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Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Modified-Release Drug Delivery Systems: Site-Targeted01:24

Modified-Release Drug Delivery Systems: Site-Targeted

Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
Micelles01:30

Micelles

Micelle formation is an intricate process that hinges on the properties of amphiphilic or amphipathic molecules and the conditions of the system in which they are found. Amphiphilic molecules, which have both hydrophilic (water-attracting) and hydrophobic (water-repelling) parts, play a critical role in this process.In aqueous environments, these molecules arrange themselves such that their hydrophilic heads are turned towards the water phase, while their hydrophobic tails are oriented away...
Site-Targeted Drug Delivery Systems: Polymeric Carriers01:24

Site-Targeted Drug Delivery Systems: Polymeric Carriers

Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
Lipid Absorption01:24

Lipid Absorption

Dietary triglycerides from chyme in the duodenum are mixed with bile salts produced by the liver to emulsify fats. As a result, large droplets are broken down into smaller ones, increasing the surface area for enzymatic action. Once emulsified, pancreatic lipases hydrolyze the triglycerides into free fatty acids and monoglycerides.
These breakdown products bind with bile salts and lecithin to form micelles, which quickly pass between microvilli to come in close contact with the apical...

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Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
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Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles

Published on: August 2, 2016

pH-responsive lipid core micelles for tumour targeting.

Elena Ravazzolo1, Stefano Salmaso, Francesca Mastrotto

  • 1Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Padova, Italy.

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V
|December 4, 2012
PubMed
Summary

A novel acid-sensitive nanocarrier, stearoyl-PEG-polySDM, was developed for targeted tumor drug delivery. This pH-responsive micelle system enhances paclitaxel

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Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?
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Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?

Published on: June 13, 2014

Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Drug Delivery Systems

Background:

  • Developing effective drug delivery systems for cancer therapy is crucial.
  • Tumor microenvironments often exhibit acidic pH, presenting an opportunity for targeted drug release.
  • Existing nanocarriers may lack sufficient pH sensitivity for optimal therapeutic outcomes.

Purpose of the Study:

  • To synthesize and characterize a novel acid-sensitive co-polymer, stearoyl-PEG-polySDM, for self-assembling micelles.
  • To evaluate the pH-responsive behavior, drug loading capacity, and biocompatibility of the developed nanocarrier.
  • To investigate the cellular uptake and in vitro cytotoxic efficacy of paclitaxel-loaded micelles at different pH values.

Main Methods:

  • Synthesis of stearoyl-PEG-polySDM via AGET-ATRP polymerization.
  • Characterization using potentiometric, turbidimetric, and chemical analyses.
  • Micelle formation, critical micelle concentration (CMC), and stability studies at varying pH.
  • In vitro cell culture studies with MCF-7 tumor cells, including biocompatibility, cellular association, and cytotoxicity assays.

Main Results:

  • Stearoyl-PEG-polySDM formed stable micelles (13.2±3.1 nm) with a CMC of 36 μM at pH 7.4.
  • The nanocarrier exhibited an apparent pKa of 7.2 and pH-dependent aggregation below pH 7.0.
  • Paclitaxel-loaded micelles demonstrated enhanced cellular uptake and significantly higher cytotoxicity at acidic pH (6.5) compared to neutral pH (7.4).

Conclusions:

  • Stearoyl-PEG-polySDM is a promising pH-sensitive nanocarrier for targeted tumor drug delivery.
  • The micelle system effectively encapsulates paclitaxel and releases it preferentially in the acidic tumor microenvironment.
  • This approach offers a strategy to improve the therapeutic index of anticancer drugs by enhancing tumor targeting and reducing systemic toxicity.