International Journal of Drug Delivery
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Targeting effect of folate on cancer cell through curcumin carrier nano-system
Get PDFFolate receptor (FR) is well known for its overexpression on surface of various cancer cell lines, which is identical to normal tissue. Folic-based targeting drug delivery systems, therefore, are one of the most effective targeting carriers that effectively bind to FR up-regulated cancer cells. Curcumin was used both for labeling and chemotherapy. The materials were characterized and structurally confirmed by FT-IR spectra, fluorescent images and FE-SEM images. Bioassays were conducted on HeLa and HT29 cancer cell lines after 4 and 12 hours. Results show that folic acid significantly enhanced both targeting efficiency and internalization of curcumin to FR-expressing cancer cells
Enhancement of solubility and oral bioavailability of poorly soluble drug Valsartan by novel solid self emulsifying drug delivery system
Get PDFThe main objective of present work was to prepare a solid SEDDS for enhancement of oral bioavailability of Valsartan, poorly water soluble drug. The solubility of the drug was determined in various vehicles. A pseudo ternary phase diagram was constructed to identify the self-micro emulsification region. Further, the resultant formulations were investigated for clarity, phase separation, globule size, effect of pH and dilutions and freeze-thaw stability. The optimized SMEDDS (F4) formulation of Valsartan contained Capmul MCM (Oil), Kolliphor HS 15 (Surfactant) and PEG 400 (Co-surfactant). This optimized formulation was converted in to solid SEDDS by adding required quantity of Neusilin US2 as adsorbing agent used for in vitro dissolution and bioavailability assessment. The oral bioavailability of Valsartan from solid SEDDS was 1.6-fold higher compared to that of Valsartan suspension in rats, suggesting a significant increase (p < 0.05) in oral bioavailability of Valsartan from solid SEDDS
Demonstration of Multivariate Data Analysis for the Development of nanoemulsions containing Active Herbal Principle of Boswellia serratta for Topical Application
Get PDFInsilico modeling of chitosan as a drug delivery system
Get PDFComputational modeling of polymeric nanoparticles as drug carriers have been extensively studied due to their varied functionalities, tunable structures and the capability of controlled drug release. Nano particulate polymeric drug delivery systems enable a cell specific targeting with negligible side effects and drug release based on change in physiological conditions. Eight common polymers are modeled and the various properties have been predicted. ADMET, QSAR, thermodynamic and electronic properties have been predicted and compared using SAR as well as quantum mechanical density functional methods. Comparison of the predicted properties suggests that chitosan, which is a natural polymer and has some advantages over others is a promising drug carrier candidate for tumor
Formulation and in-vitro evaluation of fast dissolving tablets containing a poorly soluble antipsychotic drug
Get PDFThe aim of the present study was to formulate olanzapine fast dissolving tablets (FDT). Olanzapine is a poorly water soluble drug that undergoes first pass metabolism in liver resulted in low oral bioavailability. The water solubility is enhanced by formation of co-amorphous dispersion by solvent evaporation under vacuum method using a polycarboxylic acid (ascorbic acid) as a coformer in two different molar ratios (1:1 and 1:2). The prepared systems were evaluated using differential scanning calorimeter (DSC), Fourier Transform Infra-Red analysis (FTIR), X-ray powder diffraction (XRPD), Scanning electron microscopy (SEM) and saturated solubility. The co-amorphous dispersion system in a molar ratio 1:2 is higher in solubility than 1:1, so it was selected for incorporation into FDT formulation. Compatability study between olanzapine and different tablet excipients including DSC and FTIR showed that the drug is compatible with the selected tablet excipients. Direct compression method was used in FDT formulations using different types and concentrations of superdisintegrants. FDTs were evaluated for weight variation, hardness, friability, wetting time, drug content uniformity, invitro disintegration time and invitro dissolution study. All the prepared FDTs were complied with the compendia standards. F3 and F8 showed lower disintegration time and higher percent of drug dissolved, so they were selected for stability study. After storage for 3 months at 30ºC at 65% relative humidity, both formulations were physically stable regarding color and integrity and had only minor increases in disintegration time, drug content and friability after three months’ storage. The results indicate that olanzapine FDT tablets may serve as a successful strategy for enhancing the bioavailability of olanzapine
Pharmacokinetic interactions between concomitantly administered Metformin and Itopride in rats
Get PDFGastroparesis is a syndrome characterized by delayed gastric emptying, in the absence of mechanical obstruction of the stomach. Diabetes mellitus (DM) is responsible for almost one third of cases of gastroparesis. Gastroparesis typically develops after at least 10 years of evolution of DM, and often is associated with other complications. The present study aimed to investigate the safety, reliability of Metformin and possible drug interaction with Itopride when they were administered as combination treatment. The study was conducted on healthy Wistar and streptozotocin induced diabetic rats. A simple and sensitive high performance liquid chromatographic method was developed for the simultaneous estimation of Metformin and Itopride in rat plasma and also to estimate possible pharmacokinetic parameters of these drugs after oral administration. There was no significant difference in the Metformin alone and combination with Itopride and Itopride alone and combination with Metformin on day 1 and day 8 respectively. There is no significant change in tmax, cmax, AUC (0 – t) and AUC (o-inf), t½, Cl/f and V/f on day 1 and day 8 respectively in both diabetic and healthy rats. From the above results it can be concluded that the concurrent administration of these two drugs have potential benefit in the treatment of Diabetes and Gastroparesis. In addition, due to their insignificant pharmacokinetic interaction the combinational therapy can be safe and highly advantageous in Gastro paresis patients with diabetes.
Probiotics: Making a Niche as Promising Health Supplements and Complementary Medicines
No full textHippocrates once quoted, “Let food be thy medicine and medicine be thy food,” this ancient statement has certainly become a belief in today’s scenario. The live microbial food supplements, called as Probiotics (known to have beneficial effects on human health in various ways) are widely used now a days. Owing to their potential as alternative or complementary therapeutic agent in combating large number of pathological conditions and ability to enhance immune response, an overwhelming interest have developed for probiotics in medical field. Probiotics, being widely used around the globe by consumers and in clinical practice, a thorough understanding of the risks and benefits related to their use are of vital importance. This review addresses the concept of probiotics, historical development, their sources and probable mechanisms of action, clinical applications along with associated risks and contraindications related to the use of probiotics
Preparation and in vivo evaluation of SMEDDS containing Nevirapine for bioavailability improvement
Get PDFNevirapine has been formulated in lipid-based system, a Self Emulsifying Drug Delivery System (SEDDS) to target the drug to lymphoid organs where HIV-1 virus resides in large population. Nevirapine SEDDS were formulated for enhancement of solubility, dissolution rate and oral bioavailability of model drug Nevirapine. Fourteen formulations were prepared using different oils, surfactants and co-surfactants. A pseudo ternary phase diagram was constructed to identify the self-micro emulsification region. Further, the resultant formulations were investigated for clarity, phase separation, drug content, % transmittance, globule size, freeze-thaw stability and in vitro dissolution studies. On the basis of dissolution profile and other above mentioned studies, F4 was found to be the best formulation of Nevirapine SEDDS which contains Capryol 90 (Oil), Tween 80 and PEG 600 as surfactant co-surfactant respectively. In vivo studies revealed that the oral bioavailability of Nevirapine from SEDDS was 2-fold higher compared to that of pure Nevirapine suspension in rats, suggesting a significant increase in oral bioavailability of Nevirapine from SEDDS formulation. The higher bioavailability might be due to the enhanced solubility of Nevirapine by SEDDS formulation
Immunomodulatory effect of Ocimum gratissimum Linn. leaf extract on a Common Fish Clarias batrachus Linn.
Get PDFThe use of immunostimulants for the prevention of disease in fishes is considered as an attractive and promising area in the field of aquaculture. Immunostimulants are valuable for the prevention and control of fish diseases in aquaculture as they represent an alternative and supplementary treatment to vaccination. They also have additional effects such as growth enhancement and increase in the survival rates of the fishes under stress. Certain medicinal plants are believed to promote positive health and maintain organic resistance against infection by re-establishing body equilibrium and conditioning the body tissues. The present study was designed to evaluate the immunostimulant potential of crude extract of Ocimum gratissimum leaf on fish Clarius batracus in both specific and non specific levels. Our results showed that there is not a significant decrease in the amount of Glucose and cholesterol at concentration 2.5% but there is a significant reduction in glucose amount at 5% in comparison to control. But a significant increase was seen the RBC, WBC, Serum protein and globulin at 2.5% and 5% concentrations of crude extracts in both the 15 and 30 days of treatments in the blood of the fish. It may be due to the presence phenolic compounds like flavonoids, terpenoids steroids, alkaloids etc. Based on the results it is appropriate to conclude that the plant extract of Ocimum gratissimum may act as a potent Immunostimulant in Clarias batrachus
Pharmacokinetic study of Piperine in Wistar rats after oral and intravenous administration
No full textTo evaluate the potential of piperine as a therapeutic agent, we considered whole animal studies to characterize its pharmacokinetics (PK) in Wistar rats after oral and intravenous (i.v.) administration, using high performance liquid chromatography (HPLC). This study will enable in determination of piperine exposures needed to predict the dose regimen for clinical trials to test the proposed mechanism of action in enhancing the therapeutic efficacy of the concurrently administered drugs. A single dose of piperine was administered intravenously (10 mg/kg) by jugular vein cannulation and orally (20 mg/kg) by oral gavage in male Wistar rats. Serial blood samples were collected and plasma piperine concentrations were determined using HPLC. After intravenous administration the apparent terminal half-life (7.999 hr), apparent steady state volume of distribution (7.046 L/kg) and total body clearance (0.642 L/kg/hr) were calculated. After oral administration the apparent terminal half-life (1.224 hr), apparent steady state volume of distribution (4.692 L/kg) and total body clearance (2.656 L/kg/hr) were calculated. The peak plasma concentration of piperine in plasma after oral administration was found to be 0.983 μg/ml, occurred approximately 2 hr post-dose. The AUC(0-∞) of Piperine after oral and intravenous administration in rats were found out to be 7.53 μg*hr/ml and 15.6 μg*hr/ml, respectively. The absolute oral bioavailability of piperine was found to be 24%. From the results of the experiment, it can be concluded that piperine achieves extensive distribution because of its large volume of distribution in the body. These studies are useful in interpreting preclinical efficacy studies of Piperine & predicting human pharmacokinetic through scaling technique