sustain the release of salbutamol sulphate for about 12 h. It is thus safe to conclude that cross-linked Acacia seyal gum can be used as an alternative matrix material for sustaining the release of water-soluble drugs.

Gardenia aqualla, commonly referred to as Gaude in Hausa has long been utilized in the traditional medicine in Nigeria for the treatment of various ailments and is popularly claimed to improve and treat sexual disorders in men and women, respectively. Despite its extensive use as aphrodisiac in Nigeria, there is no scientific evidence to justify this claim. Therefore, this study aimed to validate the aphrodisiac potential of the plant’s root extract and fractions in male rats. The root was clean, shed dried and size reduced. It was cool macerated with methanol (70%) and partitioned with n- hexane and ethyl acetate respectively. LD₅₀ was carried out according to OECD guideline. The animals were randomly divided into four groups of five rats each. Group one (control) received 1 ml/kg distilled water while groups two, three and four received 250 mg/kg, 500 mg/kg and 1000 mg/kg of the methanol (70%) extract daily for 21 days, respectively. The same were done for hexane, ethyl acetate and residual aqueous fractions. The mating behaviour, libido and potency were determined and compared with control. The female rats that participated in mating were made receptive by hormonal treatment. Results showed that oral administration of the extract and fractions caused significant increase in the mounting frequency (MF), intromission frequency (IF), ejaculation latency (EL), Erections, quick flips, long flips as well as aggregate of penile reflexes (P < 0.05) and caused significant reduction in the mounting latency (ML), intromission latency (IL) and post ejaculatory interval (PEI) (P < 0.05). There was also a significant dose-dependent increase in serum testosterone, luteinizing hormones (LH) and follicle stimulating hormones (FSH) concentrations in all the groups (P < 0.05). In conclusion, the results of the studies indicated that the extracts of Gardenia aqualla root has aphrodisiac activities and this may support the claims for its traditional usage as aphrodisiac.

This research studied effects of chronoefficacy of alpha-lipoic acid/glimepiride/nifedipine therapy in attenuating oxidative stress and histological changes in pancreas of diabetic rats. A group of normal and another group of diabetic rats treated with distilled water 1 mL/kg respectively represented controls. All the rats in the other groups were positive for diabetes and all received 10 mg/kg glimepiride at night-time (2000h). The last four groups also received 20 mg/kg nifedipine at morning-time (0800h) while the last three groups also received additional 100 mg/kg alpha-lipoic acid (ALA) at circadian time of 0800h, 1400h and 2000h respectively. During the 28 days oral treatment, body weight was measured weekly. On the 29^th day, the rats were euthanized and the pancreas was excised and divided into two parts. Either part was preserved in phosphate buffer or formalin for antioxidant assay and histology respectively. There was a significant (p ˂ 0.01) increase in weekly weight in rats receiving night-time dosing of ALA. Malondialdehyde level for this group was significantly (p ˂ 0.01) lower than the diabetic group and other time points. Also, catalase and superoxide dismutase values were significantly (p ˂ 0.01) lower than that of the diabetic control. Furthermore, histological photomicrograph for this group showed features similar to the normal control. Time dependent alpha-lipoic acid as an adjunctive therapy in combination with glimepiride and nifedipine attenuates oxidative stress and histological changes in pancreas. This combination if explored and studied in man may serve as a clinical tool for slowing or preventing diabetic complications.

Aim: The design of plastic films imbued with some self-disinfection property would be an advantage in reducing environmental pollution and the spread of diseases. This study aimed at investigating the suitability of antioxidants-rich Aspalathus linearis (Rooibos tea) extracts for synthesis of silver nanoparticles with suitable physical properties for incorporation into a plastic matrix, in order to create a self-disinfecting film. Methods: Rooibos tea was extracted with methanol and antioxidants-rich fractions were identified by 1, 1-diphenyl-2-picryl-hydrazyl (DPPH) antioxidant assay, and then used in reduction of silver nitrate to prepare silver nanoparticles. The nanoparticles were characterized by photon correlation spectroscopy and atomic force microscopy, and their antimicrobial activities were tested in vitro against Staphylococcus aureus (S. aureus), Bacillus subtilis (B. Subtilis), Salmonella typhi (S. typhi) and Escherichia. Coli (E. coli). The most bioactive formula was incorporated into polymethylmethacrylate before polymerization. The self-disinfecting activities of the composites were tested in vitro using S. aureus and E coli. Results: The fractions gave high antioxidant activities and the reduction of silver nitrate resulted in silver nanoparticles of very low polydispersity values (<0.3) and excellent antimicrobial activities (except with Candida albicans).  The optimized film (containing 4ml of the nanosolution) inhibited microbial growth for up to 48 hrs after exposure to air for 60-90 min, whereas heavy microbial growth occurred in the control sample. Conclusion: Being edible and non-toxic, Rooibos can be used in synthesizing nanosilver with properties suitable for creating new designs of self-disinfecting plastic matrices.

Malaria is one of the most lethal tropical diseases in Africa affecting millions of people yearly. Malaria is associated with oxidative stress which has been implicated in malaria-induced anemia and other pathological changes in the body. This present study investigated the antioxidant activity of the ethyl acetate, butanol and residual aqueous fractions of Uapaca togoensis stem bark in Plasmodium berghei infected mice. Phytochemical screening and acute toxicity studies of the fractions of Uapaca togoensis stem bark was carried out using standard protocols. Effect of fractions on free radical scavenging activity and oxidative stress induced by Plasmodium berghei infection in the plasma of parasitized animals was also investigated. Flavonoids, triterpenes, glycosides, alkaloids and tannins were found present in all the fractions. Oral median lethal dose of the fractions was estimated to be greater than 5000 mg/kg. For the DPPH radical scavenging assay, IC₅₀ values obtained were 0.04 mg/mL, 0.313 mg/mL, 0.58 mg/mL and 2.30 mg/mL for ethyl acetate, butanol, residual aqueous fractions and vitamin C respectively.  At doses of 250, 500 and 1000 mg/kg, the butanol and residual aqueous fractions significantly reversed the effects of the oxidative stress. This was shown by the significant (p<0.05) reduction in MDA levels with a corresponding elevation in SOD, GSH and CAT levels. The findings from this study suggests that the antioxidant effects of the fractions might be an added advantage to it antimalarial activity.