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Site-Targeted Drug Delivery Systems: Polymeric Carriers01:24

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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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Modified-release dosage forms are designed to address the limitations of drugs with short biological half-lives. These forms maintain stable therapeutic drug concentrations over extended periods, reducing the need for frequent dosing. A consistent drug level helps minimize peak-trough fluctuations, which can reduce adverse effects, lower the risk of drug resistance, and improve overall treatment effectiveness.One common type of modified-release form is the extended-release (ER) formulation. ER...
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A Tripeptide-Stabilized Nanoemulsion of Oleic Acid
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Layer-by-layer assembled polypeptide capsules for platinum-based pro-drug delivery.

Dongfang Zhou1, Haihua Xiao, Fanbo Meng

  • 1State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Graduate School of Chinese Academy of Sciences, Renmin Str. 5625, Changchun 130022, PR China.

Bioconjugate Chemistry
|November 27, 2012
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Summary

Biodegradable microcapsules loaded with platinum(IV) pro-drug were developed. These capsules show enhanced platinum release and higher anticancer efficacy against colon cancer cells compared to cisplatin.

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Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Cancer Therapeutics

Background:

  • Platinum-based drugs like cisplatin are widely used in cancer chemotherapy.
  • Developing effective drug delivery systems is crucial to improve platinum drug efficacy and reduce side effects.
  • Platinum(IV) pro-drugs offer potential advantages over platinum(II) drugs due to their stability and reduced toxicity.

Purpose of the Study:

  • To synthesize and characterize biodegradable poly(glutamic acid)/poly(l-lysine)-platinum(IV) multilayer microcapsules.
  • To investigate the platinum release kinetics from the microcapsules under different conditions.
  • To evaluate the in vitro anticancer efficacy of the microcapsules against colon cancer cells.

Main Methods:

  • Layer-by-layer (LbL) assembly of poly(glutamic acid) (PGA) and poly(l-lysine) conjugated with platinum(IV) (PLL-Pt(IV)) on colloidal silica templates.
  • Template removal to obtain hollow multilayer microcapsules.
  • In vitro drug release studies under acidic and reductive conditions.
  • Cytotoxicity assays using CT-26 colon cancer cells.
  • Confocal laser scanning microscopy (CLSM) for cellular uptake studies.

Main Results:

  • Biodegradable PGA/PLL-Pt(IV) multilayer microcapsules (0.5 μm diameter) were successfully fabricated.
  • Platinum release rate and amount increased under acidic and/or reductive conditions.
  • Microcapsules exhibited significantly higher cytotoxicity against CT-26 cells (IC50Pt = 3.5 μg/mL) compared to free cisplatin (IC50Pt = 8.6 μg/mL).
  • Enhanced cytotoxicity was linked to effective cellular internalization of the microcapsules.

Conclusions:

  • PGA/PLL-Pt(IV) multilayer microcapsules represent a promising platform for platinum-based anticancer drug delivery.
  • The controlled release and enhanced cellular uptake contribute to improved therapeutic efficacy.
  • This approach offers a potential strategy for developing more effective colon cancer treatments.