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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...
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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.
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Fraisinib in a Shell: Liposomal Encapsulation of a GARS1 Inhibitor for Controlled Anticancer Delivery.

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Liposomes enhance Fraisinib

Keywords:
Fraisinibcalixpyrrolecancercontrolled releaseliposomes

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Area of Science:

  • Nanomedicine
  • Oncology
  • Drug Delivery

Background:

  • Fraisinib shows anticancer potential against glycyl-tRNA synthetase.
  • Fraisinib's hydrophobicity hinders clinical application due to poor solubility.
  • Liposomal encapsulation aims to improve Fraisinib's solubility and efficacy.

Purpose of the Study:

  • To develop and characterize Fraisinib-loaded liposomes for improved cancer therapy.
  • To optimize liposome formulation using different phospholipids for stability and drug release.

Main Methods:

  • Fraisinib was encapsulated into biodegradable liposomes.
  • Liposome formulations were characterized for physicochemical properties, encapsulation efficiency, and stability.
  • Drug release profiles were evaluated in vitro under different conditions.

Main Results:

  • 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) liposomes demonstrated enhanced stability and controlled drug release.
  • Optimal liposomes achieved ~90% encapsulation efficiency, 142 nm particle size, and -32 mV zeta potential.
  • Liposomal Fraisinib showed sustained release in buffer and accelerated release in serum, with delayed cytotoxicity in A549 cells.

Conclusions:

  • Liposomal Fraisinib formulation improves drug solubility and pharmacokinetic profiles.
  • This nanomedicine approach holds promise for enhanced cancer treatment.
  • Further clinical studies are warranted to validate therapeutic potential.