IRJP-VOLUME 01 ISSUE 02 NOVEMBER 2011


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International Research Journal of Pharmaceuticals      ISSN 2048-4143 
Volume 01 No.02 November 2011 (42-71)     

Title

07) Preparation and Characterization of Nanoparticles for Solubility and Dissolution Rate Enhancement of Meloxicam (pp. 42-49).

Author(s)

Amit J. Raval and Madhabahi M. Patel


Abstract

The aim of the present work was to enhance dissolution of poorly water-soluble meloxicam by preparing stable nanoparticles. Meloxicam nanoparticles were produced by combining antisolvent precipitation and high pressure homogenization approaches in presence of selected stabilizers and converting into dry powders by spray-drying. The physicochemical properties of drug and its nanoparticles were characterized by SEM, XRD, FT-IR, DSC as well as measuring the particle size and in-vitro drug dissolution.  The DSC and XRD results indicated that the antisolvent precipitation process led to the amorphization of meloxicam. An increase in the stability of the nanoparticles was also assured by the sufficient adsorption of the stabilizers onto the drug surface. Meloxicam nanoparticles increased the saturation solubility of drug almost fourfold. The in vitro studies at Q5min  showed a marked increase in the drug release from just 7% (raw drug) to 82% (Meloxicam nanoparticles). The combining of both the methods was a promising method to produce uniform and stable nanoparticles of meloxicam with remarkable improvement in dissolution rate due to an increased solubility by the effect of increased surface area and change to amorphous form of the drug. 


Title

08) Structure-Based Design of PDHK2 Inhibitors from Docking Studies (pp.50-58).

Author(s)

Rita Kakkar


Abstract

The binding site of dichloroacetate (DCA) in PDHK2 has been examined in detail. As pyruvate is known to bind at the same site, it has been docked at that site and the interactions responsible for its binding are examined. DCA is found to bind more strongly than pyruvate but because of toxicity it is not suitable as a drug. According to this point of view, a virtual library of small drug-like molecules is created and various structural, electronic and topological parameters calculated for the ligands correlated with various scoring parameters. Similar calculations are done with molecules similar to pyruvate and DCA. of a total of around 2000 molecules screened this way, a few have been short-listed, based on their strong binding affinity to PDHK2 and the absence of any serious ADME issues. They have been tested for inhibitor activity and found to be more potent than DCA.


Title

09) In-Vitro antibacterial activity of Aloe Barbadensis Miller (Aloe Vera) (pp.59-64).

Author(s)

Saba Irshad, Muneeba Butt and Hira Younus


Abstract

Medicinal plants play an important role for health care. Medicinal plants have ability to cure both infectious and non-infectious diseases. According to an estimate about 25% of medicines are derived from plants. The objective of the present study was to evaluate the antibacterial activity of Aloe barbadensis Miller (Aloe Vera) by using agar diffusion assay and gel filtration chromatography. The bacterial strains used in this research work were Escherichia coli, Bacillus subtilius, Salmonella typhi, Pseudomonas, Klebsiella pneumoniae, Staphylococcus epidermidis. Aloe Vera plant leaves and gel were macerated in different organic solvents including ethanol, methanol and distilled water. Then, by using agar diffusion assay antibacterial activity was estimated. The zones of inhibition were measured by scaling and represented by tables and graphs. The Aloe Vera extract of Methanol showed the maximum antibacterial activity as compared to other solvent extracts. Then, distilled water macerated form of Aloe Vera leaves were used for gel filtration chromatography technique in order to determine the fraction containing the active components. Fraction 8 showed maximum antibacterial activity against all above mentioned bacterial strains. This study reveals the plausibility of the presence of some bioactive components in Aloe Vera. The further investigation on crude extracts would characterize bioactive components of Aloe Vera which would be done by using High-performance liquid chromatography (HPLC).


Title

10) Novel Anti-Acne Drug Delivery System of Tretinoin (pp. 65-71).

Author(s)

Dr. Rakesh P. Patel, Kaushal P. Patel, Kushal A. Modi and Chirayu J. Pathak


Abstract

The objective of the present study was to formulate and evaluate Tretinoin niosomal gel and to carry out comparative skin irritation study with conventional Tretinoin solution and Tretinoin conventional gel. Topical Tretinoin (0.25%, 0.05%) has been a reliable treatment of acne vulgaris since 25 years but its major drawback is that it causes skin erythema on the applied area. The niosomal dispersion was prepared using different grades of non-ionic surfactants and cholesterol in different ratios along with Tretinoin. The transmission electron microscopy revealed that the niosome vesicles were of LUV type and polyhedral shape. The niosome vesicles prepared with SPAN™ 60 and cholesterol (20:1) showed maximum entrapment efficiency (53.77±1.57%) and minimum vesicle diameter (1.55±0.13 µm). The prepared niosome vesicles were incorporated into Carbopol® 971 gel base to prepare Tretinoin niosomal gel (0.05%). The stability study was carried out at different accelerated and non-accelerated conditions. The In-vitro diffusion study carried out using sigma dialysis membrane showed sustained release pattern of Tretinoin from niosomal gel. The comparative skin irritation study carried out on 18 healthy wistar rats of either sex showed remarkable decrease in signs of skin erythema, lesions and scaling caused by Tretinoin.