Intercalating pyrene with polypeptide as a novel self-assembly nano-carrier for colon cancer suppression in vitro and in vivo
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Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
Published on: September 20, 2017
Pei-Ying Lo1, Guang-Yu Lee1, Jia-Huei Zheng2
1Department of Science Education, National Taipei University of Education, No.134, Sec. 2, Heping E. Rd., Da-an District, Taipei City 106, Taiwan.
Abstract:
Giving patients right dosage is an essential concept of precision medicine. Most of nanocarriers lack of flexible drug capacity and structural stability to be customized for specific treatment, resulting in low therapeutic efficacy and unexpected side effects. Thus, a growing need emerges for fast and rigorous approaches to develop nanoparticles with properties of adjustable dosage and controllable particle size. Poly-l-Lysine is known for its enhanced bioadhesivity and pH-triggered structural swelling effect, which is utilized as the main agent to activate the multistage drug releasing. Inspired by natural bio-assembly system, we report a simple method to self-assemble Poly-l-Lysine-based nanoparticles via supramolecular recognitions of cross-linked pyrenes, which provides noncovalent force to flexibly encapsulate Doxorubincin and to construct robust nanostructures. Pyrene-modified polypeptide self-assemblies are able to adjust drug payload from 1: 10 to 2:1 (drug: polypeptide) without changing its uniform nano-spherical morphology. This nanostructure remained the as-made morphology even after experiencing the long-term (~ 10 weeks) storage at room temperature. Also, the nanoparticles displayed multi-step drug release behaviours and exhibited great in vitro and in vivo cytotoxicity towards colon cancer cells. The as-mentioned nanoparticles provide a novel perspective to compensate the clinical needs of specific drug feedings and scalable synthesis with advantages of simple-synthesis, size-adaptivity, and morphology reversibility.
Insights
Researchers developed novel Poly-l-Lysine nanoparticles for precision medicine. These adaptable nanocarriers offer adjustable drug loading and stable structure, improving therapeutic efficacy for colon cancer treatment.
Area of Science:
- Biomedical Engineering
- Materials Science
- Nanotechnology
Background:
- Precision medicine requires tailored drug dosages, but current nanocarriers lack flexible capacity and stability.
- Existing nanocarrier limitations lead to reduced therapeutic efficacy and adverse side effects.
- There is a need for rapid, robust methods to create nanoparticles with adjustable dosage and controlled size.
Purpose of the Study:
- To develop a simple, self-assembly method for creating Poly-l-Lysine-based nanoparticles.
- To engineer nanostructures with adjustable drug loading capacity and stable morphology.
- To evaluate the efficacy of these nanoparticles in colon cancer treatment.
Main Methods:
- Utilized Poly-l-Lysine's bioadhesivity and pH-triggered swelling.
- Employed supramolecular recognition of cross-linked pyrenes for self-assembly.
- Encapsulated Doxorubicin within pyrene-modified polypeptide nanostructures.
- Assessed drug payload flexibility, structural stability, and drug release kinetics.
- Evaluated in vitro and in vivo cytotoxicity against colon cancer cells.
Main Results:
- Achieved tunable drug payload from 1:10 to 2:1 (drug:polypeptide) without altering nano-spherical morphology.
- Demonstrated nanostructure stability over 10 weeks of room temperature storage.
- Observed multi-step drug release profiles.
- Exhibited significant in vitro and in vivo cytotoxicity towards colon cancer cells.
Conclusions:
- Developed a novel, simple method for synthesizing adaptable Poly-l-Lysine nanoparticles.
- These nanoparticles offer size-adaptivity, morphology reversibility, and adjustable drug feeding capabilities.
- The nanocarriers present a promising approach to address clinical needs in precision medicine and scalable synthesis for cancer therapy.

