International Journal of Drug Delivery
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Biosynthesise, Characterization and Antibacterial activity of Silver nanoparticles by Soil fungi Pencillium sps.
Microbial synthesis of nanoparticles is an eco-friendly green chemistry approach that correlates with nanotechnology and microbial biotechnology. Exposure of fungal biomass to aqueous 1Mm AgNO3 solution resulted in the reduction of the metal ions by the nitrate reductase enzyme present in the cell wall membranes and formation of silver nanoparticles. Synthesized silver nanoparticles were characterized using UV-visible spectroscopy, SEM, TEM and FTIR analysis. The synthesed silver nanoparticles were exhibited an excellent antibacterial activities against both Gram negative and Gram positive pathogenic bacterial strains which causes the diseases in human being
Statistical optimization of floating-bioadhesive drug delivery system for risedronate sodium: In vitro, ex vivo and in vivo evaluation
AbstractThe objective of the present investigation was to apply statistical design for the development of risedronate sodium floating-bioadhesive tablets (RSFBT) employing response surface methodology (RSM). A central composite design (CCD) was developed using Design of Expert (DOE) software to study the effect of formulation variables on the drug delivery system. The RSFBT were prepared by direct compression using hydroxy propyl methyl cellulose (HPMC K100M) as release retardant; carbopol (CP 974P) as bioadhesive polymer and sodium bicarbonate (NaHCO3) as a gas-former. The quantities of HPMC K100M (X1), CP 974P (X2) and NaHCO3 (X3) were taken as independent variables and percentage drug release at 2 h (Q2), 6 h (Q6) and 12 h (Q12), floating lag time (FLT), total floating time (TFT) and bioadhesive strength (BS) were selected as responses. The BS was determined using porcine gastric mucosa. In all 15 formulations were prepared and studied. The results of the CCD indicated that high levels of both X1 and X3, and low level of X2 were required for the preparation of RSFBT. Further, a good correlation was observed between predicted and experimental values of the independent variables selected for this study. The drug release profiles of all the formulations were fitted into zero-order, first-order, Higuchi and Peppas models. The optimized formulation followed the Peppas model with a non-Fickian diffusion mechanism. The statistically optimized formulation (RSFBTsopt) was found to be physically stable when stored at 40 ± 2 oC/75 ± 5% RH for 3 months. In vivo evaluation of RSFBTsopt, BaSO4-loaded tablets revealed a mean gastric retention time of 5 ± 0.86 h (n=3) in healthy volunteers.
In-vitro Modeling of the Release Kinetics of Micron and Nano-Sized Polymer Drug Carriers
This article reviews in-vitro modeling of the release kinetics of hydrophobic drugs encapsulated by polymeric materials. Major continuum models along with their assumptions and limitations for micron-sized systems will be considered. The dependence on the swelling and degradation for such systems will also be discussed. As polymer micelles have gained popularity in the past decades, applications and limitations of continuum models to such nano-sized systems will be examined. A different approach based on molecular dynamics simulation will be introduced
Effect of calcium phosphate compound (MZF-CaP) with and without fluoride in preventing bone loss in ovariectomized rats
Zinc (Zn) has been shown to inhibit osteoclast differentiation, promote osteoblast activity, and enhance the bone formation. Zinc-containing calcium phosphate (Zn-TCP) implanted in rabbit femoral defect was demonstrated to stimulate bone formation. Other studies demonstrated that calcium phosphate compounds (MZF-CaP) incorporating magnesium (Mg2+), zinc and fluoride (F-) when administered either by injection or orally were effective in preventing bone loss (osteoporosis) induced by estrogen deficiency (ovariectomy) in a rat model. The objective of the present study was to investigate the preventive effect of similar compound, with F (MZF-CaP-L, MZF-CaP-H) and without F (MZ-CaP-L), when injected in ovariectomized (OVX) rats. MZF-CaP-L and MZ-CaP-L were prepared by precipitation at 90oC and MZF-CaP-H was prepared by sintering MZF-CaP-L at 900oC. The release of the ions from acidic buffer was determined. Suspensions of Zn-TCP, MZF-CaP-H, MZF-CaP-L and MZ-CaP-L (617 μg in 0.2 ml of 1% sodium alginate saline solution) were injected intramuscularly under anesthesia into 5-week-old OVX rats on Zn-deficient diet. One week after surgery, bone mineral density (BMD) and bone mineral content (BMC) of the rat femurs were measured using X-ray CT. The injections and X-ray CT and Zn ion plasma measurements were repeated every week for 12 weeks. The rats were sacrificed and the femurs removed after 12 weeks. Bone mechanical strength was evaluated using the three-point bending test. MZ-CaP-L (without F), compared to the other compounds, showed the highest increase in the Zn2+ ion plasma concentration, and the highest BMD, BMC and mechanical strength
Preparation and evaluation of oral controlled release mucoadhesive Microspheres of Ketorolac Tromethamine
Recently, lot of emphasis is being laid on oral controlled release multiple unit particulate (MUP) dosage forms, for their significant and potential benefits. Ketorolac tromethamine (KTM) is a potent non-narcotic analgesic and anti-inflamatory drug administered orally in multiple divided doses (10 mg four times a day) for the management of mild to moderate post-operative pain. KTM’s short biological half-life demands frequent administration of the drug leading to poor patient compliance and inadequate pain management. Hence, the present investigation was undertaken to develop and evaluate oral controlled release mucoadhesive microspheres by ionotropic gelation method using natural and biodegradable polymers such as sodium carboxy methyl cellulose (Na CMC) and sodium alginate (SA). The influence of various formulation factors on the drug entrapment efficiency, in vitro drug release, micromeritic properties, and mucoadhesion ability was investigated. Scanning electron micrographs of alginate beads loaded with drug exhibited rough surface morphology and sizes were found to be in the range of 842 to 1265 µm. Among all the formulations, the drug loaded microspheres of formulation CA6 showed the highest drug release retarding effect over a period of 8 hours. The drug-polymer compatibility studies and solid state properties were investigated by Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) X- Ray diffraction techniques (X-RD)
Aripiprazole loaded PLGA nanoparticles for controlled release studies: Effect of Co-polymer ratio
Poly (lactic-co-glycolic acid) nanoparticles loaded with Aripiprazole has been developed as a new therapeutic strategy to achieve its controlled release profile suitable for parenteral administration. Nanospheres composed of different lactic/glycolic acid ratios and drug compositions were synthesized and loaded with Aripiprazole by emulsion/solvent evaporation method and subsequently characterized by particle-size distribution, scanning electron microscopy, encapsulation efficiency and in–vitro drug release studies. Specific drug-polymer interactions are engineered by optimizing the lactide to glycolide ratio (L:G ratio) and including specific polymer hydrophobicity
comparative study of duration of analgesia with epidural bupivacaine & bupivacaine with tramadol in lower limb and lower abdominal surgeries
Background: The administration of local anaesthetic opioid mixtures neuraxially (particularly epidurally) is excellent for post-operative pain following abdominal, pelvic or orthopaedic procedures on lower extremities. The rational for this relatively new technique in post-operative pain management is a better quality of analgesia that can be achieved by systemically administered analgesics, a lower incidence of side-effects, improved surgical outcome and high levels of patient satisfaction. Therefore, this study was taken up to evaluate the efficacy of epidural opioids in the management of post-operative pain. Methods: A total of 80 patients group A 40& group B 40 ,of age 20-70yrs and ASAI &II, were selected for the study who were admitted for lower abdominal and lower limb surgeries . Group A was given epidural bupivacaine 0.5% & group B was given epidural bupivacaine 0.5% with tramadol 50mg. The onset & duration of analgesia, effects on the hemodynamics and side effects were evaluated and compared between two groups. Pain was evaluated on VAS scale and end point of study was when rescue analgesic was given on demand. Result- In this study, we used 1 ml (50 mg) tramadol with 0.5% bupivacaine (15-20 ml) through epidural route in patients for short surgical procedures in lower extremity & lower abdomen, it was found that mean duration of analgesia was significantly longer than the patients who received 15-20 ml 0.5% bupivacaine only through the same route. Key words- neuraxial, epidural, tramadol, bupivacain
Pharmacokinetics and biodistribution of zidovudine loaded in a solidified reverse micellar delivery system.
The aim of the research was to study the stability, release profile, pharmacokinetic and biodistribution properties of zidovudine (AZT)-solidified reverse micellar microparticulate. Lipid matrices formulated with Phospholipon® 90H and goat fat at ratios of 1:1, 2:1, 3:1 and 2:3 were used to prepare AZT-loaded SLM by melt dispersion followed by lyophilization. In vitro release studies of the drug were carried out using a sequential drug release method in both SGF (pH 1.2) and SIF (pH 7.2) while the in vivo drug release studies were carried out using Wistar albino rats. The result of our findings showed that the drug is compatibility with the lipid matrix with the 1:1 showing the most stable microparticle preparation which was then optimized. The formulations showed a concentration dependent increase in their concentration maximum (Cmax) with values of 116.05 µg/ml, 124.21 µg/ml, 128.95 µg/ml, 138.95 µg/ml and time to reach maximum concentration (Tmax) values of 5h, 8 h, 8 h, and 5 h for batches B1, B2, B3 and B4 containing 1 %, 2 %, 3 % and 5 % of AZT respectively. The area under curves (AUCs) of the microparticles formulated showed that the bioavailabilities of the microparticles were comparable to that of the conventional release tablet. The biodistribution studies of the microparticles in rats showed highest concentration of the drug in the liver with the least in the brain and higher biodistribution in various organs than pure AZT. The data suggested that SLM could be a promising drug delivery system to improve on the shortcomings of pharmacokinetics and bio-distribution properties of conventional AZT tablets like fluctuation in blood levels of the drug
VESICULAR DRUG DELIVERY SYSTEMS: A NOVEL APPROACH FOR DRUG TARGETING
The objective of the study is to evaluate the potential of novel vesicular drug delivery systems for drug targeting. Novel vesicular drug delivery systems aim to deliver the drug at a rate directed by need of body during the period of treatment, and channel the active entity to the site of action. Vesicular drug delivery systems have been used to improve the therapeutic index, solubility, stability and rapid degradation of drug molecule. Thus a number of novel vesicular drug delivery systems have been developed that allow drug targeting and sustained or controlled release of drug. The focus of this review is to discuss various lipoidal and non-lipoidal vesicles with special emphasis on targeting of drugs
Enhancing the solubility of Candesartan cilexetil-Inclusion Complexation using β-CD
Candesartan is primarily used as Anti-Hypertensive which is poorly soluble drug. It is available as salt form of cilexetil i.e., Candesartan cilexetil included under class II of Biopharmaceutical classification system whose bioavailability is 15%.The aim of the study is to enhance the solubility of the Candesartan cilexetil using inclusion complexation technique with β-CD as complexing agent. The complexation is evaluated both in liquid and solid state. The phase solubility profiles in different media (Millipore water, O.1N HCl, PBS 7.4) showed AL- type. Binary Mixtures of Candesartan cilexetil with CDs were prepared in the different ratios of 1molar experimentally with three different techniques (Physical Mixture, Kneading method, co-evaporation method). The complexes were analyzed using Fourier transform infrared spectroscopy and X-Ray diffractometery. From the analysis the complexation was confirmed in the co-evaporation and kneading method. Invitro studies were performed for all the ratios prepared by different methods in order to define the most appropriate ratio and preparation method. The percentage drug release from different mixtures, Marketed product and API is given as follows: Co evaporated Mixture > Kneaded Mixture > > >Physical Mixture≈ Marketed >AP