scholarly journals Solubilization Methods for Paclitaxel and Docetaxel: An Overview

2021 ◽  
Author(s):  
Fariba Pourkarim ◽  
Elaheh Rahimpour ◽  
Sima Alvani ◽  
Abolghasem Jouyban
Keyword(s):  
Anticancer Drugs ◽  
Intravenous Infusion ◽  
Water Solubility ◽  
Inclusion Complexation ◽  
Aqueous Solubility ◽  
Micellar Solubilization ◽  
The Past ◽  
The Poor ◽  
High Incidence ◽  
Serious Disease

Cancer is still a serious disease with high incidence over the past decades. Many anticancer drugs are discovered and used to treat cancer, among them, taxanes such as paclitaxel and docetaxel have high lipophilicity and low aqueous solubility which is further magnified considering the strong need for administering them by intravenous infusion. Currently, the poor water-solubility of taxanes is improved by prodrug formation, conjugation, inclusion complexation, micellar solubilization and liposome-based formulations. Recent achievement for solubilization of taxanes are reviewed and critically discussed regarding their pharmaceutical and chemical applications.

Recent Trends in Nanocrystals for Pharmaceutical Applications

2018 ◽  
Vol 24 (21) ◽  
pp. 2394-2402 ◽  
Author(s):  
Leming Sun ◽  
Yanzi Hu ◽  
Lianbing Zhang
Keyword(s):  
Water Solubility ◽  
New Drugs ◽  
Future Trends ◽  
Design And Development ◽  
The Past ◽  
Pharmaceutical Application ◽  
The Poor ◽  
Pharmaceutical Applications ◽  
Recent Trends ◽  
Administration Methods

Background: As the quick development of modern methods and technologies currently, more and more drugs have been invented with a better efficiency. However, the poor water solubility has limited the drugs’ pharmaceutical application. Methods: Tremendous research has been put in the design and development of nanocrystals for pharmaceutical applications over the past few decades. The nanocrystals not only have the chance to solve the poor solubility problem, but also could conquer the bioavailability and even the specific delivery problems. The physical properties of drugs can be changed dramatically due to the change of their size in a nanodimension. Therefore, the nanocrystals have great potential to overcome the challenge to design and development of new drugs for pharmaceutical applications. Results: In this review, we provide an overview of the recent trends in nanocrystals for pharmaceutical applications. Conclusion: The current technologies including top-down, bottom-up, and combinative technologies for nanocrystals were fully examined. Most importantly, the emphasis is put on the pharmaceutical applications including their formulation, administration methods, safety, and toxicity. The commercial status, limitations, challenges, and future trends of the nanocrystals for pharmaceutical applications were also discussed.

scholarly journals Microtubule Destabilizing Sulfonamides as an Alternative to Taxane-Based Chemotherapy

2021 ◽  
Vol 22 (4) ◽  
pp. 1907
Author(s):  
Myriam González ◽  
María Ovejero-Sánchez ◽  
Alba Vicente-Blázquez ◽  
Raquel Álvarez ◽  
Ana B. Herrero ◽  
...  
Keyword(s):  
Water Solubility ◽  
Aqueous Solubility ◽  
Carcinoma Cells ◽  
Mitotic Catastrophe ◽  
Multi Drug Resistance ◽  
Cervix Carcinoma ◽  
Microtubule Network ◽  
Incidence And Mortality ◽  
High Incidence

Pan-Gyn cancers entail 1 in 5 cancer cases worldwide, breast cancer being the most commonly diagnosed and responsible for most cancer deaths in women. The high incidence and mortality of these malignancies, together with the handicaps of taxanes—first-line treatments—turn the development of alternative therapeutics into an urgency. Taxanes exhibit low water solubility that require formulations that involve side effects. These drugs are often associated with dose-limiting toxicities and with the appearance of multi-drug resistance (MDR). Here, we propose targeting tubulin with compounds directed to the colchicine site, as their smaller size offer pharmacokinetic advantages and make them less prone to MDR efflux. We have prepared 52 new Microtubule Destabilizing Sulfonamides (MDS) that mostly avoid MDR-mediated resistance and with improved aqueous solubility. The most potent compounds, N-methyl-N-(3,4,5-trimethoxyphenyl-4-methylaminobenzenesulfonamide 38, N-methyl-N-(3,4,5-trimethoxyphenyl-4-methoxy-3-aminobenzenesulfonamide 42, and N-benzyl-N-(3,4,5-trimethoxyphenyl-4-methoxy-3-aminobenzenesulfonamide 45 show nanomolar antiproliferative potencies against ovarian, breast, and cervix carcinoma cells, similar or even better than paclitaxel. Compounds behave as tubulin-binding agents, causing an evident disruption of the microtubule network, in vitro Tubulin Polymerization Inhibition (TPI), and mitotic catastrophe followed by apoptosis. Our results suggest that these novel MDS may be promising alternatives to taxane-based chemotherapy in chemoresistant Pan-Gyn cancers.

Utilization of Lipid-based Nanoparticles to Improve the Therapeutic Benefits of Bortezomib

2020 ◽  
Vol 20 (6) ◽  
pp. 643-650 ◽  
Author(s):  
Mitra Korani ◽  
Shahla Korani ◽  
Elham Zendehdel ◽  
Mahmoud R. Jaafari ◽  
Thozhukat Sathyapalan ◽  
...  
Keyword(s):  
Proteasome Inhibitor ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Cell Lymphoma ◽  
Aqueous Solubility ◽  
Therapeutic Benefits ◽  
Mantle Cell ◽  
The Us ◽  
High Incidence ◽  
And Control

Cancer is a condition where there is an uncontrolled growth of cells resulting in high mortality. It is the second most frequent cause of death worldwide. Bortezomib (BTZ) is a Proteasome Inhibitor (PI) that is used for the treatment of a variety of cancers. It is the first PI that has received the approval of the US Food and Drug Administration (FDA) to treat mantle cell lymphoma and multiple myeloma. High incidence of sideeffects, limited dose, low water solubility, fast clearance, and drug resistance are the significant limitations of BTZ. Therefore, various drug delivery systems have been tried to overcome these limitations of BTZ in cancer therapy. Nanotechnology can potentially enhance the aqueous solubility of BTZ, increase its bioavailability, and control the release of BTZ at the site of administration. The lipid-based nanocarriers, such as liposomes, solid lipid NPs, and microemulsions, are some of the developments in nanotechnology, which could potentially enhance the therapeutic benefits of BTZ.

High-Resolution, Low-Voltage SEM of Cell Wall Regeneration of Yeast Shizosaccharomyces Pombe Protoplasts

1988 ◽  
Vol 46 ◽  
pp. 208-211
Author(s):  
M. Osumi ◽  
N. Yamada ◽  
T. Nagatani
Keyword(s):  
Electron Microscope ◽  
Scanning Electron Microscope ◽  
Low Voltage ◽  
Cell Wall Regeneration ◽  
The Past ◽  
The Poor ◽  
Probe Size ◽  
Beam Damage ◽  
Biological Field ◽  
Scanning Electron

Even though many early workers had suggested the use of lower voltages to increase topographic contrast and to reduce specimen charging and beam damage, we did not usually operate in the conventional scanning electron microscope at low voltage because of the poor resolution, especially of bioligical specimens. However, the development of the “in-lens” field emission scanning electron microscope (FESEM) has led to marked inprovement in resolution, especially in the range of 1-5 kV, within the past year. The probe size has been cumulated to be 0.7nm in diameter at 30kV and about 3nm at 1kV. We have been trying to develop techniques to use this in-lens FESEM at low voltage (LVSEM) for direct observation of totally uncoated biological specimens and have developed the LVSEM method for the biological field.

Theodore W. Schultz. The Economics of Being Poor. Oxford: Blackwell. 1993. ix+340 pp.+ Index. Hardbound. £ 40.00.

1995 ◽  
Vol 34 (1) ◽  
pp. 84-85
Author(s):  
Mir Annice Mahmood
Keyword(s):  
Economic Policy ◽  
Human Capital ◽  
Policy Formulation ◽  
The Past ◽  
The Poor ◽  
Logical Sequence ◽  
Standards Of Living ◽  
Economic Journals ◽  
Material Conditions ◽  
Demand For Children

Improving the material conditions of the poor has been the main focus of economic policy formulation for the past fifty years or so. Thus, in this connection, a vast body of literature has been published which deals with such issues as identifying the poor and suggesting remedies to alleviate their lot. The book by Theodore W. Schultz deals specifically with the economics of the poor. The book is primarily a collection of articles the author wrote over a fortyyear period (1950-1990), and these have been published previously in a number of leading economic journals. The articles have been grouped under three headings: "Most People Are Poor"; "Investing in Skills and Knowledge"; and "Effects of Human Capital". The articles basically deal with the concept of human capital. There is a logical sequence to the articles that make up this book; the poor are identified and steps are then suggested to improve their standing. Issues such as women's economic emancipation and the demand for children are highlighted in the collection of articles dealing with these two subjects. By investing in themselves through education, the poor raise their level of skills, and thus their level of wages/salaries, allowing them to enjoy higher standards of living.

NMR Studies of the Inclusion Complexes Between Ezetimibe and Cyclodextrins

2018 ◽  
Vol 69 (7) ◽  
pp. 1838-1841
Author(s):  
Hajnal Kelemen ◽  
Angella Csillag ◽  
Bela Noszal ◽  
Gabor Orgovan
Keyword(s):  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Water Solubility ◽  
Solution Nmr ◽  
Spectroscopic Techniques ◽  
Nmr Studies ◽  
The Poor ◽  
Poor Water Solubility

Ezetimibe, the antihyperlipidemic drug of poor bioavailability was complexed with native and derivatized cyclodextrins.The complexes were characterized in terms stability, stoichiometry and structure using various 1D and 2D solution NMR spectroscopic techniques. The complexes were found to be of moderate stability (logK[3). The least stable inclusion complex is formed with b-cyclodextrin, while the ezetimibe-methylated-b--cyclodextrin has a 7-fold higher stability. The results can be useful to improve the poor water-solubility and the concomitant bioavailability of ezetimibe.

Oleanolic Acid Derived from Plants: Synthesis and Pharmacological Properties of A-ring Modified Derivatives

2020 ◽  
Vol 17 (9) ◽  
pp. 1084-1101
Author(s):  
Tingjuan Wu ◽  
Xu Yao ◽  
Guan Wang ◽  
Xiaohe Liu ◽  
Hongfei Chen ◽  
...  
Keyword(s):  
Drug Design ◽  
Oleanolic Acid ◽  
Water Solubility ◽  
Future Application ◽  
The Novel ◽  
Pharmacological Effects ◽  
Framework Structure ◽  
Design And Synthesis ◽  
The Past ◽  
The Relationship

Background: Oleanolic Acid (OA) is a ubiquitous product of triterpenoid compounds. Due to its inexpensive availability, unique bioactivities, pharmacological effects and non-toxic properties, OA has attracted tremendous interest in the field of drug design and synthesis. Furthermore, many OA derivatives have been developed for ameliorating the poor water solubility and bioavailability. Objective: Over the past few decades, various modifications of the OA framework structure have led to the observation of enhancement in bioactivity. Herein, we focused on the synthesis and medicinal performance of OA derivatives modified on A-ring. Moreover, we clarified the relationship between structures and activities of OA derivatives with different functional groups in A-ring. The future application of OA in the field of drug design and development also was discussed and inferred. Conclusion: This review concluded the novel achievements that could add paramount information to the further study of OA-based drugs.

scholarly journals Survey of Glyphosate-Resistant Junglerice Accessions in Dicamba-Resistant Crops in Tennessee

2020 ◽  
pp. 1-31
Author(s):  
Clay M. Perkins ◽  
Thomas C. Mueller ◽  
Lawrence E. Steckel
Keyword(s):  
Resistance Factor ◽  
Relative Resistance ◽  
Roundup Ready ◽  
The Past ◽  
Growing Seasons ◽  
The Poor

Abstract Junglerice has become a major weed in Tennessee cotton and soybean fields. Glyphosate has been relied upon to control these accessions over the past two decades but in recent years cotton and soybean producers have reported junglerice escapes after glyphosate + dicamba and/or clethodim applications. In the growing seasons of 2018 and 2019, a survey was conducted of weed escapes in dicamba-resistant crops. Junglerice was the most prevalent weed escape in these dicamba-resistant (Roundup Ready Xtend®) cotton and soybean fields in both years of the study. In 2018 and 2019, junglerice was found 76% and 64% of the time in dicamba-resistant cotton and soybean fields, respectively. Progeny from junglerice seeds collected during this survey was screened for glyphosate and clethodim resistance. Seventy percent of the junglerice accessions tested had an effective relative resistance factor (RRF) of 3.1 to 8.5 to glyphosate. In all, 13% of the junglerice accessions could no longer be effectively controlled with glyphosate. This research also showed that all sampled accessions could still be controlled with clethodim in a greenhouse environment but less control was observed in the field. These data would also suggest that another cause for the poor junglerice control is dicamba antagonizing the glyphosate and clethodim activity.

A case of two spellings for Humboldt’s blue-winged mosquito (Diptera: Culicidae)

Zootaxa ◽  
2021 ◽  
Vol 4974 (1) ◽  
pp. 191-192
Author(s):  
RALPH E. HARBACH ◽  
NEAL L. EVENHUIS
Keyword(s):  
Mosquito Species ◽  
Know How ◽  
The Past ◽  
The Poor ◽  
Magdalena River ◽  
Perceived Color ◽  
Dark Blue

While adding taxon names to the Systema Dipterorum database (Evenhuis & Pape 2021), one of us (NLE) discovered that Humboldt (1819) had spelled the proposed name of a nominal mosquito species in two ways. He described the species, which was found in swampy places along the Magdalena River near Tenerife, Colombia, as Culex cyanopennis on page 340 and afterwards referred to it as Culex cyanopterus on pages 345 and 349. Both names have the same meaning: cyano- (Gr. kyanos, dark blue), pennis (L. penna, feather, wing) and pteron (Gr. feather, wing). The species was named for the perceived color of the wings: “Alæ cæruleæ, splendore semi-metallico…” (wings blue, a bright semi-metallic). On page 345, Humboldt states, translated from the French: “We have been informed in the Rio de la Magdalena that in Simitì no other Culex than the jejen [je·jén: Sp., gnat, mosquito] was known in the past. You can spend the night there quietly, because the jejen is not a nocturnal insect. Since the year 1801, the big blue-winged mosquito (Culex cyanopterus) has shown itself in such abundance that the poor inhabitants of Simitì do not know how to get a peaceful sleep.” Thus, in addition to having the same meaning, the two names are associated with the same locality. 

A Review on Formulation and Development of Solid Self-Nano Emulsifying Drug Delivery Systems

2021 ◽  
Vol 14 (4) ◽  
pp. 5519-5228
Author(s):  
Sunitha M Reddy ◽  
Sravani Baskarla
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Drug Loading ◽  
Aqueous Solubility ◽  
Delivery Systems ◽  
Particle Size Reduction

This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.  

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