Lipopolyplexes: A Next Generation Lipid and Polymer Based
Gene Delivery Systems
Dhiraj Bhavsar*
Department of Botany, Shri Anand College, Ahmednagar, Maharashtra, India
*
For Correspondence: Dr. Dhiraj Bhavsar, Department of Botany, Shri Anand College, Ahmednagar, Maharashtra,
India, Tel: 86059 53537; E-mail: bhavsardv@gmail.com
Received date: 23/01/2018; Accepted date: 26/01/2018; Published date: 02/02/2018
Copyright: © 2018 Bhavsar D. This is an open-access article distributed under the terms of the Creative Commons
Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original
author and source are credited.
Editorial
Nucleic acids and Oligonucleotides like DNA, siRNA, miRNA and miRNA inhibitors have overriding attention as payloads
of gene delivery systems for cancer treatment. The advancement of nanotechnology in last few decades has rapidly
transformed the chemistry and functionality of the gene delivery nanocarriers. Lipoplexes (Lipid based delivery vehicles)
[1]
and Polyplexes (Cationic polymer based delivery vehicles)
[2,3]
are widely explored for their surface modification,
complexation efficiency, endosomal escape and release of nucleic acids from carriers in the cytoplasm, the ideal
characteristics of a gene delivery nanocarrier. Despite these advantages, Lipoplexes and polyplexes succumb to
cytotoxicity, immunogenicity and premature dissociation of nucleic acid material
[4-6]
. Hence, these delivery vehicles
aren’t fruitful in clinical trials. Cytotoxicity is a foremost limitation impeding the therapeutic use of gene knockdown and
gene delivery vehicles. Apart from immunogenicity and cytotoxicity, low cellular uptake and rapid degradation are
additional important factors manipulating therapeutic use of gene delivery vehicles. However, recent research showed
that the gene delivery nanocarriers with neutral or negatively charged Lipoplexes have squashed issues likes cytotoxicity
and immunogenicity generated by cationic carriers. Investigation also yielded encouraging out comes in in vitro and in
vivo than cationic lipids as being used currently
[7]
. However, negatively charge lipids lack the positive charge, which is
essential to promote interaction with nucleic acids for efficiently encapsulating. This understanding leads to the
possibility of development of new type of gene nanocarrier blend called Lipopolyplexes with the combined affirmative
characteristics of Lipoplexes and polyplexes. The combination of a cationic polymer and negative or neutral lipid with
genetic material is principally a fascinating concept of developing these possibly next generation gene nanocarriers.
Lipopolyplexes showed improved encapsulation efficiency by condensation of the nucleic acid payload by cationic
polymers. This also showed enhanced colloidal stability and also lowers the cytotoxicity and immunogenicity compared to
cationic Lipoplexes and polyplexes. In addition, they can be stored at room temperature or can be nebulized without
altering their physicochemical integrity and biological activity thus appear suitable for gene therapy
[8]
. The effectiveness
of Lipopolyplex mediated gene delivery system mainly depends on the lipid and polymer chemical structure, lipid/Nucleic
acid and Polymer/nucleic acid molar ratios. Lipoplexes formulated using cationic lipids such as DOTAP, DPPC-DSPE,
DPPC: DPPG, DOPE: Cholesteryl Hemisuccinate: Folate-Polyethlene Glycol-DOPE, DOCSPER, DOSPER, DOTMA
[9-14]
, have
shown improved transfection efficiency in cancer cell lines. The relationship between cationic polymers (PEI, chitosan,
PAA and PLL, etc.)
[15-18]
and lipids can be selected rationally to make an effective gene delivery. The polyplex part of the
Lipopolyplexes improves the intracellular trafficking of nucleic acid material while the lipids encourage cellular uptake of
the lipopolyplexes
[19,20]
. Lipopolyplexes formulated with negatively charged lipid in different combinations such as DPPC:
DSPE-PEG, DOPE: DPPC: Cholesterol, have been playing an imperative role in gene therapy and offer preclinical proof of
concept. Lipopolyplex a novel technology is going to be explored widely for cancer treatment in the coming days. The
Lipopolyplexes will support the cause of gene therapy, resulting in advances in the medical industry and, more vitally, to
the patients.
REFERENCES
1. Zylberberg C, et al. Engineering liposomal nanoparticles for targeted gene therapy. Gene Ther. 2017;24:441-452.
2. Molinaro R, et al. Polyethylenimine and chitosan carriers for the delivery of RNA interference effector. Exp Opin Drug
Deliv. 2013;10:1653-1668.
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Research & Reviews: Drug Delivery
Res Rev Drug Deliv | Volume 2 | Issue 1 | June, 2018
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