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FABRICATION AND CHARACTERIZATION OF CURCUMIN
NANOEMULSION AS COLLOIDAL CARRIER
Department of Chemical and Environmental Engineering, University of Nottingham
(Malaysia campus), Selangor 43500, Malaysia
Curcumin, a yellow figment extracted from Curcuma Longa
dried rhizome, was found to have significantpharmaceutical activities, for instance anti-cancer, anti- carcinogenic, anti-inflammatory, anti-oxidantand etc. However, bioavailability of curcumin after oral administration is always low due to its extremelylow solubility in water at acidic or neutral pH. In order to improve the absorption rate of curcumin invivo
, curcumin encapsulated nanoemulsion was developed using nanoemulsifying approach associatedwith ultrasonic cavitation. Nanoemulsions with droplets size in the range of 20-100nm were successfullyprepared using Brij56/Span20 as surfactants. Colloidal characteristics of resultant formulations wereprecisely studied using Zetasizer, up to 50%w/w of curcumin solution was well rendered in water with 5or 10%w/w surfactant. Obtained results showed that curcumin nanoemulsion Particle Size Distribution(PSD) was a function of surfactant HLB number and surfactant concentration. Curcumin 0.1% addedto water had a negligible effect on particle size, this was generally disagreed with most of the publication.
Despite an approximately 0 zeta potential was detected in all formulations, Zeta-Average andPolydispersity Index (PdI) of selected formulations indicated promising physical stability of formulationafter 10 days storage.
INFLUENCE OF PH ON THE RELEASE OF IBUPROFEN FROM
NANOEMULSION SYSTEM FOR TOPICAL APPLICATION
KH Chong1, M Basri1, A Kassim1, MBA. Rahman1, H Basri2, RNZRA Rahman3, AB Salleh3,
1Faculty of Science, Universiti Putra Malaysia, 43300 UPM Serdang, Selangor, Malaysia
2Faculty of Medicine and Health Sciences, Universiti Putra Malaysia,
43300 UPM Serdang, Selangor, Malaysia
3Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia,
43300 UPM Serdang, Selangor, Malaysia
4Faculty of Pharmacy, Universiti Kebangsaan Malaysia, 50300 Kuala Lumpur, Malaysia
5Sime Darby Bhd., Lot 2664, Jalan Pulau Carey, P.O.Box 207, 42700 Banting,
Nanoemulsion system containing ibuprofen was developed from palm kernel oil esters, phospholipidsand polysorbates to provide an alternative to conventional delivery vehicles such as tablets and gels. The
and L(2,3) were 2,475.56 microgram, 15.98 hours and 75.53/hours, respectively. According to the highestvalue of desirability index, Design Expert indicated the optimum enhancer mixture consisted of 30.21%OA, 35.85% PG and 33.94% VO.
COMPARING SUITABILITY OF DIFFERENT GRADES OF
GELUCIRE FOR DELIVERY OF TINIDAZOLE BY IN VITRO
School of Pharmacy and Technology Management, NMIMS, Vile Parle (w), Mumbai, India
Tinidazole is a poorly aqueous soluble drug and hence it is available in very high doses for treatment. Theobjective of the present study was to enhance the solubility of tinidazole by preparation of solid dispersionsusing different grades of excipients: Gelucire 44/14 and Gelucire 50/13. Phase solubility with both gradeswas carried out. Solid dispersions were prepared by the method of physical mixing, closed meltingmethod, kneading and coprecipitation. Improvement in saturation solubility, dissolution and dissolutionrate was studied. All complexes were characterized by FTIR and XRD. In phase solubility, both grades
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showed an A type relationship. A considerable improvement in saturation solubility was seen in complexes
prepared by all methods. Comparatively, closed melting and coprecipitation methods were more effectiveapproaches in solid dispersion design.
COMPARATIVE EFFICIENCY OF VARIOUS CYCLODEXTRIN
DERIVATIVES IN IMPROVING DELIVERY OF CANDESARTAN
CILEXITIL BY USING NOVEL TECHNIQUE OF FLUIDIZED
School of Pharmacy and Technology Management, NMIMS, Vile Parle (W),
Sparingly water soluble drugs such as Candesartan Cilexitil offer challenges in developing drug productwith adequate bioavailability. The objective of the present study was to enhance solubility of CandesartanCilexitil(CC) by preparing complexes of Candesartan Cilexitil and beta cyclodextrin (BCD), hydroxypropylated beta cyclodextrin (HPBCD) and gamma cyclodextrin (GCD) .Complexes were prepared in
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two ratios of drug: CD (1:1 and 1:2) by novel technique of fluidized bed processing by using pan glattprocessor top spray method. Prepared complexes were characterized by FTIR, XRD, and DSC. Allcomplexes were evaluated for increase in saturation solubility, dissolution and dissolution rate in 0.1 NHCL, pH 6.8 phosphate buffer, dissolution medium comprising of pH 6.5 phosphate buffer + 0.35% tween20 and water. Considerable increase in saturation solubility, dissolution and dissolution rate was observed in
of Costus speciosus
extract decreased testis weight, tubulus seminiferus diameter, number of leydigcells, sertoli cells, spermatosit cells and spermatid cells at a dose of 400mg/kg body weight but not atdoses of 100mg/kg and 200mg/kg.
THE POTENCY OF GARLIC (Allium sativum) EXTRACT AS
ANTI ALLERGY AGENT IN MICE
Faculty of Pharmacy, Dharmawangsa Dalam Airlangga University Pharmacy of Faculty
Campus B 60286 Surabaya, East Java, Indonesia
The aim of this research was to know the potency of garlic (Allium sativum
) extract as anti allergy inmice. The mice were divided into the negative control groups (mice were given saline solution perorally);positive control group (mice were given saline solution perorally and given ovalbumine 1µg/kg BWintraperitonelly); garlic extract groups (mice were given doses of 100; 200 and 400mg/kg garlic exctractperorally and given ovalbumine intraperitoneally at dose 1µg/kg BW 60 minute after administration garlicextract). Results of this research indicated that the positive control significantly increased immunoglobulinE production compared with control negative. While administration of the garlic exctract at dose 200and 400mg/kg BW but not garlic exctract at dose 100mg/kg BW significantly inhibited the increase ofimmunoglobulin E in mice which were given ovalbumine. These results suggest that garlic exctractat dose 200 and 400mg/kg BW has antiallergy properties.
INVESTIGATIONS INTO HYPOGLYCEMIC ACTIVITY OF
Verbesina encelioides BENTH. ROOTS EXTRACT
Rakesh K Sindhu, Inderbir Singh, Shridhar Nrayan, Sandeep Arora
Key Laboratory for Advanced Phytochemical Screening, Chitkara College of Pharmacy,
Rajpura, Patiala-140401, Punjab, India
Medicinal plants play an important role in the management of diabetes mellitus especially in developingcountries where resources are meager. Plant-based drugs have been used against various diseases sincea long time. The nature has provided abundant plant wealth for all the living creatures, which possessmedicinal virtues. Therefore, there is a necessity to explore their uses and to conduct pharmacognosticand pharmacological studies to ascertain their therapeutic properties. In fact, nowadays, diabetes is aglobal problem. Hence, the present study aims to open new avenues for the improvement of medicinal
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uses of Verbesina encelioides
Benth. roots for the selected area for diabetes. Dried aqueous and alcoholicextracts
were subjected for hypoglycaemic activity in swiss albino mice (30-40g). Blood sugar level wasdetermined using digital glucometer. The oral administration of roots extracts at doses of 400mg/kg led toa significant blood glucose reduction in normal and in Streptozotocin/alloxan-induced diabetic micesignificantly within 4 hours. Continued, daily administration of the drug produced a sustained effect.
the melting points of PHBV, thermal decomposition of the material via random scission process maytake place leading to shorter chains with terminal carboxyl groups. These terminal carboxyl groups maytrigger chemical reactions with the reactive sites in ENR. This melt reaction may serve as in-situcompatiblization for these immiscible green polymer blends. Isothermal melt reaction of PHBV withENR has been detected at temperatures ranging from 220 to 234°C. The rate of reaction increases withthe increasing isothermal melt reaction temperature (T ). Merging of the separate glass transition
temperatures (T ) (corresponding to those of the neat constituents) into one T may reflect increasing
adjustment of the two constituents after melt reaction. After melt reaction, finer and uniformly dispersedof PHBV spherulites in the matrix of ENR are observed. The rate of crystallization of PHBV has beenimpeded significantly after melt reaction for all blend compositions. These blends may be proposed aspotential pharmaceutical packaging material.
GATIFLOXACIN LOADED OCCULAR NANOPARTICULATE
DRUG DELIVERY SYSTEM
Mastiholimath VS, Dandagi PM, Gadad AP, Sharma SG
Department of Pharmaceutics, KLES University’s College of Pharmacy,
Biodegradable colloidal nanoparticles of Polylactide-co-glycolide (PLGA) have received considerableattention as a possible means of delivering drugs because of their biocompatibility and resorbabilitythrough natural pathways. As the occular efficacy of drugs is greatly influenced by the corneal contacttime, the most promising approach to increase occular bioavailability is to increase pre-corneal residencetime by using adequate drug delivery systems. PLGA nanoparticles exhibit highest uptake compare tolarger particles, PLGA nanoparticles are used for enhancement of occular drug absorption and the
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controlled release of protein and drug. The aim of the present research study is to formulate PLGAnanoparticle systems of Gatifloxacin for occular delivery. A modified solvent-evaporation technique wasused to prepare biodegradable and biocompatible PLGA nanoreservoir systems, stabilized by polyvinylalcohol (PVA). The prepared nanoparticles were characterized for particle size and size distribution,zeta potential, drug content and encapsulation efficiency and in vitro
drug release profile. Surfaceproperties of the nanoparticles were studied by Scanning Electron Microscopy. The designed nanoparticlesshowed average particle size from 278-441nm and zeta potential from 21-36mV at pH 7.4. The developedformulations were therapeutically efficacious, stable, non-irritant and provided sustained release of thedrug over an eight hour period. The developed system was thus a viable alternative to conventional eyedrops.
DEVELOPMENT AND CHARACTERIZATION OF A
PARTICULATE DRUG DELIVERY SYSTEM FOR ETOPOSIDE
Dandagi PM, Mastiholimath VS, Gadad AP, Manvi FV, Patil PS
Department of Pharmaceutics, KLEUniversity’s College of Pharmacy, JNMC Campus,
Nehru Nagar, Belgaum-590010, Karnataka
The present study was aimed to prepare and evaluate polymeric biodegradable nanoparticles of Etoposide(ETP). Nanoparticles were prepared by modified spontaneous emulsification solvent diffusion methodusing polylactic-co-glycolide acid (PLGA) as biodegradable matrix. The formulations were thencharacterized with respect to size and its surface morphology, zeta potential, entrapment efficiency, invitro
drug release profile, stability studies and in vivo
tissue distribution study. The formulated Etoposide-PLGA nanoparticles were spherical with a diameter ranging from 150nm to 250nm. The lowest entrapment
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efficiency was found to be 51.07% and the highest was found to be 62.16%. Highest cumulative percentdrug release was observed with F-8 (85.24%) and lowest with F-1 (44.05%) in 120 hrs. Based on thehighest regression values (R), the best-fit model was Peppa’s for all eight formulations. Formulation F-8 with optimal particle size, high entrapment efficiency and satisfactory in vitro
release was selected forin vivo
studies. The average targeting efficiency of the injected dose of drug loaded nanoparticles wasfound to be 11.23 ± 0.13% in liver, 27.72 ± 0.42% in lungs, 10.63 ± 0.27% in kidney and 13.24 ± 0.57%in spleen whereas accumulation of pure drug in liver was 7.93 ± .2.104%, in lungs it was 8.57 ± 1.724%,in kidney it was 08.10 ± 0.827% and spleen 11.35 ± 0.503% of the injected dose. The results revealedthat, the drug loaded nanoparticles showed preferential drug targeting to lungs followed by liver, kidneyand spleen. Stability studies indicated that 4°C is the most suitable and ideal temperature for storage ofPLGA nanoparticles. This drug delivery is endowed with several exclusive advantages and hence holdspotential for further research and clinical application.
FABRICATION OF AN INTEGRATED MICROFLUIDIC
PERFUSION SYSTEM FOR MIXING DIFFERENT SOLUTIONS
Alireza Bahadorimehr, Burhanuddin Yeop Majlis, Jumril Yunas
Institute of Microengineering and Nanoelectronics, Universiti Kebangsaan Malaysia,
We present a simple and low cost fabrication of Microfluidic mixer for use in different applications inMicro Total Analysis Systems especially for automated perfusion of multiple solutions to a single cellculture chamber. This device consists of 6 inlets and 2 outlets with additional 3 inlet/outlet channels forflow rate alteration and other mixing purposes such as electrophoresis activation, which is capable ofproducing mixtures of the various solutions. All the inlets are connected to PTFE and silicone tubings
using special PDMS fittings technique for fluid leakage avoidance. The inputs are controlled by aprogrammable micro-syringe pump in order to activate each input in any sequence of time. Typicalmicroscopic glass slides are utilized as a substrate for fabrication of microchannels and chamber whichhas the minimum effect on most of biology samples. The same un-etched glass is used as cover glass forbonding purposes. Using photo-resist as an etch mask instead of some deposition methods makes theprocedure more convenient and cost effective compare to other expensive techniques such as DRIE,etc. The baking time of photo-resist is a critical factor for longer resistance against etchant solution whichis optimized by this method. In addition the etchant concentration in wet etching process is discussed toachieve a decent surface and wall characteristics for bio-applications. A smooth channel surface withacceptable sharp wall edges makes this procedure suitable for many applications which vertical walls arenot crucial. Different dye samples were tested inside the chamber and promising results were attained.
ANTICONVULSANT ACTIVITY OF Kigelia pinnata BARK
Abhishek Singh, Umesh kumar Sharma, Umashankar Sharma, Niranjan Sutar,
Department of Pharmacy, Sirmadanlal Group of Institutions, Etawah (U.P.)
The present studies revealed the anticonvulsant activity by PTZ (pentylene tetrazole) and MES (maximalelectro shock) induced convulsions in wistar rats using Kigelia pinnata
bark methanolic (KPM) andaqueous (KPA) extracts extracted successively. Alkaloids, glycosides, carbohydrates, steroids, tannins,phenolic compounds, proteins, amino acids, saponins, flavonoids were present in both extracts. 250 mg/kg and 500mg/kg of KPM and KPA were given intraperitonially. The latency of seizures, death time andpercentage of mortality were observed. KPM gave significant protection against the PTZ and MES
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induced convulsions (p < 0.0001).
THE POTENCY OF Mimosa pudica EXTRACT FOR
ANALGESIC AND ANTI-INFLAMMATORY EFFECT
Faculty of Pharmacy, Dharmawangsa Dalam Airlangga University Campus B 60286
The aim of this research was to know the analgesic and antiinflammatory effect of Putri malu (Mimosapudica
) exctract. Putri malu extract was evaluated for antiinflammatory effect by carrageen-inducedrat paw inflammation. The analgesic activity was tested by hot plate method in albino mice. The Putrimalu extract in doses of 200 and 400mg/kg BW showed significantly inhibition of paw inflammation. Inthe hot plate model, the Putri malu extract at 200 and 400mg/kg BW significantly inhibited the pain after
associated with bone formation. They reduce fracture incidence by improving bone qualities in additionto increasing bone mass. Osteoblast plays a crucial role in bone formation through the proliferation anddifferentiation. Especially, osteoblast differentiation, an important process for its function, confers markedrigidity and strength to the bone while still maintaining some degree of elasticity. In order to find the idealanabolic agent with stimulation on alkaline phosphatase (ALP) activity as a marker of osteoblastdifferentiation, I carried out the screening of 32 Indonesian traditional medicinal plants. Based on thescreening, Barleria lupulina
aerial parts, Graptophyllum pictum
leaf, and Spilanthes acmella
aerialparts stimulated ALP activity to 139%, 128% and 169% respectively. Based on phytochemistry screeningdata, alkaloid, flavonoid, tannin and antraquinon were found on Graptophyllum pictum
. Also terpenoid was found on Spilantes acmella
. The hexane, ethyl acetate, n-butanol andwater fraction from Graptophyllum pictum
and Spilanthes acmella
were evaluated the stimulativeactivity on alkaline phosphatase (ALP) of MC3T3-E1 osteoblast cells. ALP activity is a marker ofosteoblast differentiation. Among the tested fractions, the n-butanol and water fraction stimulated ALPactivity to 112% and 122% for Graptophyllum pictum
, stimulated ALP activity to 126% and 127% forSpilanthes acmella
GRAFT COPOLYMER (POLYVINYLPYRROLIDONE –CO-
ACRYLAMIDE): OPTIMIZATION OF SYNTHESIS,
CHARACTERIZATION AND FILM PROPERTIES STUDY
MK Tripathy1, S Tripathy2, S Gupta2, DK Tripathi1
1Faculty of Pharmacy, Puncak Alam Campus, University Teknologi MARA(UiTM), Malaysia
2Sri Jayadev College of Pharmaceutical sciences, Naharkanta, Orissa, India
Both Polyvinylpyrrolidone (PVP) and Acrylamide (Acr) are the polymers commonly used inpharmaceutical formulations. To prepare transdermal drug delivery systems (TDDS), none of these canbe used alone to make a film, so they are mixed with suitable other polymers .The present study dealswith the synthesis of a novel copolymer, its characterization and the evaluation of film properties. Thesepolymers have been reacted under controlled conditions in a specially designed jacketed reaction vessel
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and process optimization was done on the basis of variables like initiator (ammonium persulphate)concentration, the ratio of virgin polymers and physical environment of the reaction vessel to make agraft copolymer. The principle of polymerization used was atom radical copolymerization. The synthesismethod was optimized for the optimum graft yield by evaluating the effect of the process variables onthe graft yield. The synthesized copolymer has been characterized by X-ray diffraction (XRD), Differentialscanning calorimetry (DSC), Fourier transformed infrared (FTIR) spectroscopic technique and scanningelectron microscopy (SEM) to confirm copolymerization. The film was casted with graft copolymer bysolvent evaporation technique using glycerin as plasticizer. The film alone and loaded with the drugMethotrexate (Mtx) were tested for their water vapor transmission (WVT), moisture absorptivity (MA),tensile strength (TS), film thickness, flatness and weight variation. The results of the tests revealed thatthe copolymer alone can be proposed to be a suitable polymeric material for making patches for drugdelivery specifically for transdermal drug delivery systems.
containing C8 was produced by lipase catalyzed acidolysis of C8 and VCO. The production of theSVCO was optimized based on the caprylic acid (%) incorporated in the reaction products using centralcomposite design (CCD). The in vitro
release profiles were assessed using automated vertical diffusioncells (Microette) with cellulose membrane to simulate skin barrier. a-Tocopherol (5% w/v) was formulatedseparately in 15%w/v of the oils in ethanol. Samples were collected hourly for the first eight hours andthen at 24 hours for cumulative drug release profiles using rapid resolution high chromatography. Thesynthesized SVCO containing 34.38% caprylic acid showed a more enhanced drug release profileswithin the first 8 hours than VCO. After 24 hours, the cumulative amount of drug release for VCO was31.02%, while for SVCO the amount was increased to 56.90%. The results indicated that caprylic acidin the SVCO influenced the in vitro
release profiles of the model drug, thus highlighting its potential as apenetration enhancer of a-tocopherol.
PHOSPHOLIPID COMPLEX AS A CARRIER OF Kaempferia
galanga RHIZOME EXTRACT TO IMPROVE ITS
Department of Pharmakognosy and Phytochemistry, Airlangga University Dharmawangsa
Dalam Surabaya 60286 Surabaya, East Java, Indonesia
Preparation of lipophilic complex of Kaempferia galanga
rhizome extract using phospholipid was intendedto improve the bioavailability of some compounds in it. These complexes formation showed a goodinteraction confirmed by DSC, SEM and FTIR spectroscopy, comparing between the complex to theone of the individual component (ethyl p-methoxycinnamate, a marker compound of Kaempferia galanga
rhizome) and their mixture (the extract). The analgesic activity, determined using writhing test, showedan increase in biological activity of ethyl p-methoxycinnamate in comparison with this compound in thefree form at an equivalent dosage. In the contrary happened in the extract. The extract in the free formshowed better activity than its lipophilic complex.
FORMULATION AND DEVELOPMENT OF MATRIX TABLETS
OF TRAMADOL USING KATIRA GUM AS RELEASE MODIFIER
Inderbir Singh, Rakesh Kumar, Shridhar Narayan, Sandeep Arora
Chitkara College of Pharmacy, Chandigarh-Patiala National Highway,
Rajpura– 140401, Patiala, Punjab, India
The present study was aimed to study the drug release retardant property of katira gum in matrix tabletscontaining tramadol as a model drug. Katira gum was characterized in terms of pH, viscoisity and
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APPLICATION NOTE Separation and Quantitation of R and SEnantiomers using Normal PhaseChromatography on an API 3000™LC/MS/MS System Normal phase chromatography can strates that it is possible to safely and be used for the analysis of chiral compounds using the API 3000™ LC/MS/MS System. Overview Key Features Figure 1. Verapamil calibration curves for enantiomer R and