Formulation and Evaluation of Antimicrobial Activities of Herbal Cream Containing Ethanolic Extracts of Azadirachta indica Leaves and Aloe Vera Gel
Pages 137-142
Chukwuemeka Paul Azubuike, Sandra Ebele Ejimba, Abel Olusola Idowuand Issac Adeleke
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.02.6
Published: 12 May 2015

Abstract: The antimicrobial activity of ethanolic extract of dried leaves of Azadirachta indica (Neem), fresh gel of Aloe vera, combination of the two extracts and the creams formulated with these extracts were evaluated.

The preliminary in vitro antimicrobial activity of the extracts at various concentrations and those of their creams were determined against some microorganisms using the agar cup plate method. The growth inhibition zones of the extracts on the microorganisms were noted. The minimum inhibitory concentration (MIC) was also determined by agar dilution method. The physical properties of the creams formulated with these extracts were evaluated using standard procedures.

Gram positive bacteria were more susceptible to Neem extract of which Staphylococcus aureus was the most susceptible with the lowest MIC value (2.5mg/ml). The fungal strain Candida albicans had the lowest MIC value (2.0mg/ml) for the Aloe vera gel extract. The MIC values (mg/ml) of Neem leaves against Bacillus subtilis, Escherichia coli, Staphylococcus aureus, Pseudomonas aeroginosa, Candida albicans and Aspergillus niger were 5.00, 5.00, 2.50, 10.00, 2.50, 5.00 respectively, while MIC of Aloe extract were 8.00, 8.00, 4.00, 8.00, 2.00, 4.00 respectively. Among the formulated creams, the formulation containing equal concentrations of the extracts (1:1) showed the highest antimicrobial activity, however the commercial brand Funbact A^® had better antimicrobial activity. Most of the creams showed comparable physical properties.

The study showed that the creams containing equal concentrations of the two ethanolic extracts have high potentials as topical antimicrobial agents especially against skin infections due to the tested Gram positive bacteria and Candida albicans.

Keywords: Azadirachta indica, Aloe vera, Antimicrobial activity, Herbal Creams.

Development and Evaluation of Controlled Release Bilayer Tablets of Hydrochlorothiazide and Losartan Potassium
Pages 84-94
Manoj Kumar Mishra, Dubey Deepti and Upamanyu Neeraj
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.01.13
Published: 16 February 2015

Abstract: The aim of the present research work was to develop bilayer tablet dosage form containing combination of immediate and sustained matrix prepared from Hydrochlorothiazide (HTZ) and Losartan Potassium (LP) respectively for the treatment of hypertension and its associated complications. Immediate release HTZ was prepared using different superdisintegrants. LP sustained layer was prepared by compression technique. Both pre-compression and post-compression parameters were analyzed for all the tablets. In vitro release studies were carried out as per USP in pH (1.2) and phosphate buffer pH (6.8) using USP-XXI type II. Bilayer tablet (F6) formulated using higher concentration of HPMC K 15 exhibiting higher LP release rate (83.553± 0.22) for the period of 12 h. The In vitro release profile of drug from sustained matrix could be best expressed by First order as the plot showed highest linearity (R² = 0.990) and diffusion was the dominating mechanism of drug release. The stability and FTIR studies are also indicating the absence of strong interaction between drug and polymer and compatibility among them.

In Vitro Activity of Cocoa Powder Extracts on Some Biomarkers Implicated in P. falciparum Malaria Pathogenesis
Pages 38-42
Seth Kwabena Amponsah and Nana Nim Dwumfour
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.01.6
Published: 16 February 2015

Abstract: Malaria is a public health concern in many developing countries, including Ghana, and efforts are being made to eradicate it. Extracts from natural products have been used in several malaria endemic areas for malaria prophylaxis and treatment. Natural cocoa powder has been reported to possess in vitro direct inhibitory on P. falciparum. This study investigated the effect of natural cocoa powder on inducible nitric oxide, TNF-α and IL-10, biomarkers that play different roles in malaria pathogenesis. Chloroform and ethylacetate fractions of cocoa powder were cultured together with phytohemagglutinin-stimulated peripheral blood mononuclear cells (PBMCs) for 24 hours at 37°C with 5% CO₂. Cell free supernatants were harvested and assayed for iNO, TNF-α and IL-10. Inducible NO was determined by diazotization reaction developed by Griess. TNF-α and IL-10 were determined by ELISA. This study showed that TNF-α and iNO in phytohemagglutinin-stimulated PBMCs were significantly reduced by cocoa fractions (p < 0.05), but IL-10 levels did not change significantly (p > 0.05), although TNF-α is known to up-regulate IL-10.Apart from the documented direct inhibitory effect of cocoa powder on P. falciparum, it can be hypothesized that the antiplasmodial activity of unsweetened cocoa powder could also be due to its ability to significantly inhibit iNO and TNF-α, inflammatory substances implicated in severe malaria pathogenesis.

In Silico Design & Development of Some Selected Flavonols Against Beta–Glucuronidase Inhibitory Activity 
Pages 43-49
Sovan Pattanaik, Sudam Chandra Si, Sudhanshu Sekhar Rout, Anindya Bose and Siva Shankar Nayak
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.01.7
Published: 16 February 2015

Abstract: Drug discovery process develops faster due to more advances in computational techniques. The protein ligand interaction well predicted due to the in-silico approach study. The present investigation focused towards the development of lead structure for treatment of hepatic disorders. An increase in serum acid hydrolase, including β-glucuronidase has been reported in numbers of pathological conditions such as arthritis, renal diseases and epilepsies. Enhancement of this enzyme β–glucuronidase in blood has been found to correlate significantly with liver damage. β-glucuronidase inhibitor is a novel approach which is different from the available hepatoprotective drug therapies.

Method: The current study is based on in-silico ligand screening and in-vitro estimation of the three flavonols [Naringenin, Quercetin and 2-(3, 4-Dihydroxy Phenyl)-7-Hydroxy-3-(2-Hydroxy Ethoxy) 4-H-Chromen-4one] compounds with enzyme β-glucuronidase. Molecular docking software Py Rex and Py Mol was used to dock the selected ligand in the binding site of the crystal structure of protein.

Results: Docking results are based on the least binding energy of the selected flavonols compounds. Further attempt has been made towards in-vitro estimation of this enzyme with those selected compounds. The binding affinity with existence of hydrogen bonds leads to find out the mechanism which was well correlated with the findings of in-vitro inhibitory activity.

Conclusion: The result outcome of the binding orientation of 2-(3, 4-Dihydroxy Phenyl)-7-Hydroxy-3-(2-Hydroxy Ethoxy) 4-H-Chromen-4one linked with the active amino acid residue of the protein and the binding affinity leads to find out the mechanism for its potential in-vitro inhibitory activity.

Bioactive Metabolites from Indigenous Actinomycetes Isolated from Marine Water 
Pages 57-63
Syed Abdus Subhan, Abdul Wahab, Talat Yasmeen Mujahid,Tanveer Abbas, Nayyar Mehmood and Iqra Ahmed
DOI: http://dx.doi.org/10.6000/1927-5951.2015.05.01.9
Published: 16 February 2015

Abstract: Microbial natural products have continued to play an important role in the discovery of novel chemicals for the development of important therapeutic agents. Actinomycetes form a potent reservoir of biologically active secondary metabolites and enzymes. The need for finding novel bioactive compounds for the development of new therapeutic agents is required due to the emergence of antibiotic resistance among pathogenic bacteria. Actinomycetes are considered as one of the best producers of variety of antagonistic compounds that could serve as potential chemotherapeutic agents. The present study was undertaken to find new antagonistic compounds from actinomycetes. Actinomycetes were successfully isolated from marine water samples collected at various locations of Karachi. Initially 39 isolates were collected out of which 23 were found to produce active metabolites against one or more test bacterial cultures. Actinomycetes strains IS26, IS33, and IS39 showed significant potential of having bioactive metabolites. Further, the spectrum of those strains was tested against gram positive and gram negative bacteria and results showed variable potential of actinomycetes to inhibit bacterial growth.