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Delivery of Therapeutic siRNA to the CNS Using Cationic and Anionic Liposomes
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Anti-angiogenic therapy via cationic liposome-mediated systemic siRNA delivery

Tatsuaki Tagami1, Takuya Suzuki, Mariko Matsunaga

  • 1Department of Pharmacokinetics and Biopharmaceutics, Subdivision of Biopharmaceutical Sciences, Institute of Health Biosciences, The University of Tokushima, 1-78-1, Sho-machi, Tokushima 770-8505, Japan.

International Journal of Pharmaceutics
|November 22, 2011
PubMed

Insights

Polyethylene glycol (PEG)-coated cationic liposomes effectively deliver small interfering RNA (siRNA) to tumor blood vessels. This targeted delivery enables anti-angiogenic cancer therapy, suppressing tumor growth with minimal side effects.

Area of Science:

  • Biotechnology
  • Nanomedicine
  • Cancer Therapy

Background:

  • Small interfering RNA (siRNA) holds therapeutic potential for genetic diseases, including cancers, but efficient in vivo delivery remains a challenge.
  • Cationic liposomes are promising nucleic acid carriers that can target angiogenic tumor vasculature, enabling anti-angiogenic strategies.
  • Systemic delivery of siRNA for cancer therapy requires effective carriers that can overcome biological barriers and target tumor sites.

Purpose of the Study:

  • To develop and optimize polyethylene glycol (PEG)-coated cationic liposome-siRNA complexes (siRNA-lipoplexes) for targeted delivery to angiogenic tumor blood vessels.
  • To evaluate the binding avidity of various siRNA-lipoplexes to tumor vasculature using a murine dorsal air sac (DAS) model.
  • To assess the therapeutic efficacy and safety of systemic siRNA-lipoplex injection in a murine cancer model.

Main Methods:

  • Preparation and characterization of multiple PEGylated siRNA-lipoplex formulations with varying lipid compositions and charge ratios.
  • Screening of siRNA-lipoplex avidity for newly formed blood vessels in a murine dorsal air sac (DAS) model.
  • Systemic administration of optimized siRNA-lipoplexes containing siRNA targeting Argonaute2 in mice with Lewis lung carcinoma.

Main Results:

  • A specific lipoplex composition (DC-6-14/POPC/CHOL/DOPE/mPEG(2000)-DSPE = 20/30/30/20/5 molar ratio) and a charge ratio of 3.81 demonstrated superior binding to angiogenic vessels.
  • Systemic injection of the optimized siRNA-lipoplex carrying apoptosis-inducible siRNA resulted in significant suppression of Lewis lung carcinoma tumor growth.
  • The treatment exhibited a favorable safety profile, with no severe side effects observed in the treated mice.

Conclusions:

  • PEGylated cationic liposomes are effective carriers for systemic siRNA delivery, targeting angiogenic tumor vasculature.
  • This targeted delivery facilitates anti-angiogenesis, leading to significant tumor growth suppression.
  • The developed siRNA-lipoplex system represents a promising strategy for developing novel cancer therapies with enhanced efficacy and safety.

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