Abstract: Intravitreal injection (IVI) is the most common treatment for eye posterior segment diseases such as endopthalmitis, retinitis, age-related macular degeneration, diabetic retinopathy, uveitis, and retinal detachment. Most of the drugs used to treat vitreoretinal diseases, have a narrow concentration range in which they are effective, and may be toxic at higher concentrations. Therefore, it is critical to know the drug distribution within the eye following intravitreal injection. Having knowledge of drug distribution, ophthalmologists can decide on drug injection frequency while minimizing damage to tissues. The goal of this study was to develop a computer model to predict intraocular concentrations and pharmacokinetics of intravitreally injected drugs. A finite volume model was created to predict distribution of two drugs with different physiochemical properties in the rabbit eye. The model parameters were obtained from literature review. To validate this numeric model, the in vivo data of spatial concentration profile from the lens to the retina were compared with the numeric data. The difference was less than 5% between the numerical and experimental data. This validation provides strong support for the numerical methodology and associated assumptions of the current study.
Abstract: Today, cancer remains one of the major diseases that
lead to death. The main obstacle in chemotherapy as a main cancer
treatment is the toxicity to normal cells due to Multidrug Resistance
(MDR) after the use of anticancer drugs. Proposed solution to
overcome this problem is the use of MDR efflux inhibitor of cinchona
alkaloids which is delivered together with anticancer drugs
encapsulated in the form of polymeric nanoparticles. The particles
were prepared by the hydration method. The characterization of
nanoparticles was particle size, zeta potential, entrapment efficiency
and in vitro drug release. Combination nanoparticle size ranged 29-45
nm with a neutral surface charge. Entrapment efficiency was above
87% for the use quinine, quinidine or cinchonidine in combination
with etoposide. The release test results exhibited that the cinchona
alkaloids release released faster than that of etoposide. Collectively,
cinchona alkaloids can be packaged along with etoposide in
nanomicelles for better cancer therapy.
Abstract: Researchers of drug-drug interaction alert systems
have often suggested that there were high overridden rate for alerts and
also too false alerts. However, research about decreasing false alerts is
scant. Therefore, the aim of this article attempts to proactive
identification of false alert for drug-drug interaction and provide
solution to decrease false alerts. This research involved retrospective
analysis prescribing database and calculated false alert rate by using
MYSQL and JAVA. Results of this study showed 17% of false alerts
and the false alert rate in the hospitals (37%) was more than in the
clinics. To conclude, this study described the importance that
drug-drug interaction alert system should not only detect drug name
but also detect frequency or route, as well as in providing solution to
decrease false alerts.
Abstract: Studies were carried out to determine the in vitro
susceptibility of the typhoid pathogens to combined action of Euphorbia hirta, Euphorbia heterophylla and Phyllanthus niruri. Clinical isolates of the typhoid bacilli were subjected to susceptibility testing using agar diffusion technique and the minimum inhibitory
concentration (MIC) determined with tube dilution technique. These
isolates, when challenged with doses of the extracts from the three
medicinal plants showed zones of inhibition as wide as 26±0.2mm, 22±0.1mm and 18±0.0mm respectively. The minimum inhibitory concentration (MIC) revealed organisms inhibited at varying
concentrations of extracts: E. hirta (S. typhi 0.250mg/ml, S. paratyphi A 0.125mg/ml, S. paratyphi B 0.185mg/ml and S. paratyphi C 0.225mg/ml), E. heterophylla (S. typhi 0.280mg/ml, S. paratyphi A
0.150mg/ml, S. paratyphi B 0.200mg/ml and S. paratyphi C 0.250mg/ml) and P. niruri (S. typhi 0.150mg/ml, S. paratyphi A 0.100mg/ml, S. paratyphi B 0.115mg/ml and S. paratyphi C 0.125mg/ml). The results of the synergy between the three plants in
the ration of 1:1:1 showed very low MICs for the test pathogens as follows S. typhi 0.025mg/ml, S. paratyphi A 0.080mg/ml, S. paratyphi B 0.015mg/ml and S. paratyphi C 0.10mg/ml with the
diameter zone of inhibition (DZI) ranging from 35±0.2mm,
28±0.4mm, 20±0.1mm and 32±0.3mm respectively. The secondary
metabolites were identified using simple methods and HPLC. Organic components such as anthroquinones, different alkaloids,
tannins, 6-ethoxy-1,2,3,4-tetrahydro-2,2,4-trimethyl and steroids were identified. The prevalence of Salmonellae, a deadly infectious disease, is still very high in parts of Nigeria. The synergistic action of these three plants is very high. It is concluded that pharmaceutical companies should take advantage of these findings to develop new
anti-typhoid drugs from these plants.
Abstract: To compare Healing Effects of an
Ayurvedic Preparation and Silver Sulfadiazine on burn wounds in
Albino Rats.
Methods: Albino rats– 30 male / female rats weighing between
150-200 g were used in the study. They were individually housed and
maintained on normal diet and water ad libitum. Partial thickness
burn wounds were inflicted, on overnight-starved animals under
pentobarbitone (30mg/kg, i.p.) anaesthesia, by pouring hot molten
wax at 80oC into a plastic cylinder of 300 mm2 circular openings
placed on the shaven back of the animal. Apart from the drugs under
investigation no local/ systemic chemotherapeutic cover will be
provided to animals. All the animals were assessed for the percentage
of wound contraction, signs of infection, scab formation and
histopathological examination.
Results: Percentage of wound healing was significantly better in
the test ointment group compared to the standard. Signs of infection
were observed in more animals in the test ointment group compared
to the standard. Scab formation also took place earlier in the test
ointment group compared to standard. Epithelial regeneration and
healing profile was better in the test ointment compared to the
standard. Moreover the test ointment group did not show any raised
margins in the wound or blackish discoloration as was observed in
silver sulfadiazine group.
Conclusion: The burn wound healing effect of the ayurvedic
ointment under study is better in comparison to standard therapy of
silver sulfadiazine. The problem of infection encountered with the
test ointment can be overcome by changing the concentrations and
proportions of the ingredients in the test ointment which constitutes
the further plan of the study.
Abstract: The present research was designed to investigate the
anti-microbial activity of aristolochic acid from the root of
Aristolochia bracteata. From the methanolic & ethyl extract extracts
of Aristolochia bracteata aristolochic acid I was isolated and
conformed through IR, NMR & MS. The percentage purity of
aristolochic acid I was determined by UV & HPLC method. Antibacterial
activity of extracts of Aristolochia bracteata and the
isolated compound was determined by disc diffusion method. The
results reveled that the isolated aristolochic acid from methanolic
extract was more pure than the compound from ethyl acetate extract.
The various extracts (500μg/disc) of Aristolochia bracteata showed
moderate antibacterial activity with the average zone of inhibition of
7-18 mm by disc diffusion method. Among the extracts, ethyl acetate
& methanol extracts were shown good anti-microbial activity and the
growth of E.coli (18 mm) was strongly inhibited. Microbial assay of
isolated compound (Aristolochic acid I) from ethyl acetate &
methanol extracts were shown good antimicrobial activity and the
zone of inhibition of both at higher concentration 50 μg/ml was
similar with the standard aristolochic acid. It may be concluded that
the isolated compound of aristolochic acid I has good anti-bacterial
activity.
Abstract: There is an urgent need to develop novel
Mycobacterium tuberculosis (Mtb) drugs that are active against drug
resistant bacteria but, more importantly, kill persistent bacteria. Our
study structured based on integrated analysis of metabolic pathways,
small molecule screening and similarity Search in PubChem
Database. Metabolic analysis approaches based on Unified weighted
used for potent target selection. Our results suggest that pantothenate
synthetase (panC) and and 3-methyl-2-oxobutanoate hydroxymethyl
transferase (panB) as a appropriate drug targets. In our study, we
used pantothenate synthetase because of existence inhibitors. We
have reported the discovery of new antitubercular compounds
through ligand based approaches using computational tools.
Abstract: Information regarding early onset neonatal sepsis
(EONS) pathogens may vary between regions. Global perspectives
showed Group B Streptococcal (GBS) as the most common causative
pathogens, but the widespread use of intrapartum antibiotics has
changed the pathogens pattern towards gram negative
microorganisms, especially E. coli. Objective of this study is to
describe the pathogens isolated, to assess current treatment and risk
of EONS. Records of 899 neonates born in three General Hospitals
between 2009 until 2012 were retrospectively reviewed. Proven was
found in 22 (3%) neonates. The majority was isolated with gram
positive organisms, 17 (2.3%). All grams positive and most gram
negative organisms showed sensitivity to the tested antibiotics. Only
two rare gram negative organisms showed total resistant. Male was
possible risk of proven EONS. Although proven EONS remains
uncommon in Malaysia, nonetheless, the effect of intrapartum
antibiotics still required continuous surveillance.
Abstract: Data mining incorporates a group of statistical
methods used to analyze a set of information, or a data set. It operates
with models and algorithms, which are powerful tools with the great
potential. They can help people to understand the patterns in certain
chunk of information so it is obvious that the data mining tools have
a wide area of applications. For example in the theoretical chemistry
data mining tools can be used to predict moleculeproperties or
improve computer-assisted drug design. Classification analysis is one
of the major data mining methodologies. The aim of thecontribution
is to create a classification model, which would be able to deal with a
huge data set with high accuracy. For this purpose logistic regression,
Bayesian logistic regression and random forest models were built
using R software. TheBayesian logistic regression in Latent GOLD
software was created as well. These classification methods belong to
supervised learning methods.
It was necessary to reduce data matrix dimension before construct
models and thus the factor analysis (FA) was used. Those models
were applied to predict the biological activity of molecules, potential
new drug candidates.
Abstract: Carbon tetrachloride (CCl4) is a well-known
hepatotoxin and exposure to this chemical is known to induce
oxidative stress and causes liver injury by the formation of free
radicals. Flacourtia indica commonly known as 'Baichi' has been
reported as an effective remedy for the treatment of a variety of
diseases. The objective of this study was to investigate the
hepatoprotective activity of aqueous extract of leaves of Flacourtia
indica against CCl4 induced hepatotoxicity. Animals were pretreated
with the aqueous extract of Flacourtia indica (250 & 500 mg/kg
body weight) for one week and then challenged with CCl4 (1.5 ml/kg
bw) in olive oil (1:1, v/v) on 7th day. Serum marker enzymes (ALP,
AST, ALT, Total Protein & Total Bilirubin) and TBARS level
(Marker for oxidative stress) were estimated in all the study groups.
Alteration in the levels of biochemical markers of hepatic damage
like AST, ALT, ALP, Total Protein, Total Bilirubin and lipid
peroxides (TBARS) were tested in both CCl4 treated and extract
treated groups. CCl4 has enhanced the AST, ALT, ALP and the
Lipid peroxides (TBARS) in liver. Treatment of aqueous extract of
Flacourtia indica leaves (250 & 500 mg/kg) exhibited a significant
protective effect by altering the serum levels of AST, ALT, ALP,
Total Protein, Total Bilirubin and liver TBARS. These biochemical
observations were supported by histopathological study of liver
sections. From this preliminary study it has been concluded that the
aqueous extract of the leaves of Flacourtia indica protects liver
against oxidative damages and could be used as an effective protector
against CCl4 induced hepatic damage. Our findings suggested that
Flacourtia indica possessed good hepatoprotective activity
Abstract: Microbubbbles incorporating ultrasound have been used to increase the efficacy of targeted drug delivery, because microstreaming induced by cavitating bubbles affects the drug perfusion into the target cells and tissues. In order to clarify the physical effects of microstreaming on drug perfusion into tissues, a preliminary experimental study of perfusion enhancement by a stably oscillating microbubble was performed. Microstreaming was induced by an oscillating bubble at 15 kHz, and perfusion of dye into an agar phantom was optically measured by histology on agar phantom. Surface color intensity and the penetration length of dye in the agar phantom were increased more than 70% and 30%, respectively, due to the microstreaming induced by an oscillating bubble. The mass of dye perfused into a tissue phantom for 30 s was increased about 80% in the phantom with an oscillating bubble. This preliminary experiment shows the physical effects of steady streaming by an oscillating bubble can enhance the drug perfusion into the tissues while minimizing the biological effects.
Abstract: The aim of this article is to narrate the utility of novel simulation approach i.e. convolution method to predict blood concentration of drug utilizing dissolution data of salbutamol sulphate microparticulate formulations with different release patterns (1:1, 1:2 and 1:3, drug:polymer). Dissolution apparatus II USP 2007 and 900 ml double distilled water stirrd at 50 rpm was employed for dissolution analysis. From dissolution data, blood drug concentration was determined, and in return predicted blood drug concentration data was used to calculate the pharmacokinetic parameters i.e. Cmax, Tmax, and AUC. Convolution is a good biwaiver technique; however its better utility needs it application in the conditions where biorelevant dissolution media are used.
Abstract: The essential oil of M. × piperita L. was formulated
into a topical gel. The prepared gel was characterized for its pH,
viscosity, spreadiblity, consistency and extrudiblity, while its stability
was evaluated under different temperature conditions. The prepared
M. × piperita oil gel was clear and transparent. The pH value of
developed gel was 6.6, while its viscosity was 1200 cP. Spreadability
and consistency of the M. × piperita oil gel was 10.7 g.cm/sec and 7
mm, respectively. The prepared gel showed good extrudiblity. During
the stability studies, no significant change in pH and viscosity as a
function of time for gel was observed, indicating stability of prepared
formulation. The gel developed in this study is expected to forward
the usage of M. × piperita essential towards commercial application.
Abstract: In this study, the forty Thai medicinal plants were
used to screen the antibacterial activity against Campylobacter jejuni.
Crude 95% ethanolic extracts of each plant were prepared.
Antibacterial activity was investigated by the disc diffusion assay,
and MICs and MBCs were determined by broth microdilution. The
results of antibacterial screening showed that five plants have activity
against C.jejuni including Adenanthera pavonina L., Moringa
oleifera Lam., Annona squamosa L., Hibiscus sabdariffa L. and
Eupotorium odortum L. The extraction of A. pavonina L. and A.
squamosa L. produced an outstanding against C. jejuni, inhibiting
growth at 62.5-125 and 250-500 μg/mL, respectively. The MBCs of
two extracts were just 4-fold higher than MICs against C. jejuni,
suggesting the extracts are bactericidal against this species. These
results indicate that A. pavonina and A. squamosa could potentially
be used in modern applications aimed at treatment or prevention of
foodborne disease from C. jejuni.
Abstract: The potential of antioxidant activities of the plant
extract Gynura procumbens, Achyranthes aspera and Polygenum
tomentosum were studied by using 1, 1-diphenyl-2-picrylhydrazyl
(DPPH) .Antioxidant activity was qualitatively and quantitatively
determined. In this analysis , Ascorbic acid (Vitamin C) was used as
the standard .The antioxidant activities were observed all three plant
extracts and the EC50 values of G procumbens A.aspera and
P.tomemtosum were 13.7 μg /ml,14.37 μg /ml and 14.35 μg /ml.
Among these plants, G.procumbens is more potent antioxidant
activity then others. Antitumor activities were found with A.aspera
(s2) extracts in the dose of 100ppm in carrot disks and G.procumbens
(s1) and P.tomentosum (s3) in the dose of 1000 ppm. Therefore, these
herbal plants are used in traditional medicines.
Abstract: Pepper spray use has gained momentum since 1992
and although the active ingredient is readily available, it is considered
a weapon with restricted use in many regions, including The
Bahamas. In light of controversy in the literature regarding the
severity of presenting respiration complaints among individuals postacute
exposure of pepper spray inhalation, this descriptive case series
study was conducted to assess the respiratory status of persons
evaluated during a mass casualty in The Bahamas. Parameters noted
were patients- demographics and respiration severity determined via
clinical examination findings, disposition and follow-up review of the
20 persons. Their most common complaint was difficulty breathing
post exposure. Two required admission and stayed for
Abstract: Removal of PCP by a system combining
biodegradation by biofilm and adsorption was investigated here.
Three studies were conducted employing batch tests, sequencing
batch reactor (SBR) and continuous biofilm activated carbon
column reactor (BACCOR). The combination of biofilm-GAC
batch process removed about 30% more PCP than GAC adsorption
alone. For the SBR processes, both the suspended and attached
biomass could remove more than 90% of the PCP after
acclimatisation. BACCOR was able to remove more than 98% of
PCP-Na at concentrations ranging from 10 to 100 mg/L, at empty
bed contact time (EBCT) ranging from 0.75 to 4 hours. Pure and
mixed cultures from BACCOR were tested for use of PCP as sole
carbon and energy source under aerobic conditions. The isolates
were able to degrade up to 42% of PCP under aerobic conditions in
pure cultures. However, mixed cultures were found able to degrade
more than 99% PCP indicating interdependence of species.
Abstract: pH-sensitive drug targeting using nanoparticles for
cancer chemotherapy have been spotlighted in recent decades. Graft
copolymer composed of poly (L-histidine) (PHS) and dextran
(DexPHS) was synthesized and pH-sensitive nanoparticles were
fabricated for pH-responsive drug delivery of doxorubicin (DOX).
Nanoparticles of DexPHS showed pH-sensitive changes in particle
sizes and drug release behavior, i.e. particle sizes and drug release rate
were increased at acidic pH, indicating that DexPHS nanoparticles
have pH-sensitive drug delivery potentials. Antitumor activity of
DOX-incorporated DexPHS nanoparticles were studied using CT26
colorectal carcinoma cells. Results indicated that fluorescence
intensity was higher at acidic pH than basic pH. These results
indicated that DexPHS nanoparticles have pH-responsive drug
targeting.
Abstract: Delayed wound healing in diabetes is primarily
associated with hyperglycemia, over-expression of inflammatory
marker, oxidative stress and delayed collagen synthesis. This
unmanaged wound is producing high economic burden on the
society. Thus research is required to develop new and effective
treatment strategies to deal with this emerging issue. Our present
study incorporates the evaluation of wound healing effects of 50%
ethanol extract of Ocimum sanctum (OSE) in streptozotocin
(45mg/kg)-induced diabetic rats with concurrent wound ulcer. The
animals showing diabetes (Blood glucose level >140 and
Abstract: Leonotisleonurus a shrub indigenous to Southern
Africa is widely used in traditional medicine to treat a variety of
conditions ranging from skin diseases and cough to epileptic fits and
‘heart problems’. Studies on the aqueous extract of the leaves have
indicated cycloxegenase enzyme inhibitory activity and an
antihypertensive effect.
Five methanol leaf extract fractions (MLEa - MLEe) of L.
leonurus were tested on anaesthetized normotensive male Wistar rats
(AWR) and isolated perfused working rat hearts (IWH). Fraction
MLEc (0.01mg/kg – 0.05mg/kg) induced significant increases in BP
and HR in AWR and positive chronotropic and inotropic effects in
IWH (1.0mg/ml – 5.0mg/ml). Pre-administration of atenolol
(2.0mg/kg) and prazosin (60μg/kg) significantly inhibited MLEc
effect on HR and MAP respectively in vivo, while atenolol
(7.0mg/ml) pre-perfusion significantly inhibited MLEc effect in vitro.
The hypertensive effect of MLEc is probably via β1agonism.
Results also indicate the presence of multiple cardioactive
compounds in L. leonurus.