International Journal of Drug Delivery
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Determination of Bosentan in Pharmaceutical Dosage Forms by High Performance Liquid Chromatography
Get PDFA simple and sensitive high performance liquid chromatographic method is developed for the estimation of bosentan in pharmaceutical dosage forms. Chromatographic separation of the drug was achieved with an Thermo Scientific C18 column (250 mm × 4.6 mm I.D., 5 μm particle size) analytical column using ammonium bicarbonate (pH was adjusted to 5.0 with phosphoric acid) and acetonitrile (70:30 v/v) as mobile phase. The instrumental settings are flow rate of 1.0 ml/min, column temperature at 25±1°C, detector wavelength of 220 nm and the run time was 5 min. The retention time of the drug was 1.986 min. The developed method shows linearity over a range of 5-100 μg/ml of bosentan with correlation coefficient of 0.9991. The relative standard deviation is less than 1.5%. The proposed method was found to be suitable and accurate for quantitative determination of bosentan in pharmaceutical dosage forms
Solid Dispersions: A tool for improving the Solubility and Dissolution of Metronidazole
Get PDFMetronidazole is a broad spectrum antibiotic. It is sparingly soluble in water but has oral bioavailability of 93-95%. So solid dispersions (SDs) containing metronidazole was prepared in different ratios (1:1, 1:2 and 1:5) and using different carriers like dextrose, citric acid, polyethylene glycol (PEG-4000) and polyvinylpyrrolidone (PVP). Fusion or melting method was used for SD containing dextrose and citric acid and Solvent evaporation method was used for SD containing PVP and PEG-4000. The solubility studies revealed that solubility of metronidazole was enhanced to manifolds. Best result was exhibited when drug carrier ratio is in the order of 1:5>1:2>1:1. Among the different carriers, the solubility and dissolution was increased to maximum in case of PVP and PEG and almost 100 % drug released within 1 hour. The development of solid dispersions was further confirmed by DSC and XRD
Formulation and Evaluation of Taste-Masked Orally Disintegrating Tablets of Nicergoline based on β-cyclodextrin Inclusion Complexation
Get PDFComplexation of nicergoline with β-cyclodextrin (β-CD) into an inclusion complex has been used successfully to improve the drug’s solubility, dissolution rate and hence per oral absorption. In addition, masking of the bitter taste was also achieved. The preparation of inclusion complexes was performed using two different techniques, namely; physical mixing and kneading. The apparent stability constant (Kc) of the complex was calculated from the phase solubility analysis. Compatibility of nicergoline and β-CD complex with disintegrants and superdisintegrants were evaluated using powder x-ray diffractometry (PXRD), differential scanning calorimetry (DSC), and fourier transform infrared spectroscopy (FTIR). The morphology of complex particles was studied using scanning electron microscopy. Pharmaceutical characterization confirmed that all additives were compatible with the drug and no signs of physical or chemical interaction were detected. Orodispersible tablets (ODTs) of nicergoline complexed with β-CD and containing 7-9 % camphor had rapid disintegration time (7-12 seconds) and fast drug release profiles (90-100 % in 10 minutes). Therefore, nicergoline ODTs are considered a valuable choice dosage form with improved per oral absorption and taste acceptability
Lipid shell modified with combination of lipid and phospholipids in solid lipid nanoparticles for engineered specificity of paclitaxel in tumor bearing mice.
Get PDFPaclitaxel (PTX) is an anticancer drug belonging to the class of Taxan. It is active against various types of carcinomas. The marketed formulation of paclitaxel is associated with deleterious effects with lack of specificity to tumor. Solid lipid nanoparticles (SLN) are colloidal carriers extensively studied and developed for there potential uses especially for controlled release and site specificity. The present study was designed to develop a formulation of PTX in the form of SLN to be administered via IV route with improved tumor specificity, in which the lipid shell was modified by using combination of lipid with phospholipids. Total eight formulations were prepared and were characterized by various in vitro and in vivo parameters. The microemulsification method was used for the preparation of SLN.The production yield of resulting process for all SLN was high. Average particle size was ranged between 209 nm to 385 nm. The developed PTX-SLN showed high percentage entrapment efficiency. The zeta potential values showed the good stable feature of the sln.The in vitro dissolution study showed that drug release was more retarded and was found to dependent on concentration of lipids employed. In vitro cytotoxicity study was performed on MCF-7 cancer cell line, which showed that formulation G2 is having more potentiating effect on cancer cell line. Tissue targeting study and tumor growth inhibition studies were performed on mice where the PTX loaded SLN from batch G2 shown more promising outcome. Results obtained from this study indicated strongly that developed SLN are having potential as an efficient drug delivery system for paclitaxel
Comparative pharmacokinetic study of two prokinetic drugs in the form of buccal gels against their market products
No full textThis study was to investigate the efficiency of buccal dosage forms to deliver poor orally absorbed drugs. Two buccal gel formulations containing two gastrokinetic drugs with low oral bioavailability; domperidone and mosapride citrate; were tested against their market products. Twenty-four volunteers were enrolled in this study divided into two groups in a single dose, two treatment and two periods cross over design. Both buccal formulations achieved high relative bioavailabilities (Frel) compared to the market products where buccal gel of domperidone achieved Frel of 202% and buccal gel of mosapride citrate achieved 162%. The study reveals the importance of the buccal route for administration of poorly absorbed drugs from the gastrointestinal tract
Design and evaluation of oral delivery formulations based on dextran with theophylline
Get PDFThe purpose of this investigation was to develop and evaluate different oral drug release delivery formulations namely, tablets and capsules, based on dextran, in order to determine how the quantity of dextran and the form-structure of the delivery systems influence drug release and release mechanisms. Theophylline was used as the model drug. All matrix tablets and one capsule formulation demonstrated sustained release profiles. The amount of dextran and its properties (particularly erosion) along with the form of the preparation were found to considerably affect the performance of the system, the release profiles and the mechanism of release. In all cases an increase in the quantity of dextran resulted in a decrease in the release rate indicating that acted as a kind of barrier and hindered the release of drug molecules from these formulations. Significant differences were also observed among the different preparations under examination, with the matrix tablets exhibiting the slowest drug release followed by the capsules. By altering the dextran/theophylline ratio or the form of the preparation it is possible to obtain appropriate drug release. Consequently dextran appears to be a versatile material and a promising vehicle for the preparation of various oral sustained release drug delivery systems and relevant devices.
Formulation and Evaluation of Gastro Retentive Mucoadhesive Sustained Release Pellets of Acyclovir
Get PDFAcyclovir is an antiviral drug, belonging to the deoxyguanosine family, widely prescribed for the treatment of herpes simplex viral infections, as well as in the treatment of herpes zoster (shingles). Oral bioavailability of acyclovir is very low (10–20%) owing to its first pass metabolism with elimination half-life (t1/2) of 2-3 h. It has absorption window in upper gastrointestinal tract. Due to its rapid elimination from site of absorption and short biological half life, sustained release formulation system for acyclovir is advantageous. In this study, gastro retentive muco-adhesive SR pellets of acyclovir was prepared using HPMC K 100M as matrix former and Sodium CMC as mucoadhesive polymer by extrusion spheronization technique. Acyclovir pellets prepared with higher concentration of HPMC (batch G) showed in vitro drug release for 12 h with sufficient mucoadhesion strength and ex vivo resident time. Release kinetic studies indicated that drug release data had best fit to Higuchi’s model. In-vivo studies in rat model proved that relative bioavailability of acyclovir SR pellets get increased by 1.98 fold as compared plain drug suspension. The optimized formulation batch G was found to be stable during six months accelerated stability period
Development and Evaluation of Transdermal Patches of Quetiapine fumerate for the treatment of psychosis
Get PDFThe aim of the present study was to formulate and evaluate the transdermal patches of an antipsychotic drug Quetiapine fumerate (QF) for the treatment of psychosis and schizophrenia. The transdermal patches was prepared by the solvent evaporation method using hydroxy propyl methyl cellulose (HPMC) and ethyl cellulose (EC) in five different ratios 1:0, 2:1, 1:1, 1:2, 0:1. The PEG-400 and DMSO were used as plasticizers and permeation enhancer respectively to enhance the permeability of the drug. The FTIR studies showed no evidence of incompatibility between the drug and the polymers. The prepared patches were evaluated for various parameters like thickness, weight variation, folding endurance, percentage moisture uptake, percentage moisture content, drug content and in-vitro drug release. The results concluded that the formulation F2 (with HPMC and EC in 2:1 ratio) showed 80.89% in drug release during in-vitro studies after 24 hours. With the incorporation of PEG-400 and DMSO smooth, transparent and flexible film were produced
Evaluation of the Liquisolid Compacts Using Response Surface Methodology
Get PDFLiquisolid Compacts technique has potential to develop sustained release formulations. It involves conversion of liquid drug (either solution or suspension) in non-volatile solvent into free-flowing, non adherent, dry looking and readily compressible powder. In the present work, an attempt was made to develop such formulation of Diltiazem HCl and evaluation using Response surface methodology. Liquisolid compacts were prepared by dissolving Diltiazem HCl in Polyethylene Glycol 400. Then a binary mixture of carrier-coating material, Avicel and Aerosil, was added to liquid medication under continuous mixing in mortar. The HPMC K4M was used as adjuvant for sustaining the drug release. The pre-compression studies for all the formulations were also carried out. The Liquisolid compacts were evaluated in-vitro dissolution studies. The experimental data was evaluated using Design Expert Software. The % Drug Concentration, ratio of Carrier to Coating material and amount of HPMC K4M are taken as three factors. Response Surface methodology was used to study the influence of the each factor on the response. The present investigation showed that Polyethylene Glycol 400 has important role in release retardation of drug in Liquisolid compacts. The reduction in Tg can be reason for same. The Response surface methodology showed that all the factors were significantly affect the release at 16 hrs.
Targeted Drug Delivery System using Photovoltaic Devices
No full textAdvances in surgical techniques and scientific research, including the development of new cytotoxic drugs and hormonal therapies, have resulted in better treatment options for cancer patients. Despite such encouraging progress, systemic oral or intravenous administration can cause severe cytoxicity, which limits the therapeutic potential of anticancer drugs. Recent discovery using solar cells for targeted drug delivery will pave the way for the development and introduction of innovative targeted therapies with improved efficacy. A photovoltaic cell holds opposite charges on its surfaces, serve as a new drug delivery system to carry cancer chemotherapeutic drugs or substances and release them when the charge intensity or polarity changes upon external photo stimulation or laser source. In this new strategy using photovoltaic device, a hypothesis is proposed to serve as a new drug delivery method. Positively charged Poly-L-Lysine and negatively charged Bovine Serum Albumin are attached the negative side and positive side of a solar cell respectively. Experimental data reveals that the PV cells significantly can release the charged molecules upon external photo stimulation, which suggests the PV has potential to be used as a new drug delivery system to carry cancer chemotherapeutic drugs