Journal articles: 'TPGS'

1

Zuccari, Guendalina, Sara Baldassari, Silvana Alfei, Barbara Marengo, Giulia Elda Valenti, Cinzia Domenicotti, Giorgia Ailuno, Carla Villa, Leonardo Marchitto, and Gabriele Caviglioli. "D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid." Pharmaceuticals 14, no. 3 (March 4, 2021): 212. http://dx.doi.org/10.3390/ph14030212.

Full text

Abstract:

All-trans-retinoic acid (ATRA) represents the first-choice treatment for several skin diseases, including epithelial skin cancer and acne. However, ATRA’s cutaneous side effects, like redness and peeling, and its high instability limit its efficacy. To address these drawbacks and to improve ATRA solubilization, we prepared ATRA-loaded micelles (ATRA-TPGSs), by its encapsulation in D-α-tocopheryl-polyethylene-glycol-succinate (TPGS). First, to explore the feasibility of the project, a solubility study based on the equilibrium method was performed; then, six ATRA-TPGS formulations were prepared by the solvent-casting method using different TPGS amounts. ATRA-TPGSs showed small sizes (11–20 nm), low polydispersity, slightly negative zeta potential, and proved good encapsulation efficiency, confirmed by a chemometric-assisted Fourier transform infrared spectroscopy (FTIR) investigation. ATRA-TPGS stability was also investigated to choose the most stable formulation. Using Carbopol® 980 as gelling agent, ATRA-TPGS-loaded gels were obtained and analyzed for their rheological profiles. Ex vivo release studies from ATRA-TPGSs were performed by Franz cells, demonstrating a permeation after 24 h of 22 ± 4 µ cm−2. ATRA-TPGSs showed enhanced cytotoxic effects on melanoma cells, suggesting that these formulations may represent a valid alternative to improve patient compliance and to achieve more efficacious therapeutic outcomes.

APA, Harvard, Vancouver, ISO, and other styles

2

Zuccari, Guendalina, Silvana Alfei, Alessia Zorzoli, Danilo Marimpietri, Federica Turrini, Sara Baldassari, Leonardo Marchitto, and Gabriele Caviglioli. "Increased Water-Solubility and Maintained Antioxidant Power of Resveratrol by Its Encapsulation in Vitamin E TPGS Micelles: A Potential Nutritional Supplement for Chronic Liver Disease." Pharmaceutics 13, no. 8 (July 23, 2021): 1128. http://dx.doi.org/10.3390/pharmaceutics13081128.

Full text

Abstract:

Children affected by chronic liver disease exhibit impaired neurocognitive development and growth due to the low absorption and digestion of nutrients. Furthermore, malnutrition is an adverse prognostic factor in liver transplantation as it is associated with an increase in morbidity and mortality. D-α-tocopheryl-polyethylene-glycol-succinate (TPGS) is currently administered per os as a vitamin E source to improve children’s survival and well-being; however, TPGS alone does not reverse spinocerebellar degeneration and lipid peroxidation. To potentiate the effects of TPGS, we loaded micelles with resveratrol (RES), a natural polyphenol, with antioxidant and antiinflammatory activities, which has demonstrated protective action in the liver. Firstly, we investigated the suitability of TPGS to encapsulate RES in micelles by means of a phase-solubility study, then RES-TPGS formulations were prepared via solvent casting and solvent diffusion evaporation methods. RES-TPGS colloidal dispersions showed small mean diameters (12 nm), low polydispersity, and quite neutral Zeta potentials. The formulations showed a sustained drug release and a good drug loading capacity, further confirmed by infrared spectroscopy and differential scanning calorimetry. RES-TPGSs exhibited unaltered antioxidant activity compared to pristine RES via the DPPH assay and a significant reduction in toxicity compared to empty TPGS on HaCaT cells. Thus, RES-TPGS micelles may overcome the challenges of current liver disease therapy by providing more protective effects thanks to the antioxidant activity of RES and by reducing the surfactant toxicity on normal cells.

APA, Harvard, Vancouver, ISO, and other styles

3

Jia, Shuxin, Shaochen Wang, Shanshan Li, Peng Hu, Shuling Yu, Jiahua Shi, and Jintao Yuan. "Specific modification and self-transport of porphyrins and their multi-mechanism cooperative antitumor studies." Journal of Materials Chemistry B 9, no. 14 (2021): 3180–91. http://dx.doi.org/10.1039/d0tb02847a.

Full text

Abstract:

The introduction of TPGS increases the cellular uptake and antitumor activity of TAPP-TPGS. TAPP-TPGS/PTX with small size increases the enrichment of drug and photosensitizer in tumor region and has excellent biocompatibility and synergistic treatment effect of TPGS, chemotherapy and PDT.

APA, Harvard, Vancouver, ISO, and other styles

4

ZHAO, TIEJUN, HEZHONG CHEN, LIXIN YANG, HAI JIN, ZHIGANG LI, LIN HAN, FANGLIN LU, and ZHIYUN XU. "DDAB-MODIFIED TPGS-b-(PCL-ran-PGA) NANOPARTICLES AS ORAL ANTICANCER DRUG CARRIER FOR LUNG CANCER CHEMOTHERAPY." Nano 08, no. 02 (April 2013): 1350014. http://dx.doi.org/10.1142/s1793292013500148.

Full text

Abstract:

Oral chemotherapy is a great way to cancer treatment because it is less stressful being that the patient will have less hospital visits and can still maintain a close relationship with health care professionals. In this research, three types of nanoparticle formulation from commercial PCL and self-synthesized TPGS-b-(PCL-ran-PGA) diblock copolymer were fabricated for oral delivery of antitumor agents, including DDAB-modified PCL nanoparticles, unmodified TPGS-b-(PCL-ran-PGA) nanoparticles and DDAB-modified TPGS-b-(PCL-ran-PGA) nanoparticles. Firstly, the TPGS-b-(PCL-ran-PGA) diblock copolymer was synthesized and characterized. DDAB was adopted to increase retention time at the cell surface, thus increasing the chances of nanoparticle uptake by the gastrointestinal mucosa and improving drug absorption. The TPGS-b-(PCL-ran-PGA) nanoparticles were found by FESEM of spherical shape and around 200 nm in diameter. The surface charge of TPGS-b-(PCL-ran-PGA) nanoparticles was reversed from anionic to cationic after DDAB modification. The DDAB-modified TPGS-b-(PCL-ran-PGA) nanoparticles have significantly higher level of the cell uptake than that of DDAB-modified PCL nanoparticles and unmodified TPGS-b-(PCL-ran-PGA) nanoparticles. In vitro cell viability studies showed advantages of the DDAB-modified TPGS-b-(PCL-ran-PGA) nanoparticles over Taxotere® in terms of cytotoxicity against A549 cells. In conclusion, oral chemotherapy by DDAB-modified TPGS-b-(PCL-ran-PGA) nanoparticle formulation may provide a promising outcome for lung cancer patients.

APA, Harvard, Vancouver, ISO, and other styles

5

Liu, Tengfei, Xiaoyan Liu, Hui Xiong, Cheng Xu, Jianxu Yao, Xiumei Zhu, Jianping Zhou, and Jing Yao. "Mechanisms of TPGS and its derivatives inhibiting P-glycoprotein efflux pump and application for reversing multidrug resistance in hepatocellular carcinoma." Polymer Chemistry 9, no. 14 (2018): 1827–39. http://dx.doi.org/10.1039/c8py00344k.

Full text

APA, Harvard, Vancouver, ISO, and other styles

6

Ji, Suping, Xiao Lin, Enjiang Yu, Chengyang Dian, Xiong Yan, Liangyao Li, Meimei Zhang, Wenchang Zhao, and Linghui Dian. "Curcumin-Loaded Mixed Micelles: Preparation, Characterization, and In Vitro Antitumor Activity." Journal of Nanotechnology 2018 (2018): 1–9. http://dx.doi.org/10.1155/2018/9103120.

Full text

Abstract:

The objective of this study was to prepare curcumin-loaded mixed Soluplus/TPGS micelles (Cur-TPGS-PMs) for oral administration. The Cur-TPGS-PMs showed a mean size of 65.54 ± 2.57 nm, drug encapsulation efficiency over 85%, and drug loading of 8.17%. The Cur-TPGS-PMs were found to be stable in various pH media (pH 1.2 for 2 h, pH 6.8 for 2 h, and pH 7.4 for 6 h). The X-ray diffraction (XRD) patterns illustrated that curcumin was in the amorphous or molecular state within PMs. The In vitro release test indicated that Cur-TPGS-PMs possessed a significant sustained-release property. The cell viability in MCF-7 cells was found to be relatively lower in Cur-TPGS-PM-treated cells as compared to free Cur-treated cells. CLSM imaging revealed that mixed micelles were efficiently absorbed into the cytoplasm region of MCF-7 cells. Therefore, Cur-TPGS-PMs could have the significant value for the chronic breast cancer therapy.

APA, Harvard, Vancouver, ISO, and other styles

7

Ji, Li Li, Qiao Ling Li, Zeng Hu Yang, Wei Jing Hu, and Kui Hua Zhang. "Fabrication and Characterization of Vitamin E TPGS Loaded Silk Fibroin/Hyaluronic Acid Nanofibrous Scaffolds." Advanced Materials Research 721 (July 2013): 274–77. http://dx.doi.org/10.4028/www.scientific.net/amr.721.274.

Full text

Abstract:

Vitamin E d-alpha-tocopheryl polyethylene glycol 1000 succinate (VE TPGS) loaded silk fibroin (SF)/ hyaluronic acid (HA) nanofibrous scaffolds were fabricated by means of electrospinning to biomimic the natural extracellular matrix. Scanning electronic microscopy (SEM) results indicated that electrospun VE TPGS loaded SF/HA nanofibers were ribbon-shaped, the width of nanofibers decreased slightly with the addition of VE TPGS to SF/HA blended solutions. Fourier transform infrared (FTIR) spectroscopy and Wide-angle X-ray diffraction (WAXD) curves revealed that VE TPGS did not induce SF conformation from random coil to β-sheet. SF conformation converted from random coil to β-sheet after being treated with 75% ethanol vapor. In vitro release studies confirmed VE TPGS had no obvious burst release and present good release behavior.

APA, Harvard, Vancouver, ISO, and other styles

8

Wang, Hai Long, Shan Kui Liu, Yao Yao Qin, and Yun Gang Chen. "Hydroxycamptothecin Stealth Liposomes: Containing TPGS as a Novel PEGylated Long-Circulating Coating Material." Advanced Materials Research 886 (January 2014): 333–36. http://dx.doi.org/10.4028/www.scientific.net/amr.886.333.

Full text

Abstract:

The goal of this study was to develop long-circulating liposomes of hydroxylcamptothecin (HCPT) with TPGS as a new coating material. Liposomes were prepared by a thin-film dispersion method with the lipids comprised phosphatidylcholine, cholesterol and TPGS. By contrast, other common PEGylated derivatives were also involved. HCPT-loaded liposomes with TPGS as coating material showed similar physicochemical characteristics andin vitrorelease profile to liposomes with DSPE-PEG or DPPE-PEG. It is suggested that TPGS can be applied as a novel coating material for long-circulating liposomes.

APA, Harvard, Vancouver, ISO, and other styles

9

Yusuf, Osman, Raisuddin Ali, Abdullah H. Alomrani, Aws Alshamsan, Abdullah K. Alshememry, Abdulaziz M. Almalik, Afsaneh Lavasanifar, and Ziyad Binkhathlan. "Design and Development of D‒α‒Tocopheryl Polyethylene Glycol Succinate‒block‒Poly(ε-Caprolactone) (TPGS−b−PCL) Nanocarriers for Solubilization and Controlled Release of Paclitaxel." Molecules 26, no. 9 (May 4, 2021): 2690. http://dx.doi.org/10.3390/molecules26092690.

Full text

Abstract:

The objective of this study was to synthesize and characterize a set of biodegradable block copolymers based on TPGS-block-poly(ε-caprolactone) (TPGS-b-PCL) and to assess their self-assembled structures as a nanodelivery system for paclitaxel (PAX). The conjugation of PCL to TPGS was hypothesized to increase the stability and the drug solubilization characteristics of TPGS micelles. TPGS-b-PCL copolymer with various PCL/TPGS ratios were synthesized via ring opening bulk polymerization of ε-caprolactone using TPGS, with different molecular weights of PEG (1–5 kDa), as initiators and stannous octoate as a catalyst. The synthesized copolymers were characterized using 1H NMR, GPC, FTIR, XRD, and DSC. Assembly of block copolymers was achieved via the cosolvent evaporation method. The self-assembled structures were characterized for their size, polydispersity, and CMC using dynamic light scattering (DLS) technique. The results from the spectroscopic and thermal analyses confirmed the successful synthesis of the copolymers. Only copolymers that consisted of TPGS with PEG molecular weights ≥ 2000 Da were able to self-assemble and form nanocarriers of ≤200 nm in diameter. Moreover, TPGS2000-b-PCL4000, TPGS3500-b-PCL7000, and TPGS5000-b-PCL15000 micelles enhanced the aqueous solubility of PAX from 0.3 µg/mL up to 88.4 ug/mL in TPGS5000-b-PCL15000. Of the abovementioned micellar formulations, TPGS5000-b-PCL15000 showed the slowest in vitro release of PAX. Specifically, the PAX-loaded TPGS5000-b-PCL15000 micellar formulation showed less than 10% drug release within the first 12 h, and around 36% cumulative drug release within 72 h compared to 61% and 100% PAX release, respectively, from the commercially available formulation (Ebetaxel®) at the same time points. Our results point to a great potential for TPGS-b-PCL micelles to efficiently solubilize and control the release of PAX.

APA, Harvard, Vancouver, ISO, and other styles

10

Liu, Yude, Lian Rao, Hongguan Zhang, Yanyou Cen, and Kaili Cheng. "Conjugation of vitamin E-TPGS and guar gum to carry borneol for enhancing blood–brain barrier permeability." Journal of Biomaterials Applications 33, no. 4 (September 12, 2018): 590–98. http://dx.doi.org/10.1177/0885328218799551.

Full text

Abstract:

Herb borneol is usually used in clinics for the treatment of central nervous system illness, for its ability of blood–brain barrier permeability, although its poor water solubility and poor bioavailability limit its clinical application to some degree. In this study, we developed a novel nanoparticle combining the benefits of vitamin E d-ɑ-tocopheryl poly(ethylene glycol) succinate (E-TPGS) (or TPGS) and guar gum to get TPGS-g-guar gum as a drug delivery system to carry borneol, which could improve the solubility of borneol and increase the drug-loading capacity efficiently. The results showed that TPGS-g-guar gum nanoparticles delivery system was suitable to carry borneol and release the drug effectively, and TPGS-g-guar gum/borneol nanoparticles would be a potential platform for improving the treatment of central nervous system illness and cerebrovascular disease.

APA, Harvard, Vancouver, ISO, and other styles

11

Pan, Jie, Pei-Jiao Li, Yi Wang, Lu Chang, Dong Wan, and Hao Wang. "Active targeted drug delivery of MMP-2 sensitive polymeric nanoparticles." Chemical Communications 54, no. 79 (2018): 11092–95. http://dx.doi.org/10.1039/c8cc05504a.

Full text

APA, Harvard, Vancouver, ISO, and other styles

12

Metin, Esra, Pelin Mutlu, and Ufuk Gündüz. "Co-delivery of Doxorubicin and D-α-Tocopherol Polyethylene Glycol 1000 Succinate by Magnetic Nanoparticles." Anti-Cancer Agents in Medicinal Chemistry 18, no. 8 (December 28, 2018): 1138–47. http://dx.doi.org/10.2174/1871520618666180313154724.

Full text

Abstract:

Background: Although conventional chemotherapy is the most common method for cancer treatment, it has several side effects such as neuropathy, alopecia and cardiotoxicity. Since the drugs are given to body systemically, normal cells are also affected, just like cancer cells. However, in recent years, targeted drug delivery has been developed to overcome these drawbacks. Objective: The aim of this study was targeted co-delivery of doxorubicin (Dox) which is an anticancer agent and D-α-Tocopherol polyethylene glycol 1000 succinate (vitamin E TPGS or simply TPGS) to breast cancer cells. For this purpose, Magnetic Nanoparticles (MNPs) were synthesized and coated with Oleic Acid (OA). Coated nanoparticles were encapsulated in Poly Lactic-co-Glycolic Acid (PLGA) and TPGS polymers and loaded with Dox. The Nanoparticles (NPs) were characterized by Fourier Transform Infrared (FTIR) spectroscopy, zetapotential analysis, Dynamic Light Scattering (DLS) analysis, Thermal Gravimetric Analysis (TGA) and Scanning Electron Microscope (SEM) analysis. Results: The results showed that NPs were spherical, superparamagnetic and in the desired range for use in drug targeting. The targetability of NPs was confirmed. Moreover, TPGS and Dox loading was shown by TGA and FTIR analyses. NPs were internalized by cells and the cytotoxic effect of drug loaded NPs on sensitive (MCF-7) and drug-resistant (MCF-7/Dox) cells were examined. It was seen that the presence of TPGS increased cytotoxicity significantly. TPGS also enhanced drug loading efficiency, release rate, cellular internalization. In MCF- 7/Dox cells, the drug resistance seems to be decreased when Dox is loaded onto TPGS containing NPs. Conclusion: This magnetic PLGA nanoparticle system is important for new generation targeted chemotherapy and could be used for breast cancer treatment after in vivo tests.

APA, Harvard, Vancouver, ISO, and other styles

13

Tesan, Fiorella C., Melisa B. Nicoud, Mariel Nuñez, Vanina A. Medina, Diego A. Chiappetta, and María J. Salgueiro. "99mTc-Radiolabeled TPGS Nanomicelles Outperform 99mTc-Sestamibi as Breast Cancer Imaging Agent." Contrast Media & Molecular Imaging 2019 (April 23, 2019): 1–9. http://dx.doi.org/10.1155/2019/4087895.

Full text

Abstract:

D-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) is a Food and Drug Administration (FDA) approved biomaterial that can form nanosized micelles in aqueous solution. TPGS micelles stand as an interesting system to perform drug delivery as they can carry lipophilic drugs and overcome P glycoprotein efflux as well. Therefore, TPGS micelles combined with other copolymers have been reported in many cancer research studies as a carrier for therapeutic drugs. Their ability to reach tumoral tissue can also be exploited to develop imaging agents with diagnostic application. A radiolabeling method with 99mTc for TPGS nanosized micelles and their biodistribution in a healthy animal model as well as their pharmacokinetics and radiolabeling stability in vivo was previously reported. The aim of this work was to evaluate the performance of this radioactive probe as a diagnostic imaging agent compared to routinely available SPECT radiopharmaceutical, 99mTc-sestamibi. A small field of view gamma camera was used for scintigraphy studies using radiolabeled TPGS micelles in two animal models of breast cancer: syngeneic 4T1 murine cell line (injected in BALB/c mice) and chemically NMU-induced (Sprague-Dawley rats). Ex vivo radioactivity accumulation in organs of interest was measured by a solid scintillation counter, and a semiquantitative analysis was performed over acquired images as well. Results showed an absence of tumoral visualization in 4T1 model for both radioactive probes by gamma camera imaging. On the contrary, NMU-induced tumors had a clear tumor visualization by scintigraphy. A higher tumor/background ratio and more homogeneous uptake were found for radiolabeled TPGS micelles compared to 99mTc-sestamibi. In conclusion, 99mTc-radiolabeled TPGS micelles might be a potential SPECT imaging probe for diagnostic purposes.

APA, Harvard, Vancouver, ISO, and other styles

14

Chou, Tzung-Han, Daniel Setiyo Nugroho, Jia-Yaw Chang, Yu-Shen Cheng, Chia-Hua Liang, and Ming-Jay Deng. "Encapsulation and Characterization of Nanoemulsions Based on an Anti-oxidative Polymeric Amphiphile for Topical Apigenin Delivery." Polymers 13, no. 7 (March 25, 2021): 1016. http://dx.doi.org/10.3390/polym13071016.

Full text

Abstract:

Apigenin (Apig) is used as a model drug due to its many beneficial bio-activities and therapeutic potentials. Nevertheless, its poor water solubility and low storage stability have limited its application feasibility on the pharmaceutical field. To address this issue, this study developed nanoemulsions (NEs) using an anti-oxidative polymeric amphiphile, d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), hydrogenated soy lecithin (HL), black soldier fly larvae (BSFL) oil, and avocado (AV) oil through pre-homogenization and ultrasonication method. Addition of TPGS (weight ratios 100 and 50% as compared to HL) into NEs effectively reduced particle size and phase transition region area of NEs with pure HL. Incorporation of Apig into NEs made particle size increase and provided a disorder effect on intraparticle molecular packing. Nevertheless, the encapsulation efficiency of NEs for Apig approached to about 99%. The chemical stability of Apig was significantly improved and its antioxidant ability was elevated by incorporation with BSFL oil and AV oil NEs, especially for NEs with single TPGS. NEs with single TPGS also exhibited the best Apig skin deposition. For future application of topical Apig delivery, NEs-gel was formed by the addition of hyaluronic acid (HA) into NEs. Their rheological characteristics were dominated by the surfactant ratios of HL to TPGS.

APA, Harvard, Vancouver, ISO, and other styles

15

Pescina, Silvia, Fabio Sonvico, Adryana Clementino, Cristina Padula, Patrizia Santi, and Sara Nicoli. "Preliminary Investigation on Simvastatin-Loaded Polymeric Micelles in View of the Treatment of the Back of the Eye." Pharmaceutics 13, no. 6 (June 9, 2021): 855. http://dx.doi.org/10.3390/pharmaceutics13060855.

Full text

Abstract:

There is increasing consensus in considering statins beneficial for age-related macular degeneration and in general, for immune and inflammatory mediated diseases affecting the posterior segment of the eye. However, all available data relate to oral administration, and safety and effectiveness of statins directly administered to the eye are not yet known, despite their ophthalmic administration could be beneficial. The aim was the development and the characterization of polymeric micelles based on TPGS or TPGS/poloxamer 407 to increase simvastatin solubility and stability and to enhance the delivery of the drug to the posterior segment of the eye via trans-scleral permeation. Simvastatin was chosen as a model statin and its active hydroxy acid metabolite was investigated as well. Results demonstrated that polymeric micelles increased simvastatin solubility at least 30-fold and particularly TPGS/poloxamer 407 mixed micelles, successfully stabilized simvastatin over time, preventing the hydrolysis when stored for 1 month at 4 °C. Furthermore, both TPGS (1.3 mPas) and mixed micelles (33.2 mPas) showed low viscosity, suitable for periocular administration. TPGS micelles resulted the best performing in delivery simvastatin either across conjunctiva or sclera in ex vivo porcine models. The data pave the way for a future viable ocular administration of statins.

APA, Harvard, Vancouver, ISO, and other styles

16

Ahmed, Osama A. A., Hany M. El-Bassossy, Heba M. El-Sayed, and Soad S. Abd El-Hay. "Rp-HPLC Determination of Quercetin in a Novel D-α-Tocopherol Polyethylene Glycol 1000 Succinate Based SNEDDS Formulation: Pharmacokinetics in Rat Plasma." Molecules 26, no. 5 (March 6, 2021): 1435. http://dx.doi.org/10.3390/molecules26051435.

Full text

Abstract:

Despite its proven efficacy in diverse metabolic disorders, quercetin (QU) for clinical use is still limited because of its low bioavailability. D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS) is approved as a safe pharmaceutical adjuvant with marked antioxidant and anti-inflammatory activities. In the current study, several QU-loaded self-nanoemulsifying drug delivery systems (SNEDDS) were investigated to improve QU bioavailability. A reversed phase high performance liquid chromatography (RP-HPLC) method was developed, for the first time, as a simple and sensitive technique for pharmacokinetic studies of QU in the presence of TPGS SNEDDS formula in rat plasma. The analyses were performed on a Xterra C18 column (4.6 × 100 mm, 5 µm) and UV detection at 280 nm. The analytes were separated by a gradient system of methanol and phosphate buffer of pH 3. The developed RP-HPLC method showed low limit of detection (LODs) of 7.65 and 22.09 ng/mL and LOQs of 23.19 and 66.96 ng/mL for QU and TPGS, respectively, which allowed their determination in real rat plasma samples. The method was linear over a wide range, (30–10,000) and (100–10,000) ng/mL for QU and TPGS, respectively. The selected SNEDDS formula, containing 50% w/w TPGS, 30% polyethylene glycol 200 (PEG 200), and 20% w/w pumpkin seed oil (PSO), showed a globule size of 320 nm and −28.6 mV zeta potential. Results of the pharmacokinetic studies showed 149.8% improvement in bioavailability of QU in SNEDDS relative to its suspension. The developed HPLC method proved to be simple and sensitive for QU and TPGS simultaneous determination in rat plasma after oral administration of the new SNEDDS formula.

APA, Harvard, Vancouver, ISO, and other styles

17

Cuerq, Charlotte, Claire Bordat, Charlotte Halimi, Emilie Blond, Marion Nowicki, Noël Peretti, and Emmanuelle Reboul. "Comparison of α-Tocopherol, α-Tocopherol Acetate, and α-Tocopheryl Polyethylene Glycol Succinate 1000 Absorption by Caco-2 TC7 Intestinal Cells." Nutrients 13, no. 1 (December 31, 2020): 129. http://dx.doi.org/10.3390/nu13010129.

Full text

Abstract:

(1) Background: vitamin E is often supplemented in the form of tocopherol acetate, but it has poor bioavailability and can fail to correct blood tocopherol concentrations in some patients with severe cholestasis. In this context, α-tocopheryl polyethylene glycol succinate 1000 (TPGS) has been of value, but very little is known about the mechanisms of its absorption. The aim of our work was to evaluate the mechanisms of absorption/secretion of TPGS compared to tocopherol acetate (TAC) and α-tocopherol by human enterocyte-like Caco-2 TC7 cells. (2) Methods: two weeks post-confluence Caco-2 cells were incubated with tocopherol- or TAC- or TPGS-rich mixed micelles up to 24 h and, following lipid extraction, TAC and tocopherol amounts were measured by high performance liquid chromatography (HPLC) in apical, cellular, and basolateral compartments. (3) Results: at equivalent concentrations of tocopherol in the apical side, the amounts of tocopherol secreted at the basolateral pole of Caco-2 cells are (i) significantly greater when the tocopherol is in the free form in the micelles; (ii) intermediate when it is in the TAC form in the micelles (p < 0.001); and (iii) significantly lower with the TPGS form (p < 0.0001). Interestingly, our results show, for the first time, that Caco-2 cells secrete one or more esterified forms of the vitamin contained in TPGS at the basolateral side.

APA, Harvard, Vancouver, ISO, and other styles

18

Yagiz, Yavuz, Gary Wang, and Liwei Gu. "Emulsification by TPGS or Quillaja Extract Increased Absorption and Affected Metabolism of Berberine in Humans." Current Developments in Nutrition 5, Supplement_2 (June 2021): 381. http://dx.doi.org/10.1093/cdn/nzab037_091.

Full text

Abstract:

Abstract Objectives Berberine is a botanical alkaloid used widely for the prevention of several diseases. However, the absorption rate of berberine is less than 1% in human. The objectives of this study were to determine whether emulsification by TPGS or Quillaja extract affect the absorption and metabolism of orally ingested berberine in human volunteers. Methods Twelve healthy subjects (7 male and 5 females, 21–50-year-old) participated this study. Each subject received 800 mg berberine in a powder form or emulsified with TPGS or Quillaja extract using a randomized crossover design with one-week washout period. Blood samples were collected at 0, 0.5, 1, 2, 3, 4, 6, 8, and 12 hours after dose. Plasma was hydrolyzed with glucuronidase and sulfatase before total content of berberine and its metabolites were analyzed on LC/MS/MS. Free forms of metabolites were determined in plasma without hydrolysis. Pharmacokinetic parameters were calculated using a non-compartment model before they were compared by analysis of covariance. Results The area under the curve (AUC) and peak plasma concentration (Cmax) of berberine was 6.6 μM.hr and 0.9 μM in participants received berberine powder. They were increased to 18.3 μM.hr and 4.5 μM by TPGS emulsification and 28 μM.hr and 5.1 μM by Quillaja extract emulsification, respectively. Berberrubine and demethylberberine were major metabolites of berberine. The AUC of free Berberrubine and demethylberberine was increased by 1.9 fold and 1.6 fold by TPGS and 5.9 folds and 2.7 folds by Quillaja extract, respectively, compared to berberine powder. Participants received berberine powder had AUC of 254 μM.hr and Cmax of 33 μM for total berberrubine. TPGS emulsification increased these values to 425 μM.hr and 54 μM, while Quillaja extract increased them to 341 μM.hr and 44 μM, respectively. Significant increases of AUC and Cmax were also observed for total demethylberberine by TPGS or Quillaja extract emulsification. Conclusions Emulsification of berberine with TPGS or Quillaja extract significantly increased the absorption of berberine and its metabolites in human compared to berberine supplement without emulsifiers. Funding Sources Florida High Tech Corridor Council and Designs for Health.

APA, Harvard, Vancouver, ISO, and other styles

19

Phuong Thu, Ha, Phan Thi Hong Tuyet, Mai Thi Thu Trang, Nguyen Hoai Nam, Truong Thi Nhu Hieu, Le Quang Duong, Tran Thi Nhu Hang, et al. "Preparation and Biological Properties of Platinum(II) Complex-Loaded Copolymer PLA-TPGS." Journal of Nanomaterials 2013 (2013): 1–9. http://dx.doi.org/10.1155/2013/768628.

Full text

Abstract:

A new nanodrug system containing bis(menthone thiosemicarbazonato) Platinum(II) complex (Pt-thiomen) encapsulated with the block copolymers polylactide-d-α-tocopheryl polyethylene glycol 1000 succinate (PLA-TPGS) was prepared by a modified solvent extraction/evaporation technique. The characteristics of the nanoparticles including surface morphology, size distribution, structure, and biological activities such as antimicrobial and cytotoxic activities werein vitroinvestigated. The spherical nanoparticles were around 50 nm in size with core-shell structure and narrow-size distribution. The encapsulated Pt-thiomen can avoid interaction with proteins in the blood plasma. The inhibitory activity of Pt-thiomen-loaded PLA-TPGS nanoparticles on the growth of some bacteria, fungi, and Hep-G2 cells suggests a possibility of developing PLA-TPGS-Pt-thiomen nanoparticles as one of the potential chemotherapeutic agents.

APA, Harvard, Vancouver, ISO, and other styles

20

Tiwari, Sanjay, Jayant Sarolia, Vrushti Kansara, Nishith A. Chudasama, Kamalesh Prasad, Debes Ray, Vinod K. Aswal, and Pratap Bahadur. "Synthesis, Colloidal Characterization and Targetability of Phenylboronic Acid Functionalized α-Tocopheryl Polyethylene Glycol Succinate in Cancer Cells." Polymers 12, no. 10 (October 1, 2020): 2258. http://dx.doi.org/10.3390/polym12102258.

Full text

Abstract:

This study reports targetable micelles developed after covalent functionalization of α-tocopheryl polyethylene glycol succinate (TPGS) with amino phenylboronic acid (APBA). Nuclear magnetic resonance (NMR) and infrared (IR) spectroscopic results showed successful attachment of APBA to the hydrophilic segment of TPGS. Dynamic light scattering and small-angle neutron scattering studies revealed that the conjugate self-assembled in water to produce spherical core-shell micelles (14–20 nm) which remained stable against temperature (ca. 25–45 °C) and pH changes. The micelles could solubilize a high payload of paclitaxel (PLX) without exhibiting changes in the average size. However, at the saturation solubility, drug molecules migrated from the core to the shell region and engaged with APBA groups via π–π stacking interaction. Confocal microscopy and cell sorting analyses verified the effective translocation ability of TPGS-APBA micelles in sialic acid (SA) expressing MDA-MB-453 cells. At equivalent PLX dose, TPGS-APBA micelles showed about a twofold improvement in apoptotic death among the cells exposed for 2 h. Our findings indicate that the attachment of APBA can be a potential strategy for improving the intra-cellular localization of carriers among cancer cells expressing SA residues.

APA, Harvard, Vancouver, ISO, and other styles

21

Calvo-Alvarez, Jazmin, Marlene Jimenez-Del-Rio, and Carlos Velez-Pardo. "Vitamin E TPGS 1000 Induces Apoptosis in the K562 Cell Line: Implications for Chronic Myeloid Leukemia." Oxidative Medicine and Cellular Longevity 2021 (June 9, 2021): 1–15. http://dx.doi.org/10.1155/2021/5580288.

Full text

Abstract:

Chronic myeloid leukemia (CML) is a hematologic malignancy derived from the myeloid lineage molecularly characterized by t(9;22)(q34;q11) resulting in BCR-ABL1 gene fusion, which is known as Philadelphia (Ph) chromosome. Although tyrosine kinase inhibitors (TKIs) have restored and maintained the quality of life of patients with CML, an important minority of patients become resistant to first-and-second-generation TKIs and require an alternative treatment. The K562 cell (Ph+, p53-/-) line was treated with Vit E TPGS 1000 (20–80 μM) only or with other products of interest (e.g., antioxidant N-acetylcysteine (NAC), specific JNK and caspase-3 inhibitor SP600125, and NSCSI, respectively) for 24 h at 37°C. Cells were analyzed by fluorescence microscopy (FM), flow cytometry (FC), and Western blotting (WB) techniques. We show that TPGS induces apoptosis in K562 cells through H2O2 signaling mechanism comprising the activation of a minimal molecular cascade: the kinase JNK>the transcription factor c-JUN>the activation of BCL-only BH3 proapoptotic protein PUMA>loss of mitochondrial membrane potential (ΔΨm)>activation of caspase-3>chromatin condensation>fragmentation of DNA. Additionally, TPGS oxidizes the stress sensor protein DJ-1-Cys106-SH into DJ-1-Cys106-SO3 and arrested the cell cycle in the S phase. Remarkably, NAC, SP600125, and NSCSI blocked TPGS-induced OS and apoptosis in K562. Since TPGS is safe in mice and humans, it is especially promising for preclinical and clinical CML leukemia research. Our findings support the view that oxidation therapy offers an important opportunity to eliminate CML.

APA, Harvard, Vancouver, ISO, and other styles

22

Song, Im-Sook, So-Jeong Nam, Ji-Hyeon Jeon, Soo-Jin Park, and Min-Koo Choi. "Enhanced Bioavailability and Efficacy of Silymarin Solid Dispersion in Rats with Acetaminophen-Induced Hepatotoxicity." Pharmaceutics 13, no. 5 (April 28, 2021): 628. http://dx.doi.org/10.3390/pharmaceutics13050628.

Full text

Abstract:

We evaluated the bioavailability, liver distribution, and efficacy of silymarin-D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) solid dispersion (silymarin-SD) in rats with acetaminophen-induced hepatotoxicity (APAP) compared with silymarin alone. The solubility of silybin, the major and active component of silymarin, in the silymarin-SD group increased 23-fold compared with the silymarin group. The absorptive permeability of silybin increased by 4.6-fold and its efflux ratio decreased from 5.5 to 0.6 in the presence of TPGS. The results suggested that TPGS functioned as a solubilizing agent and permeation enhancer by inhibiting efflux pump. Thus, silybin concentrations in plasma and liver were increased in the silymarin-SD group and liver distribution increased 3.4-fold after repeated oral administration of silymarin-SD (20 mg/kg as silybin) for five consecutive days compared with that of silymarin alone (20 mg/kg as silybin). Based on higher liver silybin concentrations in the silymarin-SD group, the therapeutic effects of silymarin-SD in hepatotoxic rats were evaluated and compared with silymarin administration only. Elevated alanine aminotransferase, aspartate aminotransferase, and alkaline phosphatase levels were significantly decreased by silymarin-SD, silymarin, and TPGS treatments, but these decreases were much higher in silymarin-SD animals than in those treated with silymarin or TPGS. In conclusion, silymarin-SD (20 mg/kg as silybin, three times per day for 5 days) exhibited hepatoprotective properties toward hepatotoxic rats and these properties were superior to silymarin alone, which may be attributed to increased solubility, enhanced intestinal permeability, and increased liver distribution of the silymarin-SD formulation.

APA, Harvard, Vancouver, ISO, and other styles

23

Nikonenko, Boris V., Venkata M. Reddy, Marina Protopopova, Elena Bogatcheva, Leo Einck, and Carol A. Nacy. "Activity of SQ641, a Capuramycin Analog, in a Murine Model of Tuberculosis." Antimicrobial Agents and Chemotherapy 53, no. 7 (May 4, 2009): 3138–39. http://dx.doi.org/10.1128/aac.00366-09.

Full text

Abstract:

ABSTRACT New delivery vehicles and routes of delivery were developed for the capuramycin analogue SQ641. While this compound has remarkable in vitro potency against Mycobacterium tuberculosis, it has low solubility in water and poor intracellular activity. We demonstrate here that SQ641 dissolved in the water-soluble vitamin E analogue α-tocopheryl polyethylene glycol 1000 succinate (TPGS) or incorporated into TPGS-micelles has significant activity in a mouse model of tuberculosis.

APA, Harvard, Vancouver, ISO, and other styles

24

Neophytou, Christiana M., and Andreas I. Constantinou. "Drug Delivery Innovations for Enhancing the Anticancer Potential of Vitamin E Isoforms and Their Derivatives." BioMed Research International 2015 (2015): 1–16. http://dx.doi.org/10.1155/2015/584862.

Full text

Abstract:

Vitamin E isoforms have been extensively studied for their anticancer properties. Novel drug delivery systems (DDS) that include liposomes, nanoparticles, and micelles are actively being developed to improve Vitamin E delivery. Furthermore, several drug delivery systems that incorporate Vitamin E isoforms have been synthesized in order to increase the bioavailability of chemotherapeutic agents or to provide a synergistic effect. D-alpha-tocopheryl polyethylene glycol succinate (Vitamin E TPGS or TPGS) is a synthetic derivative of natural alpha-tocopherol which is gaining increasing interest in the development of drug delivery systems and has also shown promising anticancer effect as a single agent. This review provides a summary of the properties and anticancer effects of the most potent Vitamin E isoforms and an overview of the various formulations developed to improve their efficacy, with an emphasis on the use of TPGS in drug delivery approaches.

APA, Harvard, Vancouver, ISO, and other styles

25

Kaur, Lakhvir, Subheet Kumar Jain, and Kanwaldeep Singh. "Vitamin E TPGS based nanogel for the skin targeting of high molecular weight anti-fungal drug: development and in vitro and in vivo assessment." RSC Advances 5, no. 66 (2015): 53671–86. http://dx.doi.org/10.1039/c5ra08374e.

Full text

APA, Harvard, Vancouver, ISO, and other styles

26

Mustafa, Sanaul, V. Kusum Devi, and Roopa S. Pai. "Kanamycin Sulphate Loaded PLGA-Vitamin-E-TPGS Long Circulating Nanoparticles Using Combined Coating of PEG and Water-Soluble Chitosan." Journal of Drug Delivery 2017 (March 2, 2017): 1–10. http://dx.doi.org/10.1155/2017/1253294.

Full text

Abstract:

Kanamycin sulphate (KS) is a Mycobacterium tuberculosis protein synthesis inhibitor. Due to its intense hydrophilicity, KS is cleared from the body within 8 h. KS has a very short plasma half-life (2.5 h). KS is used in high concentrations to reach the therapeutic levels in plasma, which results in serious nephrotoxicity/ototoxicity. To overcome aforementioned limitations, the current study aimed to develop KS loaded PLGA-Vitamin-E-TPGS nanoparticles (KS-PLGA-TPGS NPs), to act as an efficient carrier for controlled delivery of KS. To achieve a substantial extension in blood circulation, a combined design, affixation of polyethylene glycol (PEG) to KS-PLGA-TPGS NPs and adsorption of water-soluble chitosan (WSC) (cationic deacetylated chitin) to particle surface, was raised for surface modification of NPs. Surface modified NPs (KS-PEG-WSC NPs) were prepared to provide controlled delivery and circulate in the bloodstream for an extended period of time, thus minimizing dosing frequency. In vivo pharmacokinetics and in vivo biodistribution following intramuscular administration were investigated. NPs surface charge was close to neutral +3.61 mV and significantly affected by the WSC coating. KS-PEG-WSC NPs presented striking prolongation in blood circulation, reduced protein binding, and long drew-out the blood circulation half-life with resultant reduced kidney sequestration vis-à-vis KS-PLGA-TPGS NPs. The studies, therefore, indicate the successful formulation development of KS-PEG-WSC NPs with reduced frequency of dosing of KS indicating low incidence of nephrotoxicity/ototoxicity.

APA, Harvard, Vancouver, ISO, and other styles

27

Guo, Yuanyuan, Boning Niu, Qingle Song, Yongdan Zhao, Yuling Bao, Songwei Tan, Luqin Si, and Zhiping Zhang. "RGD-decorated redox-responsived-α-tocopherol polyethylene glycol succinate–poly(lactide) nanoparticles for targeted drug delivery." Journal of Materials Chemistry B 4, no. 13 (2016): 2338–50. http://dx.doi.org/10.1039/c6tb00055j.

Full text

APA, Harvard, Vancouver, ISO, and other styles

28

Jiang, Weihua, Lei Yang, Lipeng Qiu, Jingwen Xu, Xiuchun Yang, Ju Wang, Hui Zhou, and Dongkai Wang. "Multifunctional hybrid nanoparticles based on sodium carboxymethylcellulose-graft-histidine and TPGS for enhanced effect of docetaxel." RSC Advances 5, no. 66 (2015): 53835–45. http://dx.doi.org/10.1039/c5ra05586e.

Full text

APA, Harvard, Vancouver, ISO, and other styles

29

Pescina, Lucca, Govoni, Padula, Favero, Cantù, Santi, and Nicoli. "Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric Micelles." Pharmaceutics 11, no. 9 (September 14, 2019): 476. http://dx.doi.org/10.3390/pharmaceutics11090476.

Full text

Abstract:

This paper addresses the problem of ocular delivery of lipophilic drugs. The aim of the paper is the evaluation of polymeric micelles, prepared using TPGS (d-α-Tocopheryl polyethylene glycol 1000 succinate), a water-soluble derivative of Vitamin E and/or poloxamer 407, as a vehicle for the ocular delivery of dexamethasone, cyclosporine, and econazole nitrate. The research steps were: (1) characterize polymeric micelles by dynamic light scattering (DLS) and X-ray scattering; (2) evaluate the solubility increase of the three drugs; (3) measure the in vitro transport and conjunctiva retention, in comparison to conventional vehicles; (4) investigate the mechanisms of enhancement, by studying drug release from the micelles and transconjunctival permeation of TPGS; and (5) study the effect of micelles application on the histology of conjunctiva. The data obtained demonstrate the application potential of polymeric micelles in ocular delivery, due to their ability to increase the solubility of lipophilic drugs and enhance transport in and across the conjunctival epithelium. The best-performing formulation was the one made of TPGS alone (micelles size ≈ 12 nm), probably because of the higher mobility of these micelles, an enhanced interaction with the conjunctival epithelium, and, possibly, the penetration of intact micelles.

APA, Harvard, Vancouver, ISO, and other styles

30

Cuevas-Carballo, Z. B., S. Duarte-Aranda, and G. Canché-Escamilla. "Properties and Biodegradability of Thermoplastic Starch Obtained from Granular Starches Grafted with Polycaprolactone." International Journal of Polymer Science 2017 (2017): 1–13. http://dx.doi.org/10.1155/2017/3975692.

Full text

Abstract:

Granular starches grafted with polycaprolactone (St-g-PCL) were obtained using N-methylimidazole (NMI) as a catalyst. The effect of the starch/monomer ratio and catalyst content was studied to obtain different levels of grafted PCL. The highest grafting percentage (76%) and addition (43%) were achieved for reactions with a starch/monomer ratio of 50/50 and 25% catalyst. The grafting of PCL on the starch granule was verified by the emergence of the carbonyl group in the FTIR spectra and the increased diameter of the grafted starch granule. Thermoplastic starch from ungrafted starch (TPS) and grafted starch (TPGS) was obtained by mixing ungrafted or grafted starch granules with water, glycerol, or sorbitol in a mixer. TPS and TPGS behave as plastic materials, and their mechanical properties depend on the type of plasticizer used. Materials with glycerol as the plasticizer exhibited less rigidity. The presence of starch-g-PCL results in a dramatic increase in the elongation of the thermoplastic material. The starch present in the TPS or TPGS was completely biodegraded while the grafted PCL was partially biodegraded after the enzymatic degradation of the materials.

APA, Harvard, Vancouver, ISO, and other styles

31

BAGHERI, S., S. M. HASSANI, and H. GHAHREMANI. "Computational Procedure for Determining Physicochemical Properties of Doxorubicin-TPGS and Daunorubicin-TPGS as Anticancer Agents." Oriental Journal Of Chemistry 28, no. 2 (June 18, 2012): 835–40. http://dx.doi.org/10.13005/ojc/280224.

Full text

APA, Harvard, Vancouver, ISO, and other styles

32

Wang, Teng, Dunwan Zhu, Gan Liu, Wei Tao, Wei Cao, Linhua Zhang, Lijun Wang, et al. "DTX-loaded star-shaped TAPP-PLA-b-TPGS nanoparticles for cancer chemical and photodynamic combination therapy." RSC Advances 5, no. 62 (2015): 50617–27. http://dx.doi.org/10.1039/c5ra09042c.

Full text

APA, Harvard, Vancouver, ISO, and other styles

33

Shi, Chunhuan, Zhiqing Zhang, Fang Wang, Xiaoqing Ji, Zhongxi Zhao, and Yuxia Luan. "Docetaxel-loaded PEO–PPO–PCL/TPGS mixed micelles for overcoming multidrug resistance and enhancing antitumor efficacy." Journal of Materials Chemistry B 3, no. 20 (2015): 4259–71. http://dx.doi.org/10.1039/c5tb00401b.

Full text

APA, Harvard, Vancouver, ISO, and other styles

34

Isley, Nicholas A., Roscoe T. H. Linstadt, Eric D. Slack, and Bruce H. Lipshutz. "Copper-catalyzed hydrophosphinations of styrenes in water at room temperature." Dalton Trans. 43, no. 35 (2014): 13196–200. http://dx.doi.org/10.1039/c4dt00993b.

Full text

APA, Harvard, Vancouver, ISO, and other styles

35

Shi, Qiang, Xiaodong Xu, Qunfu Fan, Jianwen Hou, Wei Ye, and Jinghua Yin. "Construction of d-α-tocopheryl polyethylene glycol succinate/PEO core–shell nanofibers on a blood-contacting surface to reduce the hemolysis of preserved erythrocytes." Journal of Materials Chemistry B 3, no. 10 (2015): 2119–26. http://dx.doi.org/10.1039/c4tb01854k.

Full text

APA, Harvard, Vancouver, ISO, and other styles

36

Lian, Daizheng, Yuhan Chen, Gang Xu, Xiaowei Zeng, Zhuangling Li, Zihuang Li, Yayan Zhou, Lin Mei, and Xianming Li. "Delivery of siRNA targeting HIF-1α loaded chitosan modifiedd-α-tocopheryl polyethylene glycol 1000 succinate-b-poly(ε-caprolactone-ran-glycolide) nanoparticles into nasopharyngeal carcinoma cell to improve the therapeutic efficacy of cisplatin." RSC Advances 6, no. 44 (2016): 37740–49. http://dx.doi.org/10.1039/c6ra03440c.

Full text

APA, Harvard, Vancouver, ISO, and other styles

37

Khare, Vaibhav, Wejdan Al Sakarchi, Prem N. Gupta, Anthony D. M. Curtis, and Clare Hoskins. "Correction: Synthesis and characterization of TPGS–gemcitabine prodrug micelles for pancreatic cancer therapy." RSC Advances 7, no. 21 (2017): 12598. http://dx.doi.org/10.1039/c7ra90021j.

Full text

APA, Harvard, Vancouver, ISO, and other styles

38

Cortes-Clerget, Margery, Jean-Yves Berthon, Isabelle Krolikiewicz-Renimel, Laurent Chaisemartin, and Bruce H. Lipshutz. "Tandem deprotection/coupling for peptide synthesis in water at room temperature." Green Chemistry 19, no. 18 (2017): 4263–67. http://dx.doi.org/10.1039/c7gc01575e.

Full text

APA, Harvard, Vancouver, ISO, and other styles

39

Khare, Vaibhav, Wejdan Al Sakarchi, Prem N. Gupta, Anthony D. M. Curtis, and Clare Hoskins. "Further correction: Synthesis and characterization of TPGS–gemcitabine prodrug micelles for pancreatic cancer therapy." RSC Advances 7, no. 28 (2017): 17367. http://dx.doi.org/10.1039/c7ra90041d.

Full text

APA, Harvard, Vancouver, ISO, and other styles

40

Vuddanda, Parameswara Rao, Vijayakumar Mahalingam Rajamanickam, Madhu Yaspal, and Sanjay Singh. "Investigations on Agglomeration and Haemocompatibility of Vitamin E TPGS Surface Modified Berberine Chloride Nanoparticles." BioMed Research International 2014 (2014): 1–11. http://dx.doi.org/10.1155/2014/951942.

Full text

Abstract:

The objective of the present study is to investigate the influence of surface modification on systemic stability of NPs. Vitamin E TPGS (1% w/v) was used for surface modification of berberine chloride nanoparticles. Naked and surface modified NPs were incubated in different SBFs (pH 6.8 and 7.4) with or without bile salts and human plasma. NPs were observed for particle agglomeration and morphology by particle size analyzer and TEM, respectively. The haemocompatibility studies were conducted on developed NPs to evaluate their safety profile. The surface modified NPs were stable compared to naked NPs in different SBFs due to the steric stabilization property of vitamin E TPGS. Particle agglomeration was not seen when NPs were incubated in SBF (pH 6.8) with bile salts. No agglomeration was observed in NPs after their incubation in plasma but particle size of the naked NPs increased due to adhesion of plasma proteins. The TEM images confirmed the particle size results. DSC and FT-IR studies confirmed the coexistence of TPGS in surface modified NPs. The permissible haemolysis, LDH release, and platelet aggregation revealed that NPs were compatible for systemic administration. Thus, the study illustrated that the surface modification is helpful in the maintenance of stability of NPs in systemic conditions.

APA, Harvard, Vancouver, ISO, and other styles

41

Rehman, Saleha, Bushra Nabi, Mohammad Fazil, Saba Khan, Naimat Kalim Bari, Romi Singh, Shavej Ahmad, Varinder Kumar, Sanjula Baboota, and Javed Ali. "Role of P-Glycoprotein Inhibitors in the Bioavailability Enhancement of Solid Dispersion of Darunavir." BioMed Research International 2017 (2017): 1–17. http://dx.doi.org/10.1155/2017/8274927.

Full text

Abstract:

Objective. The aim of the present study was to improve bioavailability of an important antiretroviral drug, Darunavir (DRV), which has low water solubility and poor intestinal absorption through solid dispersion (SD) approach incorporating polymer with P-glycoprotein inhibitory potential. Methods. A statistical approach where design of experiment (DoE) was used to prepare SD of DRV with incorporation of P-glycoprotein inhibitors. Using DoE, different methods of preparation, like melt, solvent evaporation, and spray drying method, utilizing carriers like Kolliphor TPGS and Soluplus were evaluated. The optimized SD was characterized by DSC, FTIR, XRD, and SEM and further evaluated for enhancement in absorption using everted gut sac model, effect of food on absorption of DRV, and in vivo prospect. Results and Discussion. DSC, FTIR, XRD, and SEM confirmed the amorphicity of drug in SD. Oral bioavailability studies revealed better absorption of DRV when given with food. Absorption studies and in vivo study findings demonstrated great potential of Kolliphor TPGS as P-glycoprotein inhibitor for increasing intestinal absorption and thus bioavailability of DRV. Conclusion. It is concluded that SD of DRV with the incorporation of Kolliphor TPGS was potential and promising approach in increasing bioavailability of DRV as well as minimizing its extrusion via P-glycoprotein efflux transporters.

APA, Harvard, Vancouver, ISO, and other styles

42

Kang, Xu-Qi, Yue Qiao, Xiao-Yang Lu, Sai-Ping Jiang, Wei-Shuo Li, Xiao-Juan Wang, Xiao-Ling Xu, Jing Qi, Yong-Hong Xiao, and Yong-Zhong Du. "Tocopherol polyethylene glycol succinate-modified hollow silver nanoparticles for combating bacteria-resistance." Biomaterials Science 7, no. 6 (2019): 2520–32. http://dx.doi.org/10.1039/c9bm00343f.

Full text

APA, Harvard, Vancouver, ISO, and other styles

43

Li, Chunming, Bing Cai, Jing Jin, Jingchuan Liu, Xiaodong Xu, Jinghua Yin, and Ligang Yin. "Hemocompatible, antioxidative and antibacterial polypropylene prepared by attaching silver nanoparticles capped with TPGS." Journal of Materials Chemistry B 3, no. 42 (2015): 8410–20. http://dx.doi.org/10.1039/c5tb01554e.

Full text

APA, Harvard, Vancouver, ISO, and other styles

44

Pawar, Atmaram, Rabiya Patel, S. Arulmozhi, and C. Bothiraja. "d-α-Tocopheryl polyethylene glycol 1000 succinate conjugated folic acid nanomicelles: towards enhanced bioavailability, stability, safety, prolonged drug release and synergized anticancer effect of plumbagin." RSC Advances 6, no. 81 (2016): 78106–21. http://dx.doi.org/10.1039/c6ra12714b.

Full text

Abstract:

Plumbagin (PLB) loadedd-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) with folic acid (FOL) conjugated nanomicelles achieved controlled and targeted delivery with synergized anticancer potency and reduced PLB toxicity.

APA, Harvard, Vancouver, ISO, and other styles

45

Cao, Xi, Xu Zhou, Yu Wang, Tao Gong, Zhi-Rong Zhang, Renhe Liu, and Yao Fu. "Diblock- and triblock-copolymer based mixed micelles with high tumor penetration in vitro and in vivo." Journal of Materials Chemistry B 4, no. 19 (2016): 3216–24. http://dx.doi.org/10.1039/c6tb00508j.

Full text

APA, Harvard, Vancouver, ISO, and other styles

46

Caruso, Ciro, Daniela Eletto, Michele Rinaldi, Luigi Pacente, Salvatore Troisi, Francesco Semeraro, Roberto dell’Omo, and Ciro Costagliola. "Effectiveness and Safety of Topical Chlorhexidine and Vitamin E TPGS in the Treatment of Acanthamoeba Keratitis: A Survey on 29 Cases." Journal of Clinical Medicine 9, no. 11 (November 23, 2020): 3775. http://dx.doi.org/10.3390/jcm9113775.

Full text

Abstract:

This study aimed to test the effectiveness of a solution of chlorhexidine (CHX) and D-α-tocopheryl polyethylene glycol succinate (Vitamin E TPGS or TPGS) in the treatment of Acanthamoeba keratitis (AK) via a prospective, interventional case series study. Twenty-nine consecutive patients with AK were enrolled. At baseline, best-corrected visual acuity (BCVA), slit lamp examination, confocal microscopy, and polymerase chain reaction (PCR) were performed. Topical therapy with CHX 0.02% and VE-TPGS 0.2% was administered hourly/24 h for the first day, hourly in the daytime for the next three days, and finally, every two hours in the daytime up to one month. BCVA and ocular inflammation were recorded after two weeks, four weeks, and three months from baseline. Mean logMAR BCVA significantly improved at two weeks (0.78) compared to baseline (1.76), remaining stable over time (0.80 at four weeks, 0.77 at three months). Ocular inflammation improved in 14 eyes at 2 weeks, with further slow improvements in all cases. At three months, no patient had signs of corneal inflammation. The presence of corneal scars was first recorded at the two-week follow-up, with an enlargement at the four-week follow-up. At the three-month follow-up, 19 eyes still showed corneal opacities. In conclusion, the tested solution was shown to be effective for the treatment of AK. Furthermore, it might represent a good first-line treatment.

APA, Harvard, Vancouver, ISO, and other styles

47

He, Jiali, Yue Han, Gujun Xu, Lifang Yin, M. Ngandeu Neubi, Jianping Zhou, and Yang Ding. "Preparation and evaluation of celecoxib nanosuspensions for bioavailability enhancement." RSC Advances 7, no. 22 (2017): 13053–64. http://dx.doi.org/10.1039/c6ra28676c.

Full text

Abstract:

We prepare celecoxib nanosuspensions using TPGS as stabilizer via high speed shear as a pre-treatment step, followed by HPH method; and the solidification of fresh nanosuspension was carried out by freeze-drying.

APA, Harvard, Vancouver, ISO, and other styles

48

Li, Kaichun, Liying Pang, Xiaorong Pan, Shaonan Fan, Xinxin Wang, Qiaoyun Wang, Ping Dai, Wei Gao, and Jie Gao. "GE11 Modified PLGA/TPGS Nanoparticles Targeting Delivery of Salinomycin to Breast Cancer Cells." Technology in Cancer Research & Treatment 20 (January 1, 2021): 153303382110049. http://dx.doi.org/10.1177/15330338211004954.

Full text

Abstract:

Salinomycin (Sal) is a potent inhibitor with effective anti-breast cancer properties in clinical therapy. The occurrence of various side effect of Sal greatly limits its application. The epidermal growth factor receptor (EGFR) family is a family of receptors highly expressed in most breast cancer cells. GE11 is a dodecapeptide which shows excellent EGFR affinity. A series of nanoparticles derivatives with GE11 peptide conjugated PLGA/TPGS were synthesized. Nanoprecipitation method was used to prepare the Sal loaded nanoparticles at the optimized concentration. The characterization, targeting efficacy, and antitumor activity were detected both in vitro and in vivo. Encapsulation of Sal in GE11 modified PLGA/TPGS nanoparticles shows an improved therapy efficacy and lower systemic side effect. This represents the delivery system a promising strategy to enhance the therapeutic effect against EGFR highly expressed breast cancer.

APA, Harvard, Vancouver, ISO, and other styles

49

Jain, Sanyog, Sindhu Kambam, Kaushik Thanki, and Amit K. Jain. "Cyclosporine A loaded self-nanoemulsifying drug delivery system (SNEDDS): implication of a functional excipient based co-encapsulation strategy on oral bioavailability and nephrotoxicity." RSC Advances 5, no. 61 (2015): 49633–42. http://dx.doi.org/10.1039/c5ra04762e.

Full text

Abstract:

The present work focusses on the formulation development and evaluation of a functional excipient, a vitamin E TPGS loaded self-nanoemulsifying drug delivery system, for improving the deliverability and safety profile of cyclosporine A.

APA, Harvard, Vancouver, ISO, and other styles

50

Jadhav, Prakash, C. Bothiraja, and Atmaram Pawar. "Resveratrol-piperine loaded mixed micelles: formulation, characterization, bioavailability, safety and in vitro anticancer activity." RSC Advances 6, no. 114 (2016): 112795–805. http://dx.doi.org/10.1039/c6ra24595a.

Full text

Abstract:

Novel RES-carrying piperine loaded mixed micelles (RES-P-MM) composed of Poloxamer 407 and d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) were developed to enhance the solubility, oral bioavailability and anticancer potency of RES.

APA, Harvard, Vancouver, ISO, and other styles

Journal articles on the topic 'TPGS'

Create a spot-on reference in APA, MLA, Chicago, Harvard, and other styles