scholarly journals Ascorbyl palmitate/d-α-tocopheryl polyethylene glycol 1000 succinate monoester mixed micelles for prolonged circulation and targeted delivery of compound K for antilung cancer therapy in vitro and in vivo

2017 ◽  
Vol Volume 12 ◽  
pp. 605-614 ◽  
Author(s):  
Youwen Zhang ◽  
Deyin Tong ◽  
Daobiao Che ◽  
Bing Pei ◽  
Xiaodong Xia ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Cancer Therapy ◽  
Targeted Delivery ◽  
Mixed Micelles ◽  
Ascorbyl Palmitate ◽  
Compound K ◽  
Polyethylene Glycol 1000

scholarly journals Redox-Sensitive Nanocomplex for Targeted Delivery of Melittin

Toxins ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 582 ◽  
Author(s):  
Bei Cheng ◽  
Peisheng Xu
Keyword(s):  
Cancer Therapy ◽  
Targeted Delivery ◽  
Cell Permeability ◽  
Peptide Drug ◽  
New Approach ◽  
The Poor ◽  
Poor Stability ◽  
Target Effects

Although peptide therapeutics have been explored for decades, the successful delivery of potent peptides in vitro and in vivo remains challenging due to the poor stability, low cell permeability, and off-target effects. We developed a redox sensitive polymer-based nanocomplex which can efficiently and stably deliver the peptide drug melittin for cancer therapy. The nanocomplex selectively targets cancer cells through lactobionic acid mediated endocytosis and releases melittin intracellularly upon the trigger of elevated redox potential. In vivo study proved that the targeted nanocomplex shows excellent potency in inhibiting tumor growth in a xenograft colon cancer mouse model. Thus, the polymer/melittin nanocomplexes will provide a new approach for melittin based cancer therapy.

Novel folate-targeted docetaxel-loaded nanoparticles for tumour targeting: in vitro and in vivo evaluation

RSC Advances ◽  
2016 ◽  
Vol 6 (69) ◽  
pp. 64306-64314 ◽  
Author(s):  
M. H. Han ◽  
Z. T. Li ◽  
D. D. Bi ◽  
Y. F. Guo ◽  
H. X. Kuang ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Folic Acid ◽  
Cancer Therapy ◽  
Targeted Delivery ◽  
Tumour Targeting ◽  
Breast Cancer Therapy ◽  
In Vivo Evaluation ◽  
Targeted Delivery System

Cholesterol-PEG1000-FA (folic acid) was synthesized as a stabilizer to encapsulate DTX, for the construction of a promising targeted delivery system for breast cancer therapy.

Folic acid modified copper oxide nanoparticles for targeted delivery in in vitro and in vivo systems

RSC Advances ◽  
2015 ◽  
Vol 5 (83) ◽  
pp. 68169-68178 ◽  
Author(s):  
Dipranjan Laha ◽  
Arindam Pramanik ◽  
Sourav Chattopadhyay ◽  
Sandip kumar Dash ◽  
Somenath Roy ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Folic Acid ◽  
Cancer Therapy ◽  
Copper Oxide ◽  
Targeted Delivery ◽  
Copper Oxide Nanoparticles ◽  
Oxide Nanoparticles ◽  
Breast Cancer Therapy

Targeted delivery of copper oxide nanoparticles for breast cancer therapy.

scholarly journals Poloxamer-188 and d-α-Tocopheryl Polyethylene Glycol Succinate (TPGS-1000) Mixed Micelles Integrated Orodispersible Sublingual Films to Improve Oral Bioavailability of Ebastine; In Vitro and In Vivo Characterization

Pharmaceutics ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 54
Author(s):  
Nayyer Islam ◽  
Muhammad Irfan ◽  
Salah-Ud-Din Khan ◽  
Haroon Khalid Syed ◽  
Muhammad Shahid Iqbal ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Zeta Potential ◽  
Mixed Micelles ◽  
Entrapment Efficiency ◽  
Glycol Succinate ◽  
Disintegration Time ◽  
Poloxamer 188 ◽  
Pure Drug

Orodispersible sublingual films (OSFs) composed of hydrophilic polymers were loaded with poloxamer-188 and d-α-tocopheryl polyethylene glycol succinate (TPGS-1000) mixed micelles to improve the oral bioavailability of a poorly soluble drug, ebastine (EBT). Mixed micelles formed by thin-film hydration method were incorporated into orodispersible sublingual film, consisting of HPMC and glycerol, using solvent casting technique. The mixed micelles and films were thoroughly evaluated for physicochemical characterization (size, polydispersity index, zeta potential, entrapment efficiency, thickness, weight, surface pH studies, disintegration time, swelling indices, mechanical properties, FTIR, PXRD, DSC, SEM, AFM, in vitro drug release, in vivo bioavailability, and toxicological studies). The results showed that the average particle size of mixed micelles was 73 nm. The mean zeta potential and PDI of the optimal mixed micelles formulation were −26 mV and 0.16, respectively. Furthermore, the maximum entrapment efficiency 82% was attained. The film’s disintegration time was in the range of 28 to 102 s in aqueous media. The integrity of micelles was not affected upon incorporation in films. Importantly, the micelles-loaded films revealed rapid absorption, high permeability, and increased bioavailability of EBT as compared to the pure drug. The existence of ebastine loaded mixed micelles in the films enhanced the bioavailability about 2.18 folds as compared to pure drug. Further, the results evidently established in-vitro and in-vivo performance of bioavailability enhancement, biocompatibility, and good safety profile of micelles-loaded orodispersible EBT films. Finally, it was concluded that film loaded with poloxamer-188/TPGS-1000 mixed micelles could be an effective carrier system for enhancing the bioavailability of ebastine.

Cytotoxic Stilbenes and Derivatives as Promising Antimitotic Leads for Cancer Therapy

2019 ◽  
Vol 24 (36) ◽  
pp. 4270-4311 ◽  
Author(s):  
Célia Faustino ◽  
Ana P. Francisco ◽  
Vera M. S. Isca ◽  
Noélia Duarte
Keyword(s):  
Cancer Therapy ◽  
Targeted Delivery ◽  
Biological Evaluation ◽  
Chemotherapeutic Agents ◽  
Cytotoxic Agents ◽  
Stable Configuration ◽  
Antiangiogenic Agents ◽  
Antitumor Effects

The growing incidence of cancer, the toxic side-effects associated with conventional chemotherapeutic agents and the development of multidrug resistance (MDR) drive the search for novel and more effective drugs with multi-target activity and selectivity towards cancer cells. Stilbenes are a group of naturally occurring phenolic compounds of plant origin derived from the phenylpropanoid pathway that may exist as cis- or trans-isomers. Although the trans-isomer is the more common and stable configuration, resveratrol being a representative compound, cis-stilbenes are potent cytotoxic agents that bind to and inhibit tubulin polymerization, destabilizing microtubules. This review summarizes the chemistry and biological evaluation of cytotoxic stilbenes and their synthetic derivatives as promising antimitotic leads for cancer therapy, focusing on the most potent compounds, the combretastatins. Combretastatins isolated from the South African bushwillow Combretum caffrum are among the most potent antimitotic and vascular disrupting agents (VDAs) of natural origin. Preclinical studies have demonstrated their potent antitumor effects in a wide variety of tumors, both in vitro and in vivo, being currently under evaluation in phase 2 and phase 3 clinical trials for several types of solid tumors. Topics covered herein include synthetic medicinal chemistry, modes of action, structure-activity relationships (SAR), preclinical and clinical studies as VDAs in cancer therapy, either as single agents or in combination with cytotoxic anticancer drugs, antiangiogenic agents, or radiation therapy, and development of appropriate formulations based on nanocarriers (e.g., liposomes, nanoemulsions, polymeric, lipid and ceramic nanoparticles, carbon nanotubes) for improved bioavailability and targeted delivery of combretastatins to the tumor vasculature.

Polyethylene Glycol Conjugated Polymeric Nanocapsules for Targeted Delivery of Quercetin to Folate-Expressing Cancer Cells in Vitro and in Vivo

ACS Nano ◽  
2014 ◽  
Vol 8 (2) ◽  
pp. 1384-1401 ◽  
Author(s):  
Riham I. El-Gogary ◽  
Noelia Rubio ◽  
Julie Tzu-Wen Wang ◽  
Wafa’ T. Al-Jamal ◽  
Maxime Bourgognon ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Cancer Cells ◽  
Targeted Delivery ◽  
Polymeric Nanocapsules
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