The Experts below are selected from a list of 71691 Experts worldwide ranked by ideXlab platform
Abraham Joy - One of the best experts on this subject based on the ideXlab platform.
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folate receptor targeted polymeric micellar nanocarriers for delivery of orlistat as a repurposed Drug against triple negative breast cancer
Molecular Cancer Therapeutics, 2016Co-Authors: Ramasamy Paulmurugan, Rohith Bhethanabotla, Kaushik Mishra, Rammohan Devulapally, Kira Foygel, Thillai V Sekar, Jeyarama S Ananta, Tarik F Massoud, Abraham JoyAbstract:Triple-negative breast cancer (TNBC) is a recalcitrant malignancy with no available targeted therapy. Off-target effects and poor bioavailability of the FDA-approved antiobesity Drug orlistat hinder its clinical translation as a repurposed new Drug against TNBC. Here, we demonstrate a newly engineered Drug Formulation for packaging orlistat tailored to TNBC treatment. We synthesized TNBC-specific folate receptor-targeted micellar nanoparticles (NP) carrying orlistat, which improved the solubility (70-80 μg/mL) of this water-insoluble Drug. The targeted NPs also improved the delivery and bioavailability of orlistat to MDA-MB-231 cells in culture and to tumor xenografts in a nude mouse model. We prepared HEA-EHA copolymer micellar NPs by copolymerization of 2-hydroxyethylacrylate (HEA) and 2-ethylhexylacrylate (EHA), and functionalized them with folic acid and an imaging dye. Fluorescence-activated cell sorting (FACS) analysis of TNBC cells indicated a dose-dependent increase in apoptotic populations in cells treated with free orlistat, orlistat NPs, and folate-receptor-targeted Fol-HEA-EHA-orlistat NPs in which Fol-HEA-EHA-orlistat NPs showed significantly higher cytotoxicity than free orlistat. In vitro analysis data demonstrated significant apoptosis at nanomolar concentrations in cells activated through caspase-3 and PARP inhibition. In vivo analysis demonstrated significant antitumor effects in living mice after targeted treatment of tumors, and confirmed by fluorescence imaging. Moreover, folate receptor-targeted Fol-DyLight747-orlistat NP-treated mice exhibited significantly higher reduction in tumor volume compared to control group. Taken together, these results indicate that orlistat packaged in HEA-b-EHA micellar NPs is a highly promising new Drug Formulation for TNBC therapy. Mol Cancer Ther; 15(2); 221-31. ©2015 AACR.
Christelle Crampon - One of the best experts on this subject based on the ideXlab platform.
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Current situation and perspectives in Drug Formulation by using supercritical fluid technology
Journal of Supercritical Fluids, 2018Co-Authors: Elisabeth Badens, Yasmine Masmoudi, Adil Mouahid, Christelle CramponAbstract:Supercritical fluid (SCF) technology has been applied to Drug product development over the last thirty years and Drug particle generation using SCFs appears to be an efficient way to carry out Drug Formulation which will form end-products meeting targeted specifications. This article presents an overview of Drug particle design using SCFs from a rather different perspective than usual, more focused on chemical and process engineering aspects. The main types of existing processes are described in a concise way and a focus is put on how to choose the right operating conditions considering both thermodynamic and hydrodynamic aspects. It is shown that the operating conditions and parameters can be easily optimized so as to facilitate the further process scale-up. Furthermore, the new trends in particle generation using SCFs are introduced, related either to new types of Drug medicines that are treated or new ways of process implementation methods.
Rong Liu - One of the best experts on this subject based on the ideXlab platform.
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Comprar Water-Insoluble Drug Formulation | Rong Liu | 9780849396441 | CrcPress
2008Co-Authors: Rong LiuAbstract:Tienda online donde Comprar Water-Insoluble Drug Formulation al precio 302,88 € de Rong Liu, tienda de Libros de Medicina, Libros de Farmacologia Clinica - Farmacologia Clinica
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water insoluble Drug Formulation
2000Co-Authors: Rong LiuAbstract:Introduction, R. Liu Solubility Theories, S.H. Neau Prediction of Solubility, Y. Chen, X. Oi, and R. Liu PreFormulation Aspects of Insoluble Compounds, W.Q. Tong and H. Zhou Water-Insoluble Drugs and their Pharmacokinetic Behaviors, H. Zhou Regulatory Aspects of Dissolution for Low Solubility Drug Products, P. Sathe, R.A. Lionberger, and LX.. Yu Formulation Strategies and Practice Used for Drug Candidates with Water-Insoluble Properties for Toxicology, Biology, and Pharmacology Studies in Discovery Support, L.-F. Huang and J. Dong Applications of Complexation in the Formulation of Insoluble Compounds, W.-Q. Tong and H. Wen Solubilization Using CoSolvent Approach, J.S. Trivedi Emulsions, Microemulsions, and Lipid-based Drug Delivery Systems for Drug Solubilization and Delivery, Part I: Parenteral Applications, J.B. Cannon, Y. Shi, and P. Gupta Emulsions, Microemulsions, and Lipid-based Drug Delivery Systems for Drug Solubilization and Delivery, Part II: Oral Applications, J.B. Cannon and M.A. Long Micellization and Drug Solubility Enhancement, R. Liu and R.-M. Dannenfelser, and S. Li Micellization and Drug Solubility Enhancement Part II: Polymeric Micelles, R. Liu, M.L. Forrest, and G.S. Kwon Liposomes in Solubilization, R. Liu, J.B. Cannon, and Y.S. Paspal Pharmaceutical Salts, S.H. Neau ProDrugs for Improved Aqueous Solubility, S.H. Neau Particle Size Reduction, R.W. Lee, J.M. Shaw, J. McShane, R.W. Wood, and D.B. Shenoy Development of Solid Dispersions for Poorly Water-Soluble Drugs, M. Vasanthavada, W.-Q. Tong, and A. Serajuddin Alternation of the Solid State of the Drug Substances: Polymorphs, Solvates, and Amorphous Forms, P. Myrdal and M.J. Jozwiakowski Pharmaceutical Powder Technology - Building the Pyramid of Knowledge and the Challenge of FDA's PAT Initiative, H. Leuenberger and G. Betz Soft Gelatin Capsules Development, E. Tabibi and S.L. Gupta Oral Modified-Release Drug Delivery for Water-Insoluble Drugs, S. Li, N. Wang, and R. Liu Scalable Manufacturing of Water-Insoluble Drug Products, N. Pathak and R. Huang Drug Products, N. Pathak and R. Huang
Ramasamy Paulmurugan - One of the best experts on this subject based on the ideXlab platform.
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folate receptor targeted polymeric micellar nanocarriers for delivery of orlistat as a repurposed Drug against triple negative breast cancer
Molecular Cancer Therapeutics, 2016Co-Authors: Ramasamy Paulmurugan, Rohith Bhethanabotla, Kaushik Mishra, Rammohan Devulapally, Kira Foygel, Thillai V Sekar, Jeyarama S Ananta, Tarik F Massoud, Abraham JoyAbstract:Triple-negative breast cancer (TNBC) is a recalcitrant malignancy with no available targeted therapy. Off-target effects and poor bioavailability of the FDA-approved antiobesity Drug orlistat hinder its clinical translation as a repurposed new Drug against TNBC. Here, we demonstrate a newly engineered Drug Formulation for packaging orlistat tailored to TNBC treatment. We synthesized TNBC-specific folate receptor-targeted micellar nanoparticles (NP) carrying orlistat, which improved the solubility (70-80 μg/mL) of this water-insoluble Drug. The targeted NPs also improved the delivery and bioavailability of orlistat to MDA-MB-231 cells in culture and to tumor xenografts in a nude mouse model. We prepared HEA-EHA copolymer micellar NPs by copolymerization of 2-hydroxyethylacrylate (HEA) and 2-ethylhexylacrylate (EHA), and functionalized them with folic acid and an imaging dye. Fluorescence-activated cell sorting (FACS) analysis of TNBC cells indicated a dose-dependent increase in apoptotic populations in cells treated with free orlistat, orlistat NPs, and folate-receptor-targeted Fol-HEA-EHA-orlistat NPs in which Fol-HEA-EHA-orlistat NPs showed significantly higher cytotoxicity than free orlistat. In vitro analysis data demonstrated significant apoptosis at nanomolar concentrations in cells activated through caspase-3 and PARP inhibition. In vivo analysis demonstrated significant antitumor effects in living mice after targeted treatment of tumors, and confirmed by fluorescence imaging. Moreover, folate receptor-targeted Fol-DyLight747-orlistat NP-treated mice exhibited significantly higher reduction in tumor volume compared to control group. Taken together, these results indicate that orlistat packaged in HEA-b-EHA micellar NPs is a highly promising new Drug Formulation for TNBC therapy. Mol Cancer Ther; 15(2); 221-31. ©2015 AACR.
Brahmeshwar Mishra - One of the best experts on this subject based on the ideXlab platform.
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Eudragit-Based Nanosuspension of Poorly Water-Soluble Drug: Formulation and In Vitro–In Vivo Evaluation
AAPS PharmSciTech, 2012Co-Authors: Sarita Kumari Yadav, Shivani Mishra, Brahmeshwar MishraAbstract:The present study was performed to investigate potential of Eudragit RLPO-based nanosuspension of glimepiride (Biopharmaceutical Classification System class II Drug), for the improvement of its solubility and overall therapeutic efficacy, suitable for peroral administration. Nanoprecipitation method being simple and less sophisticated was optimized for the preparation of nanosuspension. Physicochemical characteristics of nanosuspension in terms of size, zeta potential, polydispersity index, entrapment efficiency (% EE) and in vitro Drug release were found within their acceptable ranges. The size of the nanoparticles was most strongly affected by agitation time while % EE was more influenced by the Drug/polymer ratio. Differential scanning calorimetry and X-ray diffraction studies provided evidence that enhancement in solubility of Drug resulted due to change in crystallinity of Drug within the Formulation. Stability study revealed that nanosuspension was more stable at refrigerated condition with no significant changes in particle size distribution, % EE, and release characteristics for 3 months. In vivo studies were performed on nicotinamide–streptozotocin-induced diabetic rat models for pharmacokinetic and antihyperglycaemic activity. Nanosuspension increased maximum plasma concentration, area under the curve, and mean residence time values significantly as compared to aqueous suspension. Oral glucose tolerance test and antihyperglycaemic studies demonstrated plasma glucose levels were efficiently controlled in case of nanosuspension than glimepiride suspension. Briefly, sustained and prolonged activity of nanosuspensions could reduce dose frequency, decrease Drug side effects, and improve patient compliance. Therefore, glimepiride nanosuspensions can be expected to gain considerable attention in the treatment of type 2 diabetes mellitus due to its improved therapeutic activity.
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eudragit based nanosuspension of poorly water soluble Drug Formulation and in vitro in vivo evaluation
Aaps Pharmscitech, 2012Co-Authors: Sarita Kumari Yadav, Shivani Mishra, Brahmeshwar MishraAbstract:The present study was performed to investigate potential of Eudragit RLPO-based nanosuspension of glimepiride (Biopharmaceutical Classification System class II Drug), for the improvement of its solubility and overall therapeutic efficacy, suitable for peroral administration. Nanoprecipitation method being simple and less sophisticated was optimized for the preparation of nanosuspension. Physicochemical characteristics of nanosuspension in terms of size, zeta potential, polydispersity index, entrapment efficiency (% EE) and in vitro Drug release were found within their acceptable ranges. The size of the nanoparticles was most strongly affected by agitation time while % EE was more influenced by the Drug/polymer ratio. Differential scanning calorimetry and X-ray diffraction studies provided evidence that enhancement in solubility of Drug resulted due to change in crystallinity of Drug within the Formulation. Stability study revealed that nanosuspension was more stable at refrigerated condition with no significant changes in particle size distribution, % EE, and release characteristics for 3 months. In vivo studies were performed on nicotinamide–streptozotocin-induced diabetic rat models for pharmacokinetic and antihyperglycaemic activity. Nanosuspension increased maximum plasma concentration, area under the curve, and mean residence time values significantly as compared to aqueous suspension. Oral glucose tolerance test and antihyperglycaemic studies demonstrated plasma glucose levels were efficiently controlled in case of nanosuspension than glimepiride suspension. Briefly, sustained and prolonged activity of nanosuspensions could reduce dose frequency, decrease Drug side effects, and improve patient compliance. Therefore, glimepiride nanosuspensions can be expected to gain considerable attention in the treatment of type 2 diabetes mellitus due to its improved therapeutic activity.
