Volume 9

April-June 2017

Review Articles

Saripilli Rajeswari, Satyajith Panda, Ranjith Prasad Swain, Vinusha Goka, Tella Prasanthi

Colon specific drug delivery has gained increased importance not just for delivery of drug for the treatment of local diseases, associated with the colon but also potential site for systemic delivery of therapeutic drug. Treatment could be more effective if it is possible for drug to be directly delivered to colon. This article gives an overview on anatomy and physiology of the colon and approaches utilized for colon specific drug delivery. This article also discusses advantages and limitations of the different approaches and also deals with the microsphere, various methods used for preparations of microspheres and advantages and disadvantages of microspheres.

Keywords: Microspheres, Controlled Release, Novel Drug Delivery, Approaches of Colon Targeting.

Research Articles

Dinesh M Morkhade, Vishwanath S Nande, Siddheshwar B Joshi

In this study, a novel crystalline form of ibuprofen (IBF) was prepared using glycerol as a medium and PEGylated rosin derivative as a crystal-habit modifier. The crystals were characterized for morphology, particle size and melting point. FT-IR spectroscopy was performed to examine the difference in peak characteristics of IBF and its novel crystalline form (IBF-glycerol). Tablets were prepared by the wet granulation method and characterized for pharmacotechnical properties. Dissolution study of IBF, IBF-glycerol and their tablets was performed in distilled water. IBF and IBF-glycerol exhibited rod and rhombic shape crystals, respectively. FT-IR spectra revealed slight differences in absorption peaks of IBF and IBF-glycerol. The colour and IR spectra of IBF and IBF-glycerol did not differ significantly. The particle size of IBF-glycerol was smaller (5-10 µm) compared to IBF (15-35 µm). Melting point of IBF and IBF-glycerol was in the range of 74-76°C and 65-68°C, respectively. The drug release from IBF and IBF-glycerol powders at the end of 600 min was 52.13% and 69.22%, respectively. Tablets could release 47.72% IBF and 58.21% IBF-glycerol at the end of 600 min. Drug release from all the tablets followed first order kinetics. Results revealed that glycerol and PRD could produce the novel rhombic crystals of IBF having lower particle size, melting temperature and markedly faster dissolution than native IBF.

Keywords: Ibuprofen, Glycerol, Novel Crystalline Form, Tablets, Release Kinetics.

Akpa P A, Kenechukwu F C, Adikwu M U, Okore V C

This aim of this study was to produce pharmaceutical grade microfine cellulose from alpha- cellulose derived from saw dust of the tropical tree Gmelina arborea, using trona (sodium sesquicarbonate), a known depolymerization agent, evaluate the physicochemical properties of the resulting cellulose and develop meltextrusion matrices containing acetaminophen using the cellulose. Alpha–cellulose was extracted from sawdust and treated with various concentrations of trona (0.1, 1, 2, 5, 10, 15 and 20 %) to produce tronated microfine cellulose – TMFC. The physicochemical properties of TMFC was determined and compared with Avicel PH 101 (Microcrystalline cellulose, MCC), a standard cellulose. TMFC was then used to prepare melt-extrusion matrices of acetaminophen. Some physicochemical properties of the matrices were determined. Drug dissolution from the meltextrusion matrices was evaluated in 0.1N HCl (pH 1.2). Results indicate that the physicochemical properties of the α–cellulose were comparable to MCC. Rf values revealed no drug-excipient incompatibility between acetaminophen and TMFC. The physicochemical tests on TMFC showed that these matrices are of sufficiently high mechanical strength and that they had relatively high uniformity in both weight and dimensions. Release studies showed that although TMFC compared favorably with MCC, TCMC slightly increased cumulative drug released from the matrices compared with non-tronated cellulose and achieved sustained release of acetaminophen in the stomach environment (pH 1.2). This study has shown that TMFC prepared from sawdust Gmelina arborea could be used along with paraffin wax in the development of melt-extrusion matrices which could be employed to achieve sustained and targeted delivery of acetaminophen in the stomach.

Keywords: Gmelina arborea, Acetaminophen, Sustained Delivery, Tronation, Saw dust, Cellulose.

Hitendra Mahajan, Shamshad Beldar

Rutin-flavonoid-polyphenolic has gained attention in prevention of brain cancer. The low permeability of Rutin (RU) across the blood-brain-barrier (BBB) leads to its insufficient delivery which in turns result in low therapeutic index. Therefore, developing a novel approaches enhancing the CNS delivery of RU are required for the treatment of Cancer. The aim of this research work was to develop in Nanoemulsion (NE) loaded with RU, for CNS targeting. Rutin is a poorly water soluble anticancer drug, with oral bioavailability is about 4%. Nanoemulsion were fabricated by Spontaneous Emulsification technique. Ethyl oleate was used as oil. Tween 80 was employed as surfactant and Polyethylene glycol 400 was employed as co-surfactant. Optimised RU-NEs (F7) had particle size of 228.60 nm and % drug content of 94.77 %. Finally characterized for different parameters. Differential Scanning Calorimetry and Transmission Electron Microscopy (TEM) study revealed that RU was completely homogenies in Nanoemulsion. Then the formulation were subjected to in vitro, ex vivo and in vitro cytotoxicity using (U373MG) cell line and Histopathological studies. IC50 value was obtained 9.8 µg/mL of RU-NE and it did not show any toxicity and so were safe for intranasal delivery for brain targeting. In-vitro diffusion studies revealed that RU loaded NE had a significantly higher release compared to plain drug suspension (PDS). From stability study, it was found that MDS, PDI, zeta potential and % DR was not significantly changed during the period of three months at 25±2°C and 60±5% RH. So, RU loaded Nanoemulsion for intranasal delivery are considered as promising vehicle for its targeting to CNS to treat the brain cancer. RU-NE was a dramatically enhanced anticancer and antiangiogenic activities.

Keywords: Intranasal Delivery, Nanoemulsion, Brain Targeting, Spontaneous Emulsification Technique.

Prashith Kekuda T R, Onkarappa R

Production of secondary metabolites by microorganisms is highly influenced by the nutritional and cultural conditions. The objective of the present study was to study the effect of nutritional and cultural conditions on the production of antibacterial metabolite by Streptomyces variabilis strain PO-178 isolated from Western Ghat soil of Agumbe, Karnataka, India. Starch casein nitrate broth was found to be the best medium for production of antibacterial agents by strain PO-178. The temperature 45°C and pH 9 was shown to be optimum for production of bioactive metabolites. Starch and casein was found to be best carbon and nitrogen source respectively. Increasing starch concentration resulted in better production of antibacterial agents. Sodium chloride at concentration 2% influenced maximum production of bioactive agents. The presence of all trace salts was required for better production of antibacterial agents. It is clear from the study that the production of bioactive agents by strain PO-178 is influenced by several nutritional and cultural conditions. Further, statistical approaches can be conducted to obtain the possible combinations of these conditions for better production of antibacterial agents.

Keywords: Streptomyces variabilis, Nutritional, Cultural, Agar Well Diffusion.

Okechukwu D C, Kenechukwu F C, Obakpolo L O

The aim of this study was to evaluate the in vitro antimicrobial interaction between the ethanol leaf extract of Moringa oleifera (MO) which is used habitually in Nigeria as a dietery supplement and tetracycline (T). Preliminary antimicrobial sensitivity screening of the extract was carried out using the agar dilution method. The minimum inhibitory concentration (MIC) of the ethanol extract of Moringa oleifera and tetracycline were determined in vitro using the agar dilution method. The antimicrobial interaction was evaluated by the checkerboard technique using Staphylococcus aureus and Pseudomonas aeruginosa. The MICs of the ethanol extract of Moringa oleifera leaf against Staphylococcus aureus and Pseudomonas aeruginosa were evaluated to be 25.0 and 50.0 mg/mL respectively while that of tetracycline was calculated to be 0.0005 and 0.016 µg/mL against Staphylococcus aureus and Pseudomonas aeruginosa respectively. Upon combination, synergism was manifested serially against Staphylococcus aureus in ratios of 9 (T):1(MO) down to 5(T):5(MO) after which additivity was manifested as the ratio of MO increased in the combination. Against Pseudomonas aeruginosa, the combined interaction showed a somewhat irregular pattern of effect, including addtivity at T:MO ratios of 9:1 and 8:2, and synergism at T:MO ratio of 7:3. Other combination ratios had no MIC, hence no observed effect. The combined antimicrobial effect of the interaction between ethanol extract of Moringa oleifera leaf and tetracycline was predominantly synergistic against Staphylococcus aureus.

Keywords: Moringa oleifera leaf, Antibacterial interaction, Checkerboard technique, Staphylococcus aureus, Pseudomonas aeruginosa, Tetracycline.

Chinmaya Keshari Sahoo, Surepalli Ram Mohan Rao, Muvvala Sudhakar

The present work was aimed to develop controlled porosity osmotic pump tablets of stavudine. Wet granulation technique was adopted for the preparation of all these formulations. Conventional spray coating pan was used to develop coating upon core tablets by using cellulose acetate as wall forming material and sorbitol as pore former. The developed tablets were evaluated for pre compression parameters, post compression parameters, in vitro drug release study, Fourier Transform Infrared Spectroscopy (FTIR) study, Differential Scanning Calorimetry (DSC) study and scanning electron microscopy (SEM) study. The formulation variables such as effect of osmogen concentration, effect of pore former concentration, effect of membrane thickness of semi permeable membrane were evaluated for drug release characteristics. For the optimized formulation effect of osmotic pressure, effect of pH and effect of agitation intensity was evaluated. The in vitro release kinetics were analyzed for different batches by different pharmacokinetic models such as zero order, first order, Higuchi, Korsmeyer Peppas and Hixson Crowell model. The optimized formulation was found to be stable up to 3 months when tested for stability study at 40±2°C/ 75±5% RH.

Keywords: CPOP, Wet Granulation, In Vitro Drug Release, Stability Study.

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