Interpenetrating polymer network hydrogel beads of pectin and sodium carboxymethyl xanthan were prepared by ionotropic gelation with Al(+3) ions and covalent cross-linking with glutaraldehyde for sustained delivery of diltiazem hydrochloride. Fourier transform infrared spectroscopy, X-ray diffraction, differential scanning colorimetry and scanning electron microscopy were used to characterise the hydrogel beads. The swelling of the hydrogel and the release of drug were relatively low in pH 1.2 buffer solutions. However, higher swelling and drug release were observed in pH 6.8 buffer solutions. The carboxyl functional groups of hydrogels undergo ionisation and the osmotic pressure inside the beads increases resulting in higher swelling and drug release in higher pH. The release of drug depends on concentration of polymer, amount and exposure time of cross-linker and drug content in the hydrogel matrices. The present study indicated that the hydrogel beads minimised the drug release in pH 1.2 buffer solutions and to prolong the drug release in pH 6.8 buffer solutions.
A new robust, simple and economic high performance thin layer chromatographic method was developed for simultaneous estimation of L-glutamic acid and γ-amino butyric acid in brain homogenate. The high performance thin layer chromatographic separation of these amino acid was achieved using n-butanol:glacial acetic acid:water (22:3:5 v/v/v) as mobile phase and ninhydrin as a derivatising agent. Quantitation of the method was achieved by densitometric method at 550 nm over the concentration range of 10-100 ng/spot. This method showed good separation of amino acids in the brain homogenate with Rf value of L-glutamic acid and γ-amino butyric acid as 21.67±0.58 and 33.67±0.58, respectively. The limit of detection and limit of quantification for L-glutamic acid was found to be 10 and 20 ng and for γ-amino butyric acid it was 4 and 10 ng, respectively. The method was also validated in terms of accuracy, precision and repeatability. The developed method was found to be precise and accurate with good reproducibility and shows promising applicability for studying pathological status of disease and therapeutic significance of drug treatment.
Oroxylum indicum Vent. (O. indicum) is a tree commonly called Indian trumpet tree found in tropical countries, such as India, Japan, China, Sri Lanka, Malaysia. The chemical constituents obtained from different parts of plant include baicalein-7-O-diglucoside (Oroxylin B), baicalein-7-O-glucoside, chrysin, apegenin, prunetin, sitosterol, oroxindin, biochanin-A, ellagic acid, baicalein and its 6- and 7-glucuronides, scutellarein, tetuin, antraquinone and aloe-emodin. Various parts of the plant are used in Ayurveda and folk medicine for the treatment of different ailments such as cancer, diarrhea, fever, ulcer and jaundice. Recent in vivo and in vitro studies have indicated its antiinflammatory, antiulcer, hepatoprotective, anticancer, antioxidant, photocytotoxic, antiproliferative, antiarthritic, antimicrobial, antimutagenic and immunostimulant properties. Exhaustive literature survey reveals that there are some activities which are still not proven scientifically. This article is an attempt to compile an up-to-date and comprehensive review on O. indicum covering its traditional and folk medicinal uses, phytochemistry and pharmacology.
Cinnamon leaf oil contains a high percentage of eugenol and has antimicrobial, antioxidant and antiinflammatory properties. However, the undiluted oil can cause irritation to the skin. Therefore, the aims of this study were to develop and evaluate cinnamon leaf oil nanocream using palm oil. Nanocream base was prepared using different ratios of oil, surfactants and water. The surfactant used were mixture of Tween 80:Carbitol or Tween 80:Span 65 at different hydrophile-lipophile balance values. The pseudoternary phase diagrams were constructed to identify the nanocream base areas and the results showed that the nanocream bases using Span 65 as co-surfactant produced bigger cream area. Fifteen formulations using mixtures of Tween 80:Span 65 were further evaluated for accelerated stability test, droplet size, zeta potential, rheological properties and apparent viscosity. The nanocream base which had an average droplet size of 219 nm and had plastic flow with thixotropic behavior was selected for incorporation of 2% cinnamon leaf oil. The nanocream containing cinnamon leaf oil had the average size of 286 nm and good rheological characteristics. The in vitro release study demonstrated that eugenol as the main constituent of cinnamon leaf oil was released for about 81% in 10 h. The short-term stability study conducted for 6 months showed that the cinnamon leaf oil nanocream was stable at a temperature of 25° and thus, cinnamon leaf oil nanocream is a promising natural based preparation to be used for topical application.
Inappropriate initial antibiotics for pneumonia infection are usually linked to extended intensive care unit stay and are associated with an increased risk of mortality. This study evaluates the impact of inappropriate initial antibiotics on the length of intensive care unit stay, risk of mortality and the co-predictors that influences these outcomes. This retrospective study was conducted in an intensive care unit of a teaching hospital. The types of pneumonia investigated were hospital-acquired pneumonia and ventilator-associated pneumonia. Three different time points were defined as the initiation of appropriate antibiotics at 24 h, between 24 to 48 h and at more than 48 h after obtaining a culture. Patients had either hospital-acquired pneumonia (59.1%) or ventilator-associated pneumonia (40.9%). The length of intensive care unit stay ranged from 1 to 52 days (mean; 9.78±10.02 days). Patients who received appropriate antibiotic agent at 24 h had a significantly shorter length of intensive care unit stay (5.62 d, P<0.001). The co-predictors that contributed to an extended intensive care unit stay were the time of availability of susceptibility results and concomitant diseases, namely cancer and sepsis. The only predictor of intensive care unit death was cancer. The results support the need for early appropriate initial antibiotic therapy in hospital-acquired pneumonia and ventilator-associated pneumonia infections.
The antibacterial activity of the methanol extract of Wedelia chinensis leave was studied and tested against three pathogenic Gram positive bacteria (Bacillus cereus, B. subtilis and Stapylococcus aureus) and three pathogenic Gram negative bacteria (Escherichia coli, Proteus rettgeri and Pseudomonas aeruginosa) by the disk diffusion assay and broth dilution methods. The extract exhibited favourable antibacterial activity against the bacterial cells but was more potent against Gram positive bacteria with the minimum inhibition concentration of 3.12 to 6.25 mg/ml compared to the Gram negative bacteria which had minimum inhibition concentration values of 25 mg/ml. The time-kill study suggested that the extract possessed bactericidal properties at higher concentrations and eradicated the growth of bacterial cells. The major abnormalities occurred to the bacterial cells after exposed to the extract were complete alterations in their morphology and collapsed of the cells beyond repair. The methanol extract of W. chinensis may be an effective antibacterial agent to treat bacterial infections.
The aim of this study was to enhance the dissolution rate of efavirenz using solid dispersion systems (binary and ternary). A comparison between solvent and fusion method was also investigated. Solid dispersions of efavirenz were prepared using polyethylene glycol 8000, polyvinylpyrrolidone K30 alone and combination of both. Tween 80 was incorporated to obtain a ternary solid dispersion system. Dissolution tests were conducted and evaluated on the basis of cumulative percentage drug release and dissolution efficiency. Physicochemical characterizations of the solid dispersions were carried out using differential scanning calorimetric, powder X-ray diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy. Dissolution was remarkably improved in both systems compared to pure efavirenz (P<0.05). An optimum ratio was identified at a drug:polymer of 1:10. Incorporation of Tween 80 to 1:10 formulations formed using solvent method showed further improvement in the dissolution rate. Physicochemical characterization results suggested that efavirenz existed in the amorphous form in all the solid dispersion systems providing evidence of improvement in dissolution. No statistically significant difference (P>0.05) in dissolution was observed between the two methods. Binary and ternary solid dispersion systems both have showed a significant improvement in the dissolution rate of efavirenz. Formulations with only polyvinylpyrrolidone K30 showed best dissolution profile and 1:10 was identified as an optimum drug-polymer weight ratio.
Hematophagous animals including leeches have been known to possess biologically active compounds in their secretions, especially in their saliva. The blood-sucking annelids, leeches have been used for therapeutic purposes since the beginning of civilization. Ancient Egyptian, Indian, Greek and Arab physicians used leeches for a wide range of diseases starting from the conventional use for bleeding to systemic ailments, such as skin diseases, nervous system abnormalities, urinary and reproductive system problems, inflammation, and dental problems. Recently, extensive researches on leech saliva unveiled the presence of a variety of bioactive peptides and proteins involving antithrombin (hirudin, bufrudin), antiplatelet (calin, saratin), factor Xa inhibitors (lefaxin), antibacterial (theromacin, theromyzin) and others. Consequently, leech has made a comeback as a new remedy for many chronic and life-threatening abnormalities, such as cardiovascular problems, cancer, metastasis, and infectious diseases. In the 20(th) century, leech therapy has established itself in plastic and microsurgery as a protective tool against venous congestion and served to salvage the replanted digits and flaps. Many clinics for plastic surgery all over the world started to use leeches for cosmetic purposes. Despite the efficacious properties of leech therapy, the safety, and complications of leeching are still controversial.
The antidiarrhoeal effect of the water extract of Melastoma malabathricum Linn. (Melastomataceae) leaves were investigated by employing four experimental models of diarrhea in Swiss mice. Melastoma malabathricum water extract treated mice showed significant reduction in the fecal output and protected them from castor oil-induced diarrhoea. The extract also reduced the intestinal fluid secretion induced by magnesium sulphate and gastrointestinal motility after charcoal meal administration in the mice. No mortality and visible signs of general weakness was observed in the mice following the test extract administration up to 2000 mg/kg dose.
The aim of the present work was to investigate the preparation of microspheres as potential drug carriers for proteins, intended for controlled release formulation. The hydrophilic bovine serum albumin was chosen as a model protein to be encapsulated within poly(D,L-lactide-co-glycolide) (50:50) microspheres using a w/o/w double emulsion solvent evaporation method. Different parameters influencing the particle size, entrapment efficiency and in vitro release profiles were investigated. The microspheres prepared with different molecular weight and hydrophilicity of poly(D,L-lactide-co-glycolide) polymers were non porous, smooth surfaced and spherical in structure under scanning electron microscope with a mean particle size ranging from 3.98 to 8.74 mum. The protein loading efficiency varied from 40 to 71% of the theoretical amount incorporated. The in vitro release profile of bovine serum albumin from microspheres presented two phases, initial burst release phase due to the protein adsorbed on the microsphere surface, followed by slower and continuous release phase corresponding to the protein entrapped in polymer matrix. The release rate was fairly constant after an initial burst release. Consequently, these microspheres can be proposed as new controlled release protein delivery system.