Solubilization of Sagopilone, a poorly water-soluble anticancer drug, using polymeric micelles for parenteral delivery

2010 ◽  
Vol 389 (1-2) ◽  
pp. 244-253 ◽  
Author(s):  
Annett Richter ◽  
Carsten Olbrich ◽  
Michael Krause ◽  
Thomas Kissel
Keyword(s):  
Anticancer Drug ◽  
Polymeric Micelles ◽  
Water Soluble ◽  
Parenteral Delivery ◽  
Poorly Water Soluble

scholarly journals Polymeric Micelles, a Promising Drug Delivery System to Enhance Bioavailability of Poorly Water-Soluble Drugs

2013 ◽  
Vol 2013 ◽  
pp. 1-15 ◽  
Author(s):  
Wei Xu ◽  
Peixue Ling ◽  
Tianmin Zhang
Keyword(s):  
Drug Delivery ◽  
Residence Time ◽  
Oral Delivery ◽  
Polymeric Micelles ◽  
Water Soluble ◽  
Gi Tract ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Accepted Form

Oral administration is the most commonly used and readily accepted form of drug delivery; however, it is find that many drugs are difficult to attain enough bioavailability when administered via this route. Polymeric micelles (PMs) can overcome some limitations of the oral delivery acting as carriers able to enhance drug absorption, by providing (1) protection of the loaded drug from the harsh environment of the GI tract, (2) release of the drug in a controlled manner at target sites, (3) prolongation of the residence time in the gut by mucoadhesion, and (4) inhibition of efflux pumps to improve the drug accumulation. To explain the mechanisms for enhancement of oral bioavailability, we discussed the special stability of PMs, the controlled release properties of pH-sensitive PMs, the prolongation of residence time with mucoadhesive PMs, and the P-gp inhibitors commonly used in PMs, respectively. The primary purpose of this paper is to illustrate the potential of PMs for delivery of poorly water-soluble drugs with bioavailability being well maintained.

Strategies to Maximize Liposomal Drug Loading for a Poorly Water-soluble Anticancer Drug

2014 ◽  
Vol 32 (4) ◽  
pp. 1451-1461 ◽  
Author(s):  
Wenli Zhang ◽  
Guangji Wang ◽  
James R. Falconer ◽  
Bruce C. Baguley ◽  
John P. Shaw ◽  
...  
Keyword(s):  
Anticancer Drug ◽  
Drug Loading ◽  
Water Soluble ◽  
Liposomal Drug ◽  
Poorly Water Soluble

Enhancing the solubility and bioactivity of anticancer drug tamoxifen by water-soluble pillar[6]arene-based host–guest complexation

2017 ◽  
Vol 53 (70) ◽  
pp. 9749-9752 ◽  
Author(s):  
Liqing Shangguan ◽  
Qi Chen ◽  
Bingbing Shi ◽  
Feihe Huang
Keyword(s):  
Anticancer Drug ◽  
Water Soluble ◽  
Poorly Water Soluble

A water-soluble pillar[6]arene functions as a solubilizing agent to enhance the solubility and bioactivity of poorly water-soluble anticancer drug tamoxifen.

Methoxy polyethylene glycol–cholesterol modified soy lecithin liposomes for poorly water‐soluble anticancer drug delivery

2020 ◽  
Vol 138 (7) ◽  
pp. 49858
Author(s):  
Ngoc Thuy Trang Le ◽  
Dinh Tien Dung Nguyen ◽  
Ngoc Hoi Nguyen ◽  
Cuu Khoa Nguyen ◽  
Dai Hai Nguyen
Keyword(s):  
Drug Delivery ◽  
Polyethylene Glycol ◽  
Anticancer Drug ◽  
Water Soluble ◽  
Soy Lecithin ◽  
Anticancer Drug Delivery ◽  
Poorly Water Soluble ◽  
Methoxy Polyethylene Glycol

Non-ionic dendritic glycerol-based amphiphiles: Novel excipients for the solubilization of poorly water-soluble anticancer drug Sagopilone

2010 ◽  
Vol 40 (1) ◽  
pp. 48-55 ◽  
Author(s):  
Annett Richter ◽  
Achim Wiedekind ◽  
Michael Krause ◽  
Thomas Kissel ◽  
Rainer Haag ◽  
...  
Keyword(s):  
Anticancer Drug ◽  
Water Soluble ◽  
Poorly Water Soluble

scholarly journals Lipid-Based Drug Delivery Systems

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Hina Shrestha ◽  
Rajni Bala ◽  
Sandeep Arora
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Parenteral Delivery ◽  
Wide Range ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Principle Objective

The principle objective of formulation of lipid-based drugs is to enhance their bioavailability. The use of lipids in drug delivery is no more a new trend now but is still the promising concept. Lipid-based drug delivery systems (LBDDS) are one of the emerging technologies designed to address challenges like the solubility and bioavailability of poorly water-soluble drugs. Lipid-based formulations can be tailored to meet a wide range of product requirements dictated by disease indication, route of administration, cost consideration, product stability, toxicity, and efficacy. These formulations are also a commercially viable strategy to formulate pharmaceuticals, for topical, oral, pulmonary, or parenteral delivery. In addition, lipid-based formulations have been shown to reduce the toxicity of various drugs by changing the biodistribution of the drug away from sensitive organs. However, the number of applications for lipid-based formulations has expanded as the nature and type of active drugs under investigation have become more varied. This paper mainly focuses on novel lipid-based formulations, namely, emulsions, vesicular systems, and lipid particulate systems and their subcategories as well as on their prominent applications in pharmaceutical drug delivery.

scholarly journals The zebrafish embryo as an in vivo model for screening nanoparticle-formulated lipophilic anti-tuberculosis compounds

2021 ◽  
Author(s):  
Nils-Jørgen Knudsen Dal ◽  
Martin Speth ◽  
Kerstin Johann ◽  
Matthias Barz ◽  
Claire Beauvineau ◽  
...  
Keyword(s):  
Zebrafish Embryo ◽  
Polymeric Micelles ◽  
Water Soluble ◽  
In Vivo Model ◽  
In Vivo Toxicity ◽  
Conventional Animal ◽  
In Vivo Testing ◽  
Poorly Water Soluble

With the increasing emergence of drug-resistant Mycobacterium tuberculosis strains, new and effective antibiotics against tuberculosis (TB) are urgently needed. However, the high frequency of poorly water-soluble compounds among hits in high-throughput drug screening (HTS) campaigns is a major obstacle in drug discovery. Moreover, in vivo testing using conventional animal TB models such as mice is time-consuming and costly, and represents a major bottleneck in lead compound discovery and development. Here, we report the use of the zebrafish embryo TB model, to evaluate the in vivo toxicity and efficacy of five poorly water-soluble nitronaphthofuran derivatives, which were recently identified to possess anti-tuberculosis activity in vitro. To aid solubilization compounds were formulated in biocompatible polymeric micelles (PM). Three of the five PM-formulated nitronaphthofuran derivatives showed low toxicity in vivo, significantly reduced bacterial burden and improved survival in infected zebrafish embryos. We propose the zebrafish embryo TB-model as a quick and sensitive tool for evaluating in vivo toxicity and efficacy of new anti-TB compounds during early stages of drug development. Thus, this model is well suited to pinpoint promising compounds for further development.

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