JOURNAL OF DRUG DELIVERY AND THERAPEUTICS

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