JOURNAL OF DRUG DELIVERY AND THERAPEUTICS

5-10

Authors: Anand Sagar, Vandana Chauhan, Ved Prakash

Anand Sagar, Vandana Chauhan, Ved Prakash

18-28

Authors: Ahmet Akici, Mehmet Murat Kilboz, Mevhibe Tamirci, Volkan Aydin, Salih Mollahaliloglu, Senay Ozgulcu, Ali Alkan

Introduction: Physicians’ perspectives are essential for rational use of medicine (RUM) activities. This study aimed at evaluation of physicians’ attitudes and experiences about therapeutical management process in terms of RUM in primary and secondary care. Methods: A survey was applied to 1062 family physicians (FP) and 562 specialist physicians (SP) in Turkey. The questionnaire consisted of items assessing physicians’ RUM approaches, stratified by their demographic and occupational characteristics. Results: A total of 55.4% of FPs and 32.1% of SPs declared that they prescribed to “>80% of their patients”. The attitude of “no prescribing without physical examination” was more in females, in seniors, and in those with longer professional experiences in SP group (p<0.05), where no difference was found among FPs. More markedly in FPs, women provided more information than men about their patients’ diseases and pharmacological/non-pharmacological treatments. Most commonly demanded drugs by patients were “analgesics/antirheumatics”, “cold-medications”, and “antibiotics”. Conclusion: Physicians’ statements showed that patients had an underestimated tendency to demand specific drug prescriptions and physicians met such demands more than expected. Moreover, female physicians are more likely to inform their patients about pharmacotherapy details in both groups. These findings may be considered as beneficial for RUM dissemination activities.

36-43

Authors: Chandran Sunitha, V S Harikrishnan, John Annie

Osteoporosis affects millions of people, especially the aged population and numerous researchers focus on developing novel pharmacotherapeutic agents for the prevention and treatment of osteoporosis. Animal models have become an indispensable part of the pre-clinical assessment of osteoporotic therapeutics and rat models have been widely preferred. The majority of studies so far reported have used young or short-term induced rat models, but they do not mimic the pathological condition in senile osteoporosis. Hence this study has focused on developing an ovariectomised and long term induced (OLI) aged rat model for the preclinical assessment studies. Long term osteoporosis was induced in Wistar rats by ovariectomy followed by the maintenance period of 10 months. Histological evaluation and Micro-CT analysis substantiated the extensive bone loss in the OLI rats compared to Control and ovariectomised and short term induced (OSI) rat model. OLI rats also exhibited impairment in the healing of 3 x 1.5 mm femoral cortical bone defect even after 8 weeks of surgery. Histomorphometric analyses indicated that OLI rats exhibited a poor regeneration efficiency (RE) ratio of 0.67 ± 0.2 compared to 0.95 ± 0.1 in the Control group. Chronic bone loss in the OLI rats together with the impaired osteogenic efficacy has been successfully demonstrated which proposes OLI rat models to be utilized for investigating novel pharmacotherapy’s or novel biomaterials intended for osteoporotic applications.

50-57

Authors: Shahanoor Momin, Shadab Khan, D M Ghadage, A V Yadav, Amit Wagh

The purpose of this study is to prepare a bilayer tablet of Propranolol HCl using Wet granulation technology and to formulate optimized formulation. Propranolol HCl, a nonselective β-adrenergic blocker which is the best drug candidate to formulate in to bilayer tablets fast release of drug from immediate release layer can give rapid onset of action which will help which will help to reduce Blood pressure within short period of time while maintenance dose of Propranolol HCl will maintain plasma concentration within therapeutic range for 12hrs having short half-life (3-5 hr) and first pass metabolism favors for sustained release dosage form. The tablets were prepared by wet granulation method. Hydrophobic matrix materials such as ethyl cellulose were used, which can release the drug up to 12 hrs in predetermined rate. Binder used was Starch paste (10%).The influence of hydrophobic polymer and granulation technique was studied. In this study, a bilayer tablet was prepared which contains an immediate release portion layer and sustained release portion. Ethyl cellulose were used as in alone, for Sustained release and Superdisintegrant Cross Povidone for immediate release used. The bilayer tablets were characterized by Calibration Curve, Calculation of Dose, Bulk Density, Tapped density, Angle of repose, Carr’s Index, Hausner’s ratio, Weight Variation, Hardness, Friability, Thickness, Drug Content and In-vitro dissolution profile. The granules showed satisfactory flow properties and compressibility. Best Formulation F3 [Drug + Ethylcellulose (1:3)] showed High % drug release 87.40% release, high drug content, high hardness and friability. Hence, it was found better than F1 and F2 so F3 is the best formulation.

62-69

Authors: Manpreet Kaur, Aruna Bhatia, Dimple Sethi, Gurpreet Kaur, Kajol Vig

The rise in infectious diseases as well as noninfectious immune related disorders causes millions of premature deaths worldwide and demands the need for the development of efficient immunomodulators. Consumer awareness about the harmful effects of chemical drugs raised a need to search for natural/ alternative therapies for the treatment of diseases. Immunotherapy is one of the alternative ways of modification of diseases. Some bacterial cell components such as peptidoglycans, lipoteichoic acid, secreted soluble substances, genomic DNA, etc, play role in immunomodulation responses. Structural difference between bacterial and eukaryotic DNA apparently account for the ability of bacterial DNA to serve as an immune activating agent, because of its high content of unmethylated CpG dinucleotides. Probiotic DNA’s efficacy could be further enhanced by loading it onto nanoparticles. Nanoparticle-assisted delivery may be a promising approach to alleviate the problem of instability and degradation of DNA. The present study was conducted to prepare and characterize the probiotic DNA loaded chitosan nanoparticles (DLCNP) and to find out the anti-diabetic potential of probiotic bacterial DNA Lactobacillus acidophilus NCDC 343 (LA DNA). Therapeutic efficacy of Probiotic DNA loaded with Chitosan Nanoparticles was evaluated in treating diabetic Balb/c mice. DNA loaded Chitosan Nanoparticles proved as effective anti-diabetic agents and in addition, the bioactivity of probiotic DNA was improved through nano delivery.

81-84

Authors: Shadab Khan, Anjum Patel, K S Bhise

The aim of present study was to evaluate in-vitro anti-oxidant properties of Punica granatum fruit (Pomegranate fruit) peel. Antioxidants are molecules involved in defense mechanisms against the deleterious effects of free radicals in most organisms. Antioxidants are the agents responsible for scavenging free radicals. A number of methods are currently being used for the evaluation of the antioxidant and free-radical scavenging properties of natural and synthetic antioxidants, including the DPPH method. The Punica granatum fruit (Pomegranate fruit) peel powder suspension was prepared and the DPPH radical scavenging assay was the method adopted to determine antioxidant potentials of aqueous suspension of pomegranate peel powder. Results revealed that DPPH aqueous solution gave comparable free-radical activity 24 hours post preparation compared with the freshly prepared solution. After 24 hours, activity was greatly reduced. It is, therefore, recommended that freshly prepared DPPH solution should be used at all times; however for prolonged experimental schedules, the DPPH solution should be used within 24 hours post preparation, so as to give comparable results with the freshly prepared solution and avoid ambiguity in results interpretation. Aqueous suspension of peel powder showed good antioxidant effect. Phenolic compounds, tannins and flavonoids are the major phytochemicals present in the pomegranate peel. Percentage of inhibition increased with the increased concentration of extracts. The present study provides evidence that the Punica granatum fruit peels is potential source of natural antioxidant

96-98

Authors: Santosh Kumar Panda, Gourab Sarkar, Manini Acharjya, P K Panda

Anti-ulcer activities of petroleum ether, chloroform, Ethanolic extract of Amaranthus spinosus leaf were tested for anti-gastric ulcer activity in Shay rat model. Oral dose of 400mg/kg of ethanolic extract reduced the ulceration and with 800mg/kg body weight ethanolic extract there is the complete absence of ulceration. The anti-gastric activity of ethanolic extract of A.spinosus 800mg/kg body weight was found to be equal to the effect produced by 2mg/kg of Famotidine orally. The reduction in gastric activity was more with Famotidine and the reduction in peptic activity is more with ethanolic extract of A.spinosus. All extracts are safe up to 4000mg/kg. The result of petroleum ether, chloroform and aqueous extract in respect of anti-ulcer activity are less prominent.

102-109

Authors: Zalak S Dodiya, Rina N Desai

Over the past decade or more, the prevalence of traditional risk factors for cardiovascular diseases has been increasing in the major populous countries of the developing world, including India, with consequent increases in the rates of coronary and cerebrovascular events. Cardiovascular diseases are predicted to be the major causes of morbidity and mortality in most developing nations around the world. Historically, most populations from South Asia have documented low levels of CV risk factors, particularly blood lipid levels, diabetes, and hypertension. However, in recent decades, the prevalence of these risk factors has increased, especially in urban areas. Numerous differences exist between younger and older women and between women and men with respect to the pathology of CHD and its incidence and prevalence over the life cycle. Women with obesity, metabolic syndrome, or diabetes have lipid profiles that adversely affect CHD risk.

119-127

Authors: Dhruvkumar Soni

Insulin is a hormone made by the pancreas that allows your body to use sugar (glucose) from carbohydrates in the food that you eat for energy or to store glucose for future use. Successful oral insulin delivery involves overcoming the enzymatic and physical barriers. Several companies across the globe are developing oral insulin based on different technology platforms. Insulin has been encapsulated in nanoparticles by mucoadhesive polymers such as chitosan, poly (lacticco-glycolic acid) (PLGA), and alginate which prevent enzymatic degradation and allow absorption across the epithelial layer in Peyer’s patches.

132-140

Authors: Piyush Agarwal, Amit Kumar, Y S Tanwar, Shailendra Sharma

Rizatriptan Benzoate undergo hepatic first pass metabolism. Aim of present research work is to improve bioavailability by formulating in-situ nasal gel. Formulation was developed to decrease the mucociliary authorization by using mucoadhesive polymer in gel, thus rising the contact time with nasal mucosa and humanizing the absorption of drug. Gels were primed by cold technique process and evaluate by Appearance, Viscosity, Gelation Temperature, Permeation Studies, Drug Content, Gel strength etc.. The gelation temperature of all studied gel formulations were found in range. Drug release was initiated in between 68.8-94.7% with K-peppas best fit model. pH of gel was in the rang and drug content was found between 92-99.89 %. Gel strength was found in range of 20-55 sec.

4-13

Authors: Anupam Kumar Sachan, Ankita Gupta, Mona Arora

Nanostructured lipid carriers (NLC)-based topical gel of Etoricoxib was prepared with the aim for the treatment of inflammation and allied conditions. The composition of NLC consisted of Stearic acid as solid lipid, oleic acid as liquid lipid and tween 80 as a surfactant. NLCs prepared by melt-emulsification and low temperature solidification techniques were characterized by particle sizing technology, scanning electron microscopy (SEM), and differential scanning calorimetry (DSC). All of the NLC showed high entrapment efficiency ranging from 69% to 76%. Both the entrapment and release rate were affected by the percentage of oleic acid. NLC-F3G-C was selected as best formulation with average particle size of 244 nm and polydispersity index of 0.690 indicating homogeneity in particle size distribution. The higher magnitude of zeta potential of NLC-F3G-C indicates the stability of formulation. The nanoparticulate dispersion was suitably gelled and assessed for Physical appearance, Homogeneity, Spreadability and in-vitro permeation study. In-vitro drug release pattern of developed NLC dispersion gel showed burst and prolong release. It was concluded that developed NLC gel of Etoricoxib holds promise for prolonged availability of drug in the skin tissues and can be used for better management of inflammatory conditions.

21-25

Authors: akshay sidharam javalgikar

Objective: Patient compliance and ease of administration are of significant importance in the design of dosage forms. Dysphasia is common among all age groups, especially in elderly and pediatrics. There are dosage forms like tablets, syrups in the market but still there is a need for new dosage form which acts effectively and locally. Jellies can provide an attractive alternative formulation in the treatment of oral candidiasis. So the present investigation aims to design, prepare and evaluate Clotrimazole jellies using xanthan gum with different concentrations. The benefits of these prepared jellies are increased bioavailability by-passing first pass metabolism. Method: The sucrose based jellies were prepared by heating and congealing method. Physical characteristics, pH, syneresis, in vitro dissolution testing, drug release kinetics, IR Spectral analysis and stability studies were conducted. Result: The prepared formulations are free from gritty particles. Among the prepared formulations, formulation C3 containing 1.5% xanthan gum released 93.22% in 30min was found to be promising. Stability studies on the promising and other formulations indicated that there were no significant changes in the drug content and in vitro dissolution characteristics. IR spectroscopic studies indicated that there were no drug-excipient interactions. Anti-fungal studies revealed that there is no change in the molecular activity of the drug. Conclusion: The prepared jellies of Clotrimazole could stay in the mouth for a longer period of time, which indicates a potential use of jellies of Clotrimazole for treating oral candidiasis.

30-36

Authors: Ashish Prakash Gorle, Ritesh Bhagavansing Rajput

Mostly the drugs are administered by oral route. Orally dispersible tablets are achieving importance when compared to novel oral drug delivery system. Orodispersible tablets are suitable for all age patients by masking the taste of drug. The objective of the present study was to optimize, formulate and evaluate orally dispersible tablet (ODT) of Paracetamol which disintegrates within few seconds in presence of saliva fluid by the use of super disintegrants. Paracetamol is widely used over-the counter analgesic (pain reliever) and antipyretic (fever reducer). It is a very bitter drug so the patients unable to take orally; hence their bitter taste were masked. ODTs Formulations were prepared by Direct Compression and wet granulation method by the use of superdisintegrants and taste masking (F7;F8) is done by Eudragit EPO. The developed formulations were evaluated in terms of weight variation, drug content, friability, thickness, hardness, disintegration and in vitro dissolution test. Stability study of optimized formulation was also carried out as per ICH guidelines. The effects of disintegrants as well as binders in different concentration on the release profile of paracetamol ODTs were studied. The studied parameters were found to be satisfactory for all formulations. Disintegration time for the formulations was found to be less than 40 seconds. Disintegration time for all ODTs decreased with increase in disintegrant concentration. ODTs prepared using Avicel possessed least disintegration time (11s), offered better dissolution profile than that of all the ODTs formulations. Accelerated studies proved that the optimized formulation was stable even after three months.

40-44

Authors: Nesar Ahmad, Noorul Hasan, Zeeshan Ahmad, Mohd Zishan, Seikh Zohrameena

Momordica charantia is a plant of the Cucurbitaceae family, is known as bitter melon, karela, and pare. It grows in tropical areas of the Amazon, , Asia, South America India, East Africa and Caribbean, and is used traditionally as both food and medicine. The fruit ripens, the flesh (rind) becomes slightly tougher and more bitter, and many think it too repulsive to eat. On the other hand, the pith becomes sweet and intensely red; it can be eaten uncooked in this state, and is a popular part in some Southeast Asian salads .Momordica charantia have provided many remedies for various diseases from ancient days to now a day. It has been used in various Asian traditional medicines for the treatment of cholera, anemia, diarrhea blood diseases, bronchitis, gout, dysentery, gonorrhea rheumatism, ulcer, colic, worms, disease of liver and spleen, cancer and diabetes etc.In preliminary phytochemical analysis we observed glycosides, phytosterols, alkaloids, phenolic, saponins compounds, fats, proteins, and fixed oils, flavonoids, and thin layer chromatography (TLC) was also performed. The medicinal values of Bitter melon lies in the bioactive phytochemical constituents that are non nutritive chemicals that produce clear-cut physiological effects on human body and protect them from various diseases. Juice of Momordica charantia the leaves used to treat piles totally. Momordica charantia is used as a blood purifier due to its bitter tonic properties.

52-56

Authors: Rishi Ram Parajuli, Prawan Dahal, Priyanka Pokhrel, Shreekrishna Lamichane, Saroj Shrestha, Purushottam Timilsina

Zika virus, a mosquito borne flavivirus transmitted primar­ily by Aedes aegypti mosquitoes is a pathogen affecting humans. These vectors also trans­mit dengue and chikungunya virus and are found throughout much of the world, including parts of the United States. An estimated 80% of persons infected with Zika virus are asymptomatic. Microcephaly is the greater risk for the infant born from the Zika Virus infected pregnant mother. This virus also causes neurological syndromes. Zika virus disease can often be diagnosed by performing reverse transcriptase-polymerase chain reaction (RT-PCR) on serum.

62-70

Authors: Amritveer Boparai, Junaid Niazi, Neha Bajwa, Preet Amol Singh

Dillenia indica f. elongata (Miq.) Miq. (Dilleniaceae) commonly known as Elephant apple. The vernacular names include Chalta, Chulta, Karambel, Bhavya and Ramphal.It is found in Bangladesh, Nepal, China, Indonesia and Assam, West Bengal, Orissa, Bihar, Myanmar regions of India. Dillenia indica f. elongata (Miq.) Miq.has been prevalently used in Indian traditional and ayurvedic medicine for curing plethora of ailments such as digestive, respiratory and central nervous systems. The information was put together, with the help of literature surveyed. Traditionally different parts of Dillenia indica f. elongata (Miq.) Miq. have been used for the relief of indigestion, asthma, influenza, dysentery,jaundice,promeho,weakness and rheumatic pain. Moreover, the extractives showed significant cytotoxic, CNS depressant and free radical scavenging activity. Wood obtained from the bark of the plant has been used for preparing rafters, tool-handles, cupboard and house pots. It is interesting to know that bark of Dillenia indica f. elongata (Miq.) Miq.is used for production of charcoal. Microspheres of metformin hydrochloride and novel mucoadhesive buccal tablets of oxytocin were also prepared from Dillenia indica f. elongata (Miq.) Miq. In vitro propagation is practised whereas micropropagation is considered at the time, when large scale plant multiplication is required. Phytochemical studies revealed substantial presence of polyphenols, tannins, alkaloids and flavanoids which are responsible for the various pharmacological activities. Major chemical constituents present in the plant are betulin (pentacyclic triterpenoid) and betulinic acid that show wide spectrum of pharmacological activities which include anti-HIV, anti-inflammatory, anti-cancer, anti-malarial etc. Furthermore, Dillenia indica f. elongata (Miq.) Miq. is found to possess analgesic, anti-diabetic, anti- microbial,anti-bacterial,anti-diabetic,anti-oxidant,anti-proliferation,anti-diarrhoeal, antiimplantation, cytotoxic, wound healing and hair waving activity.

7-10

Authors: Khalid Niaz, Abdul Qudoos, Ajaz Fatima, Hafiz Moeen-ud-din, Shah Murad

Introduction: Hyperlipidemia, either primary or secondary causes atherogenetic abnormalities leading to coronary artery disease, cardiac arrest and arrhythmias. Herbal therapy for prevention or cure of Hyperlipidemia is replacing allopathic medicine due to their bioequivalence and good compliance features. This study was conducted to compare hypolipidemic effects of Garlic and Nigella sativa. Place of Study: Study was conducted at Jinnah Hospital Lahore from July 2013 to December 2013. Seventy five hyperlipidemic patients were enrolled after getting written consent which was approved by Ethics committee of the hospital. Grouping: They were divided in three equal groups comprising 25 patients in each group. Group-A was treated by Nigella Sativa, Group-B was advised to take Garlic 10 grams twice daily for two months. Group-C was on placebo. Results: After two months therapy it was observed by statistical analysis that Nigella sativa decreased total cholesterol 12.4 mg/dl, triglycerides 16.7 mg/dl, and LDL cholesterol 27.3 mg/dl. HDL rise was 5.2 mg/dl. Garlic decreased total cholesterol 17.9 mg/dl, triglycerides 19.9 mg/dl and LDL cholesterol 14.8 mg/dl. HDL cholesterol rise was 8.0 mg/dl. Conclusion: It was concluded from this study that there is little difference between hypolipidemic effects of two important and famous herbal medicines ie, Nigella sativa and Garlic.

19-24

Authors: ASHU RATHI, Dr. Shila Jain, Dr. Alka Beotra, Dr. Manisha Trivedi, Vandana Nimker, Dr. Robin Kumar

Background; Tamoxifen, is a first-generation selective estrogen receptor modulator which is widely used for adjuvant breast cancer therapy. Tamoxifen metabolite completely bind to estrogen receptor on tumors as well as other tissues and target a nuclear complex that decreases DNA synthesis and inhibits estrogen effects. But these Selective Estrogen Receptor Modulators (SERMs) are classified as Prohibited substances according to the list of forbidden substances in sports by the World Anti-Doping Agency(WADA) In sports male athletes use tamoxifen in fighting against increase of estrogen level in the body, breast swelling , gynecomastia and fat forming a pear-silhouette very successfully. Aim; In the present study Tamoxifen was investigated carefully by administering to a Healthy volunteer . Material And Method; Urine samples are collected at different hours from 1st day to 5th day and analyzed by GC-MS. Result; It was found that Tamoxifen is rapidly metabolized in to their metabolite 3-hydrohy-4-methoxy Tamoxifen. Urinary extracts were analyzed by Gas Chromatography-Mass spectrometric Detector by using Selective ion modulator(SIM) and targeted GC-MS techniques with accurate mass. By the GC-MS study it is observed that 3-hydroxy-4-methoxy Tamoxifen metabolite gives two neutral loss m/z value at 58 & 72, but m/z value 58 shows more abundance than 72m/z value, hence it was selected as the marker m/z value to check the presence of metabolite in urine. Conclusion; After oral administration, Tamoxifen metabolite can be detected in to their maximum period up to 5 days.

34-45

Authors: Keerthi Sumana Murathoti, Trapti Saxena

The rationale of the present investigation is to develop a new oral drug delivery system utilizing both the concepts of controlled release and mucoadhesiveness, which could remain in stomach and control the drug release for longer period of time and thus to improve the bioavailability of the drug and reducing its dose related side effects. Gelatin/Acrypol 934P mucoadhesive microspheres of Levofloxacin were prepared by Emulsification cross- linking method. Drug and excipients interactions are tested using Fourier Transform-Infrared Spectroscopy, indicated no interactions. The average particle size for optimized formulations of Gelatin/Acrypol 934P microspheres were found to be 41.5µm. Photomicrographs revealed that the microspheres were spherical in shape. The drug entrapment efficiency for Gelatin/ Acrypol 934P microspheres was found to be 85.43%. In vitro drug release from Gelatin/ Acrypol microspheres showed more than 75% of the drug was released within 8 Hr, while pure drug showed complete drug release within 3 hours. This suggested controlled delivery of Levofloxacin for a longer period. Regression analysis revealed that the drug release from the microspheres was followed zero order kinetics. SEM images suggested spherical shape with smooth surface of microspheres formulations. Optimized formulation of Gelatin/ Acrypol 934P microspheres showed excellent mucoadhesivity i.e., 86.5%. Thus, the proposed Gelatin/ Acrypol 934P mucoadhesive microspheres might make a contribution in complete eradication of Helicobacter pylori owing to prolonged stomach residence time and small particle size.

51-55

Authors: Sachin Ambirwar, Amol Patil, Girish Joshi, Sudhir Pawar

Objectives: Evaluate antinociceptive activity of fluoxetine and the interaction of fluoxetine with naloxone and ondansetron. Methods: 32 albino mice of either sex were divided into 4 groups of 8 mice each: group I received normal saline, group II received fluoxetine; group III received fluoxetine + naloxone; group IV received fluoxetine + ondansetron. Fluoxetine and naloxone were given subcutaneously whereas ondansetron was given intraperitoneally. Eddy’s hot plate analgesiometer was used. Latency of licking of paw or jumping from the hot plate was recorded at intervals after giving study drugs in each group. Results: Fluoxetine produced a significant increase in the latency of licking of paw or jumping as compared to control at all time intervals except at 120 minutes with onset of antinociceptive effect within 30 min (p<0.01) and maximum effect at 60 min time interval (p<0.001). There was no significant difference between the control group and the fluoxetine + naloxone or fluoxetine + ondansetron group at any time point. Pre-treatment with naloxone and ondansetron antagonized the antinociceptive effects of fluoxetine. Conclusion: Administration of naloxone and ondansetron in fluoxetine treated mice antagonized the antinociceptive activity of fluoxetine. Therefore, antinociceptive activity of fluoxetine may be mediated through µ-opiod and 5HT3 receptors. Keywords: anti-nociceptive, Eddy’s hot plate, fluoxetine, naloxone, ondansetron.

67-92

Authors: Sunil Kumar Prajapati, Sheo Datta Maurya, Manas Kumar Das, Vijay Kumar Tilak, Krishna Kumar Verma, Ram C Dhakar

This review gives concise information about the dendrimers, properties, synthesis and application in drug delivery, diagnosis and therapy. Due to their unique architecture these have improved physical and chemical properties. They show high solubility, miscibility and reactivity due to their terminal groups. Dendrimers have well defined size, shape, molecular weight and monodispersity. These properties make the dendrimers a suitable carrier in drug delivery application. Dendrimers are unimolecular miceller in nature and due to this enhances the solubility of poorly soluble drugs. Their compatibility with DNA, heparin and polyanions make them more versatile. Dendrimers, also referred as modern day polymers, they offer much more good properties than the conventional polymers. Due to their multivalent and mono disperse character dendrimers have stimulated wide interest in the field of chemistry biology, especially in applications like drug delivery, gene therapy and chemotherapy. Self assembly produces a faster means of generating nanoscopic functional and structural systems. But their actual utility in drug delivery can be assessed only after deep understanding of factors affecting their properties and their behavior in vivo. Key words: Dendrimers PAMAM PPI Synthesis Divergent Convergent Cosmetics

8-13

Authors: Chhama Shukla, Sanchit Srivastava

As we know that, Oxadiazole is a heterocyclic compound containing an oxygen atom and two nitrogen atoms in a five-membered ring and is derived from furan by substitution of two methylene groups (=CH) with two pyridine type nitrogen (-N=) [1,2]. There are three known isomers that is 1,2,4-oxadiazole, 1,2,3-oxadiazole and 1,2,5-oxadiazole (Figure 1.0). However, 1,3,4-oxadiazole and 1,2,4-oxadiazole are better known, and more widely studied by researchers because of their many important chemical and biological properties. Among heterocyclic compounds, 1,3,4-oxadiazole has become an important construction motif for the development of new drugs. Compounds containing 1,3,4-oxadiazole cores have a broad biological activity spectrum including antibacterial, antifungal, analgesic, anti-inflammatory, antiviral, anticancer, antihypertensive, anticonvulsant, and anti-diabetic properties. They have also attracted interest in medicinal chemistry as surrogates (bioisosteres) for carboxylic acids, esters and carboxamides. The ability of 1,3,4-oxadiazole heterocyclic compounds to undergo various chemical reactions has made them important for molecule planning because of their privileged structure, which has enormous biological potential. Some examples of compounds containing the 1,3,4-oxadiazole unit currently used in clinical medicine are: Raltegravir as an antiretroviral drug and Zibotentan as an anticancer agent. They possesses various other biological activities and having various synthetic approaches, some of them are presented here in the aritcle. Keywords: Oxadiazoles synthetic approaches, biologically active ozadiazoles, oxadiazoles as anticancers etc.

18-22

Authors: A Dhulappa, K Lingappa, K G Siddalingeshwara

The main aim of the study is to enhance the biosynthesis of xylanse by incorporating nitrogen sources (both organic and inorganic). Recently, xylanases have expanded their use in many processing industries, such as pulp and paper, food and textile to newer needs such as biofuel production. .This study were taken up to the enhance the biosynthesis of xylanase by supplementation of organic nitrogen and inorganic nitrogen sources were employed in range of 0.25% to 1.25%. The organic nitrogen source were supplemented are peptone, yeast extract and beef extract and inorganic nitrogen sources are ammonium sulphate, ammonium chloride and ammonium nitrate. The yeast extract and ammonium nitrate were yielded higher xylnase production and showed 5.56 IU and 5.79 IU Key words: Xylanase, submerged fermentation, yeast extract, ammonium nitrate and assay.

31-34

Authors: Hasmukh R Jadav, Galib R, PK Prajapati

Objective: Apamarga Kshara Yoga (APK), a classical Ayurvedic formulation containing Apamarga Kshara (alkaline substance of Achyranthes aspera Linn.), Manahshila (Arsenic Disulphide) and Gomutra (cow’s urine) is effective in cases of Shvitra (vitiligo). As the formulations has short shelf life, inconvenient to patients and involve longer duration of pharmaceutical preparation; it is planned to convert into more convenient form. Design: Raw materials were authenticated and APK was prepared. Further, organoleptic and physico-chemical properties were evaluated. Results: An average 909.8 gm (90.98 %) yield after Taila Paka and 1379.6 gm ointment was observed in the process. Conclusions: As observed in present study, addition of wax to attain ointment consistency is mandate. Residue as Apamarga Kshara and Manahshila incorporated in preparation of ointment yielded more without losing its consistency.

43-55

Authors: Anshuman Keshari, Dr. PUSHPENDRA Kumar Tripathi, Arjita Srivastava, Ratan Vishwas

The aim present investigation is Formulation and Evaluation of Effervescent Floating Tablets of antidiabetic drug. Gastric retention are such systems, which increase the gastric retention time of the dosage forms at the stomach and upper part of the small intestine and suitable for the drug having site-specific absorption from the above sites. The Metformin HCl an orally administered biguanide of BCS class-3 High solubility and low permeability, which is widely use in the management of and the type-II diabetes, is an oral anti- hyperglycemic agent, shows incomplete absorption from the gastrointestinal tract and from the gastrointestinal track and absolute bioavailability is 50-60%with relatively short plasma half-life of 1.5-4.5 hours. It was using different polymers studying of deferent factors affecting the floating behavior of the prepare tablets was of our goals and important target in this part. Gastro-retentive tablets of Metformin HCl were prepared by wet granulation method using HPMC K200M (Hydroxylpropyl methyl cellulose) micro crystalline cellulose PH 101, sodium bicarbonate, HPMC K100 (LV), Magnesium stearate, colloidal silicon dioxide. In this formulation HPMC K 200 M was using different concentration. The Gastro-retentive tablet of Metformin HCl was evaluation of compression blend Angle of repose, Bulk density, tapped density, Drug compressibility study, Drug release rate, floating lag time etc. Result of our present study suggests that gastro-retentive tablets of Metformin HCl can be successfully designed to develop sustained release drug delivery which can reduce dosing frequency. Keywords: Effervescent system, gas generating system, gastro retentive drug delivery system, sustained drug release, Metformin hydrochloride

60-62

Authors: Saroj Yadav, K G Siddalingeshwara

Fibrin is a protein that forms in the blood clots after trauma or injury. This is essential to stop blood loss. There are more than twenty enzymes in the body that assist in clotting of the blood, while only one that can break the clot down. It is an endogenously produced fibrinolytic enzyme called plasmin. Streptokinase is an extracellular metallo-enzyme produced by beta-haemolytic streptococcus and is used as an effective and cheap clot-dissolving medication in some cases of myocardial infarction (heart attack) and pulmonary embolism. It belongs to a group of medications known as fibrinolytics. Fibrinolytic enzymes can be found in a variety of foods, such as Japanese Natto, Tofuyo, Korean Chungkook-Jang soy sauce, and edible honey mushroom. Fibrinolytic enzymes producing Aspergillus japonicum KSS 05 strain were screened for the production by fibrin plate assay method. The maximum zone of fibrin hydrolysis were found 6 mm diameter. Further the Aspergillus japonicum KSS 05 were employed for the production by submerged fermentation and it showed 235 IU by pH 6, temperature 300C and 1 ml inoculums size. Key words: Fermentation kinetics, effect of pH, fibrinolytic enzymes and fibrin

5-8

Authors: Pradeep Kumar Chaudhary, Subhash Goyal, Nanak Chand Mahajan, Saurabh Kansal, Priti Sinha

Cholecystitis is defined as inflammation of the gallbladder. Ninety percent of cases involve stones in the cystic duct and gall bladder, (i.e., calculus cholecystitis) with the other 10% of cases representing acalculus cholecystitis.(1) The association of gallstones with Helicobacter pylori has been investigated but not clearly demonstrated. In this study, the presence of H. pylori in the gallbladder mucosa of patients with symptomatic cholecystitis and cholelithiasis was investigated.The study included 50 cases of cholecystitis and cholelithiasis randomly selected who were admitted to the surgical wards of M.M.I.M.S.R, Mullana in last 2 years. All patients underwent cholecystectomy and gall bladder mucosa was histopathologically examined by giemsa staining (silver slide test). We concluded that no gall bladder mucosa exhibits presence of H. Pylori. Keywords: Cholelithiasis; Cholecystitis; H. pylori; Giemsa

19-25

Authors: K B Patel, J R Vyas, U M Upadhyay

The objective of this work was to prepare and evaluate oral sustained release matrix tablet of Nateglinide and to study the effect of proportion of wax and addition of release liner on in-vitro release of drug.The prepared tablets were evaluated for pre and post compression parameters. Stability study of the promising formulation was also performed. The matrix tablets were prepared by Direct compression, Co-processed & melt granulation, method using wax in concentration 25%, 35% & 45% and evaluated for on in-vitro drug release using Compritol & Precirol. No interactions were found between drug and excipients. Formulation containing 25% Precirol F13 shows releases up to 12 hours. Tablets with release characteristics offers critical advantages such as site specificity with improved absorption and efficacy etc. Keywords: Nateglinide, Sustained release, Compritol 888, Precirol ATO 5, Melt Granulation, Direct compression,

33-40

Authors: Salim Abou-Baker, T A El-Desouky, EL-Sedeek Lamyaa

Heterocyclic amines (HCAs) are a group of toxic chemicals, play an important role in the etiology of human cancer which formed at high temperature during cooking meat and fish. Antioxidants have proved to inhibit the formation of HCAs due to different mechanisms scavenging free radical, inhibits oxidative enzymes like cyochrome P450 and chelates metal ions like Fe+2 as well as protecting lipids against oxidation. Clove has potent antioxidants and antimicrobial activities standing out among the other species. Therefore current study done to show efficiency of 0.5% clove at preventing the formation of two most common HCAs: 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline (MeIQx) and 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) through seasoning of beef steaks before grilling and estimate antioxidant status of animals fed on the experimental diets. HCAs levels in food and blood samples were analyzed by HPLC. The results showed that content of MeIQx and PhIP in grilled beef meat steak were 23.0 ±2.87 and 15.0±2.14 ng/g, respectively. While the content of MeIQx and PhIP in seasoning grilled steak were degraded to 1.9 ± 0.31 and 1.6 ± 0.23 ng/g, respectively. On the other hand the results showed that the percentages of reduction of MeIQx and PhIP were 91.7 and 89.3% in seasoning grilled steak, respectively comparing with un- seasoning grilled steak. The levels of tested HCAs also showed significant differences among rat groups fed on the experimental diets. The highest MeIQx and PhIP concentrate in serum rats group fed on untreated grilled meat diet (positive control) were11.1±1.85 and 8.77±8.77 ng/ml, respectively, while seasoning with 0.5% clove before grilling led to decrease in MeIQx and PhIP concentrate to 0.82±0.16 and 0.51±0.09 ng/ml respectively with decreasing percent reached 92.6 % and 94.2% respectively. In addition, the results revealed that fed rats on un-seasoning grilled steak (positive control) caused high significant increased in lipid peroxide (malonaldhyde, MDA) accompanied by significant decreased in the levels of reduced glutathione content (GSH) and activities of antioxidant defense enzymes glutathione peroxidase (GHPx) and catalase (CAT), compared with basal diet group (negative control). However, clove treatment group lowered the level of lipid peroxidation and enhanced the antioxidant status of animals. Seasoning beef meat steaks before grilling with potent antioxidant clove species inhibit HCAs formation and their potential hazards to human health. This might be due to the powerful antioxidant activity of clove as strong hydrogen donating, metal chelating and scavenging of free radicals, hydrogen peroxide and superoxide. Keywords: Heterocyclic amines (HCAs), 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline (MeIQx) , 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP), clove, grilled beef meat, antioxidant plants, lipid peroxide, antioxidant defense enzymes.

48-55

Authors: Mohammed Asadullah Jahangir, Dr MA Saleem, Mohammed Shadab Shahab, Abdul Muheem, Shakir Saleem

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64-71

Authors: Bilal Tessema, Anteneh Belete, Tsige Gebre-Mariam

D. abyssinica was partially hydrolyzed in 6% HCl solution at room temperature for different lengths of time, (2, 4, 8, 16, and 32 days), dried using oven- and spray- drying techniques and subsequently investigated as directly compressible excipient in paracetamol tablet formulations. Native dioscorea starch (NDS) and oven dried acid modified dioscorea starch (AMDS) exhibited poor flow characteristics, whereas spray dried AMDS was found to be free flowing powder with 21.37 ± 1.39° angle of repose and 13.24 ± 0.76 g/sec flow rate. Both swelling power and percent solubility of the starches were found to increase with increase in temperature; AMDS showed higher percent solubility of 68.53%. Lubricant sensitivity and dilution potential of spray dried NDS and spray dried AMDS were investigated by incorporating magnesium stearate and paracetamol, respectively. In tablet formulations, spray dried AMDS and Starch 1500® tablets were produced with acceptable tablet characteristics up to 1% and 0.5% magnesium stearate concentrations, respectively. The spray dried AMDS was able to accommodate up to 40% paracetamol with acceptable criteria. Thus, it can be concluded that AMDS can be used as an alternative directly compressible excipient in tablet formulations. Keywords: Dioscorea starch, acid modification, spray drying, directly compressible excipient.