Volume 7

January-March 2015

Review Articles

C V Pardeshi, Y H Vanjari, A D Kulkarni

Now a day, nasal drug delivery has occupied an important place in the field of drug delivery technology. A range of medicaments can be successfully delivered at the site of action using drug delivery devices. A successful nasal drug delivery device seems to deliver medication efficiently, necessarily non-invasive, helps in rapid onset of action, patient friendly for self administration and should exhibit minimal side effects. Since constructing an efficient drug delivery device, capable of achieving sufficient local, systemic or brain distribution of drug is a challenge, usually requires a robust and innovative technology. Fortunately, the nose offers easy access to a large mucosal surface, well suited for delivery of many therapeutics including proteins and peptides. Present review deals with such novel nasal drug delivery devices, more specifically, OptiNose, ViaNase, Direct Haler, MAD-nasal TM mucosal atomizer, which have proven their proficiency in delivering medications. The clinical status of the therapeutics administered by these devices along with their regulatory requirements has also been extended.

Keywords: Nasal Drug Delivery, Drug Delivery Devices, OptiNose, ViaNase, Direct Haler , MAD-nasal TM Mucosal Atomizer.

Sahani Vandana, Bhatt Ganesh, Kothiyal Preeti

Cirrhosis is one of the chronic generalised disease and has a variety of clinical manifestations and complications some of which can be a life threatening. This results in decrease in hepatocellular mass and thus functions. It is 12th leading cause of death in United States. Hepatic stellate cells (HSC) plays a crucial role in the development of liver fibrosis because of their prominent role in extracellular matrix production, regulation of vascular tone, and production of inflammatory mediators such as transforming growth factor-b (TGF-b) and platelet-derived growth factor (PDGF). Therefore, these cells are major target for the treatment of Cirrhosis. Anti-fibrotic drugs are not efficiently taken up by HSC or may produce unwanted side-effects outside the liver. Cell-specific delivery can provide a solution to these problems, but a specific drug carrier for HSC has not been described until now. The mannose 6-phosphate/insulin-like growth factor II (M6P/IGF-II) receptor, which is expressed in particular upon HSC during fibrosis, may serve as a target-receptor for a potential carrier. The primary aim of drug targeting is to manipulate the whole body distribution of drugs, that is, to prevent distribution to non-target cells and concomitantly increase the drug concentration at the targeted site. Carrier molecules are designed for their selective cellular uptake, taking advantage of specific receptors or binding sites present on the surface membrane of the target cell.

Keywords: Liver, Cirrhosis, Hepatic Stellate Cells Targeting.

Juyal Divya, Dhyani Archana

Liver is a vital organ of the human body. It plays an important role in the human body. Acetaminophen when taken in therapeutic doses, it is used in the treatment of various conditions. Hepatotoxicity is the prime factor responsible for drug withdrawal from the market. There is no doubt that hepatotoxicity requires considerable attention and that every viable measure be taken towards an efficient mechanism for hepatoprotection. The overdose of acetaminophen causes acute liver failure. The hepatotoxicity can be treated by targeting the liver by the various carriers like liposomes, nanoparicles, phytosomes etc. However the hepatoprotective therapies require better targeting, stability and better bioavailability. Such focus areas can be effectively met with the aid of lipid based delivery systems which can prove to be a breakthrough in the field of hepatoprotection.

Keywords: Hepatotoxicity, Acetaminophen, Acute Liver Failure.

Research Articles

Shete Amol, Patil Vishal, Yadav Adhikrao, Sakhare Sfurti, Shirke Supriya

The objectives of present investigation were to design and evaluate stable, delayed Controlled release formulation of zileuton, which may provide peak plasma concentration early morning and compare with marketed formulation available in USA under the brand name of “Zyflo® CR”. The matrix coated and bialyer tablets, were prepared by wet granulation technology and some critical processing parameters were studied like in granulation time and extent of granulation. Loss on drying of the granules, coating pan speed, inlet temperature, bed temperature, Distance between spray gun and product bed. The prepared tablets were evaluated for official evaluation parameters and effect of speed of agitation and Ph of dissolution media were studied. ZIB/03 showed the same dissolution profile that of the innovator at pH 6.8 and 7.2 tris buffer but, compare to innovator at pH 1.2 and 4.5 acetate buffer it showed dissolution dissimilarity. One month accelerated stability study of the batch no. ZIB/03 showed a slightly faster release than the initial. Developing delayed and controlled release formulation of zileuton might provide peak plasma concentration in the early morning. So it could be said that a superior formulation than currently marketed formulation (Zyflo CR) was achieved.

Keywords: Delayed Release, Controlled Release, Chronopharmaceutics, Zileuton, Bilayer Tablet.

U Salmanul Faris, O M Fasalu Rahiman, Shejina M, Mohthash Musambil

Today a number of research works are carried out in production of enzymes from an isolated organism, and evaluating its effect on animal studies. L-Asparaginase is now known to be a potent antineoplastic agent in animals and has given complete remission in some human leukemia’s. Extensive clinical trials of this enzyme, however, were not possible in the past because of inadequate production. Strain improvement of organisms is one alternative method that can be implemented to tackle this problem. Strain improvement can enhance the production, and increase the activity of enzymes produced. L-asparaginases are found to be responsible for catalyzing the deamination of Asparagines to yield Aspartic acid and an ammonium ion, resulting in depletion of free circulatory Asparagines in plasma. Its use in therapeutics is found to be remarkable, especially for those specific cases where blood cells become cancerous, such as in acute lymphoblastic leukemia. The commercial availability of L-asparaginase has revolutionized the molecular therapy of acute lymphocytic leukemias and melanosarcoma. Therefore, highly purified and effective Asparaginase is of great importance for today’s practical interests. The present study deals with successful isolation and purification of L-asparaginase enzyme from Aspergillus niger by solid state fermentation. L-asparaginase produced was purified and characterized. The anticerous activity of the enzyme was studied on human cancer cell line by MTT Assay method and the results showed clear positive results

Keywords: Anticancerous Enzyme, L-asparaginase, MTT Assay, Aspergillus niger, Solid State Fermentation.

Rakhi Negi, Laxmi Goswami, Preeti Kothiyal

The main aim of the current study was to formulate and evaluate microballoons for Telmisartan which is having poor bioavailability. Telmisartan belongs to class II according to BCS classification of drugs, i.e. low solubility and high permeability. The Microballoons for Telmisartan were prepared by emulsion solvent evaporation method using different polymers and their ratios. The polymers include ethyl cellulose and HPMC. The obtained microballoons formulations were evaluated for percentage yield, particle size, buoyancy, drug content in-vitro release studies. The bioavailability of Telmisartan can be increased by formulating it as gastroretentive drug delivery i.e. microballoons. Formulation F4 shows good results with 73.7 % obtained yield, 65.932 % drug content and 75.169 % buoyancy. Microballoons prepared were spherical in size with smooth surfaces concluding it to be optimized formulations.

Keywords: Telmisartan, Emulsion Solvent Evaporation, Buoyancy, Floating Drug Delivery, Gastro Retention.

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