The Experts below are selected from a list of 1416 Experts worldwide ranked by ideXlab platform
Biswajit Mukherjee - One of the best experts on this subject based on the ideXlab platform.
-
Preparation and characterization of Tamoxifen Citrate loaded nanoparticles for breast cancer therapy.
International journal of nanomedicine, 2014Co-Authors: Ruma Maji, Niladri Shekhar Dey, Bhabani Sankar Satapathy, Biswajit Mukherjee, Subhasish MondalAbstract:Background Four formulations of Tamoxifen Citrate loaded polylactide-co-glycolide (PLGA) based nanoparticles (TNPs) were developed and characterized. Their internalization by Michigan Cancer Foundation-7 (MCF-7) breast cancer cells was also investigated.
-
Development of biodegradable polymer based Tamoxifen Citrate loaded nanoparticles and effect of some manufacturing process parameters on them: a physicochemical and in-vitro evaluation.
International journal of nanomedicine, 2010Co-Authors: Basudev Sahana, Kousik Santra, Sumit Basu, Biswajit MukherjeeAbstract:The aim of the present study was to develop nanoparticles of Tamoxifen Citrate, a non-steroidal antiestrogenic drug used for the treatment of breast cancer. Biodegradable poly (D, L- lactide-co-glycolide)-85:15 (PLGA) was used to develop nanoparticles of Tamoxifen Citrate by multiple emulsification (w/o/w) and solvent evaporation technique. Drug-polymer ratio, polyvinyl alcohol concentrations, and homogenizing speeds were varied at different stages of preparation to optimize the desired size and release profile of drug. The characterization of particle morphology and shape was performed by field emission scanning electron microscope (FE-SEM) and particle size distribution patterns were studied by direct light scattering method using zeta sizer. In vitro drug release study showed that release profile of Tamoxifen from biodegradable nanoparticles varied due to the change in speed of centrifugation for separation. Drug loading efficiency varied from 18.60% to 71.98%. The FE-SEM study showed that biodegradable nanoparticles were smooth and spherical in shape. The stability studies of Tamoxifen Citrate in the experimental nanoparticles showed the structural integrity of Tamoxifen Citrate in PLGA nanoparticles up to 60°C in the tested temperatures. Nanoparticles containing Tamoxifen Citrate could be useful for the controlled delivery of the drug for a prolonged period.
-
Tamoxifen Citrate encapsulated sustained release liposomes: preparation and evaluation of physicochemical properties
Scientia pharmaceutica, 2010Co-Authors: Buddhadev Layek, Biswajit MukherjeeAbstract:The present study was designed for the development of a stable sustained release liposomal drug delivery system for Tamoxifen Citrate (TC) using soya phosphatidylcholine (SPC), cholesterol (CH) and span 20 as main ingredients. Liposomes were prepared by formation of thin lipid film followed by hydration. The mean vesicle diameter was found to be 203.5 ± 19.5 nm with 21% of the liposomal population having average diameter below 76.72 ± 6.7 nm. There was a good vesicular distribution with the polydispersity index of 0.442 ± 0.03. The maximum loading of drug was determined to be 53.60% of the initial amount that is 34.58 μg of drug per mg of lipid. Amongst the different storage conditions, liposomes stored at 2–8°C were found to be most stable and only 4% of the drug was lost over the storage period of 5 weeks. In vitro release studies of liposomes showed that 50% of drug was released within 3 hours (h) whereas 95% drug was released in 30 h. This indicates the usefulness of the liposomal delivery system for sustaining the in vitro release of Tamoxifen Citrate.
Subhasish Mondal - One of the best experts on this subject based on the ideXlab platform.
-
Preparation and characterization of Tamoxifen Citrate loaded nanoparticles for breast cancer therapy.
International journal of nanomedicine, 2014Co-Authors: Ruma Maji, Niladri Shekhar Dey, Bhabani Sankar Satapathy, Biswajit Mukherjee, Subhasish MondalAbstract:Background Four formulations of Tamoxifen Citrate loaded polylactide-co-glycolide (PLGA) based nanoparticles (TNPs) were developed and characterized. Their internalization by Michigan Cancer Foundation-7 (MCF-7) breast cancer cells was also investigated.
Paolo Colombo - One of the best experts on this subject based on the ideXlab platform.
-
lecithin chitosan controlled release nanopreparations of Tamoxifen Citrate loading enzyme trigger release and cell uptake
Journal of Controlled Release, 2013Co-Authors: Stefano Barbieri, Fabio Sonvico, Caterina Como, Gaia Colombo, Franca Zani, Francesca Buttini, Ruggero Bettini, Alessandra Rossi, Paolo ColomboAbstract:Abstract Tamoxifen Citrate (TAM), an anticancer drug with amphiphilic properties, was loaded in lecithin/chitosan nanoparticles (LCN) with a view to oral administration. The influence of Tamoxifen loading on the physico-chemical properties of nanoparticles was studied. Size, surface charge and morphological properties of Tamoxifen-loaded nanoparticles (LCN-TAM) were assessed. The increase in the Tamoxifen amount in the LCN-TAM preparation up to 60 mg/100ml maintained the positive zeta potential value of about + 45 mV. A statistically significant decrease in particle size was observed for TAM amounts between 5 and 20 mg. A strong influence of loaded Tamoxifen on the structure of lecithin/chitosan nanoparticles was observed, supported by the quantification of free chitosan and morphological analysis. A loading of Tamoxifen in nanoparticles of around 19% was obtained. The release of the drug from the LCN-TAM colloidal dispersion was measured, showing that Tamoxifen Citrate was released very slowly in simulated gastro-intestinal fluids without enzymes. When enzymes able to dismantle the nanoparticle structure were added to the dissolution medium, drug release was triggered and continued in a prolonged manner. Tamoxifen-loaded nanoparticles showed cytotoxicity towards MCF-7 cells comparable to that obtained with Tamoxifen Citrate solution, but the rate of this toxic effect was dependent on drug release. Caco-2 cells, used as a model of the intestinal epithelium, were shown to take up the TAM loaded nanoparticles extensively.
-
Lecithin/chitosan controlled release nanopreparations of Tamoxifen Citrate: loading, enzyme-trigger release and cell uptake.
Journal of controlled release : official journal of the Controlled Release Society, 2013Co-Authors: Stefano Barbieri, Fabio Sonvico, Caterina Como, Gaia Colombo, Franca Zani, Francesca Buttini, Ruggero Bettini, Alessandra Rossi, Paolo ColomboAbstract:Abstract Tamoxifen Citrate (TAM), an anticancer drug with amphiphilic properties, was loaded in lecithin/chitosan nanoparticles (LCN) with a view to oral administration. The influence of Tamoxifen loading on the physico-chemical properties of nanoparticles was studied. Size, surface charge and morphological properties of Tamoxifen-loaded nanoparticles (LCN-TAM) were assessed. The increase in the Tamoxifen amount in the LCN-TAM preparation up to 60 mg/100ml maintained the positive zeta potential value of about + 45 mV. A statistically significant decrease in particle size was observed for TAM amounts between 5 and 20 mg. A strong influence of loaded Tamoxifen on the structure of lecithin/chitosan nanoparticles was observed, supported by the quantification of free chitosan and morphological analysis. A loading of Tamoxifen in nanoparticles of around 19% was obtained. The release of the drug from the LCN-TAM colloidal dispersion was measured, showing that Tamoxifen Citrate was released very slowly in simulated gastro-intestinal fluids without enzymes. When enzymes able to dismantle the nanoparticle structure were added to the dissolution medium, drug release was triggered and continued in a prolonged manner. Tamoxifen-loaded nanoparticles showed cytotoxicity towards MCF-7 cells comparable to that obtained with Tamoxifen Citrate solution, but the rate of this toxic effect was dependent on drug release. Caco-2 cells, used as a model of the intestinal epithelium, were shown to take up the TAM loaded nanoparticles extensively.
Dimitrios A. Adamopoulos - One of the best experts on this subject based on the ideXlab platform.
-
Effectiveness of combined Tamoxifen Citrate and testosterone undecanoate treatment in men with idiopathic oligozoospermia
Fertility and sterility, 2003Co-Authors: Dimitrios A. Adamopoulos, Stamatina Nicopoulou, Athina Pappa, Evangelia Billa, Eftychia Koukkou, John MichopoulosAbstract:Abstract Objective To assess the effect of treatment with a combination of the antiestrogen Tamoxifen Citrate and the androgen testosterone undecanoate on sperm variables and pregnancy incidence in men with idiopathic oligozoospermia and couple subfertility. Design Prospective, randomized, placebo-controlled trial. Setting Clinical research in a tertiary care academic hospital. Participant(s) Two hundred twelve men with idiopathic oligozoospermia and 82 normozoospermic men with female factor subfertility. Intervention(s) Oligozoospermic patients were randomly assigned to two treatment groups with Tamoxifen Citrate, 20 mg/d, and testosterone undecanoate, 120 mg/d (n = 106) or placebo treatment (n = 106) for 6 months. Normozoospermic men were followed for the same period. Couple counseling was part of the intervention in all groups. Main outcome measure(s) Pregnancy incidence and sperm characteristics after 3 and 6 months on medication and 3 months after the end of the trial. Result(s) In the active treatment group, total sperm count (median [25th, 75th percentile], 27.1 × 10 6 cells/mL [9.4, 54.0 × 10 6 cells/mL] at baseline and 61.5 × 10 6 cells/mL [28.2, 119.6 × 10 6 cells/mL] at 6 months), progressive motility (mean [±SD] , 29.7% ± 12.0% at baseline and 41.6% ± 13.1% at 6 months), and normal morphology (mean, 41.2% ± 14.0% at baseline and 56.6% ± 11.5% at 6 months) were noted. No marked changes were observed in placebo recipients or normozoospermic men. The incidence of spontaneous pregnancy was 33.9% in the active treatment group and 10.3% in the placebo group (36 vs. 11 pregnancies), with a relative risk of 3.195 (95% CI, 2.615 to 3.765). Conclusion(s) Treatment with Tamoxifen Citrate and testosterone undecanoate improved sperm variables and led to a higher incidence of pregnancy in couples with subfertility related to idiopathic oligozoospermia.
-
The combination of testosterone undecanoate with Tamoxifen Citrate enhances the effects of each agent given independently on seminal parameters in men with idiopathic oligozoospermia
Fertility and sterility, 1997Co-Authors: Dimitrios A. Adamopoulos, Stamatina Nicopoulou, Niki Kapolla, Maria Karamertzanis, Evangelia AndreouAbstract:Abstract Objective: To evaluate the effects of combined Tamoxifen Citrate and T undecanoate treatment on seminal parameters in men with idiopathic oligozoospermia. Design: Prospective randomized clinical study. Setting: A state hospital tertiary clinic. Patient(s): Eighty oligozoospermic men were included in the protocol. Intervention(s): Patients were randomized to receive placebo, T undecanoate (40 mg three times per day), Tamoxifen Citrate (10 mg two times per day), or T undecanoate plus Tamoxifen Citrate. Result(s): Tamoxifen Citrate plus T undecanoate treatment produced a satisfactory improvement of total sperm number, motility, and functional sperm fraction after 3 and 6 months. Comparisons with other active treatment groups showed significantly higher increment values for motility and functional fraction, whereas aniline, acrosine, and free L-carnitine also were markedly better in the combination treatment group. Conclusion(s): These results indicate that the combination of Tamoxifen Citrate with T undecanoate not only improves significantly important seminal parameters but also compares favorably with the single treatments used. Therefore, this combination deserves a place as a first line of treatment in idiopathic oligozoospermia.
Jagadeesh G Hiremath - One of the best experts on this subject based on the ideXlab platform.
-
An Approach to Enhance Dissolution Rate of Tamoxifen Citrate
BioMed research international, 2019Co-Authors: Nagaraja Sreeharsha, Jagadeesh G Hiremath, Swathi Chilukuri, Rajesh Kumar Aitha, Bandar E. Al-dhubiab, Katharigatta N. Venugopala, Abdullah M. Alzahrani, Girish MeravanigeAbstract:We tested the solubility and dissolution of Tamoxifen Citrate to ascertain the optimal conditions for faster dissolution. Using the solvent evaporation method and hydrophilic carriers, we formulated Tamoxifen Citrate (TC) that contained solid dispersions (SDs). We increased the solubility and dissolution rate of TC with a solid dispersion system that consisted of polyethylene glycol (PEG-6000), beta-cyclodextrin (β-CD), and a combination of carriers. Physicochemical characteristics of solubility (mg/ml) were found to be 0.987±0.04 (water), 1.324±0.05 (6.8pH PBS), and 1.156±0.03 (7.4 pH PBS) for F5 formulation, percentage yield was between 98.74 ± 1.11% and 99.06 ± 0.58%, drug content was between 98.06±0.58 and 99.06±1.10, and dissolution studies binary complex showed a faster release of TC as compared to a single polymer and pure drug. Furthermore, thermal properties, physicochemical drug and polymer interaction, crystal properties, and morphology were determined using differential scanning calorimetry (DSC), infrared spectroscopy (FT-IR), X-ray differential studies, and scanning electron microscopy. We used the same proportion of carrier concentrations of the formulations to calculate the solubility of TC. Our results demonstrated that increased concentrations of β-C yielded an improved solubility of TC, which was two times higher than pure TC. The uniformity in drug content was 97.99 %. A quicker drug release occurred from the binary complex formulation as seen in the dissolution profile. FTIR demonstrated an absence in the physicochemical interaction between the drug and carriers. The drug was also found to be dispersed in the amorphous state as revealed by DSC and XRD. The drug concentration did not vary during various storage conditions. Our in vivo studies demonstrated that SD displayed significantly higher values of Cmax (p < 0.05) and AUC0-24 (p < 0.05) as compared to free TC. Furthermore, Tmax in SD was significantly lower (p < 0.05), as compared to free TC.
-
Preparation and in vitro characterization of poly (epsilon-caprolactone)-based Tamoxifen Citrate- loaded cylindrical subdermal implant for breast cancer
Asian Journal of Pharmaceutics, 2011Co-Authors: Jagadeesh G Hiremath, V. Kusum DeviAbstract:In the present study cylindrical poly(epsilon-caprolactone) (PCL)-based biodegradable polymeric Tamoxifen Citrate-loaded subdermal implants were prepared by laboratory-based modified melt extrusion technique. The prepared implants were evaluated for their physicochemical parameters. Drug content in implants by high-performance liquid chromatographic (HPLC) method, differential scanning calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscope (SEM) studies of Tamoxifen Citrate-loaded implants. Determination of in vitro hydrolytic degradation of polymeric and Tamoxifen Citrate-loaded implants and in vitro drug release was carried out by using indigenously developed dissolution apparatus. DSC and XRD studies proved that the drug is entrapped in the implant. The highest rate of hydrolytic degradation (weight loss) was observed in blank implants when compared to Tamoxifen Citrate-loaded implants.The studies proved that the developed method have potential in terms of industrial feasibility.
-
Tamoxifen Citrate loaded biodegradable poly(sebacic acid-co- ricinoleic acid) microparticles, in vitro characterization
Journal of Drug Delivery Science and Technology, 2011Co-Authors: Jagadeesh G Hiremath, C.g. Rudani, R. V. Suthar, Abraham J. DombAbstract:The aim of the present investigation was to develop biodegradable microparticles of the antineoplastic drug, Tamoxifen Citrate, for the treatment of breast cancer, using poly(sebacic acid-co-ricinoleic acid) 70:30 w/w as a drug carrier. Drug loaded microparticles were prepared by utilizing solvent displacement technique and characterized for particle size and distribution, surface morphology, drug physical state and crystalline nature, entrapment efficiency, drug loading and in vitro release characteristics. Spherical microparticles were obtained with a smooth surface and a mean particle size of 1.0-1.6 μm. The entrapped Tamoxifen Citrate in microparticles has no evidence of any chemical or physical interaction with polymer and drug was in the form of amorphous state. In vitro release studies showed zero order and Korsmeyer-Peppas model release being exhibited. A significant difference in sustaining capacity was seen in microparticles with different drug loading. Sustained release effect was more pronounced in microparticles prepared with loading level.
-
Characterization of cylindrical and strip-shaped Tamoxifen Citrate-loaded biodegradable implants
Asian Journal of Pharmaceutics, 2011Co-Authors: Jagadeesh G Hiremath, Rajesh Kumar Aitha, Pragnesh B Patel, Prasanthkumar Mura, Subhash Palavalli GAbstract:The aim of this study was to prepare Tamoxifen Citrate (TC)-loaded cylindrical and strip-shaped polymeric subdermal implants. The implant was based on poly(e-caprolactone), a low-melting, biodegradable and biocompatible polymer. Polyethylene glycol (PEG 4000) was used to enhance solubility and release of the drug in the phosphate buffer saline pH 7.4. Implants were prepared by a standardized melt manufacturing method. The prepared implants were evaluated for their physicochemical parameters and drug content in implants by UV spectrophotometric method. PCL-based implants were characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry, X-ray diffraction studies(XRD) and scanning electron microscopy (SEM). DSC studies showed that the TC in the implants was in the amorphous state. In vitro drug release studies were performed in methanol:phosphate-buffered saline (pH 7.4) at 37±2°C by using horizontal water bath shaker. Stability study was carried out for 90 days, there was no significant change in drug content and other parameters of the PCL-based formulations.
-
biodegradable poly sebacic acid co ricinoleic ester anhydride Tamoxifen Citrate implants preparation and in vitro characterization
Journal of Applied Polymer Science, 2008Co-Authors: Jagadeesh G Hiremath, Kshama Devi, Kusum V Devi, Abraham J. DombAbstract:The aim of this study was to prepare Tamoxifen Citrate loaded cylindrical polymeric implants for application at tumor sites. The implant was based on poly (sebacic acid-co-ricinoleic-ester anhydride) 70 : 30 w/w [poly(SA-RA) 70 : 30 w/w], a low-melting, biodegradable, and biocompatible polymer. Implants were prepared by a standardized melt manufacturing method. Differential scanning calorimetry and scanning electron microscopy were used for implant characterization. In vitro drug release studies were performed in phosphate-buffered saline (pH 7.4) at 37 ± 2°C. The drug content was estimated by high-performance liquid chromatography. The differential scanning calorimetry studies showed that the Tamoxifen Citrate in the implants was in the amorphous state. The cumulative percentage of drug release from 10 and 20 wt % drug-loaded poly(SA-RA) 70 : 30 w/w implants after 30 days was found to be 42.36 and 62.60%, respectively. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci, 2008
