siRNA LNCs – A novel platform of lipid nanocapsules for systemic siRNA administration

David, Stéphanie; Resnier, Pauline; Guillot, Alexis; Pitard, Bruno; Benoit, Jean‐Pierre; Passirani, Catherine

doi:10.1016/j.ejpb.2012.02.010

Cited by 29 publications

(31 citation statements)

References 9 publications

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“…The addition of the drug during the last cooling cycle has already been used to encapsulate siRNA, known to be sensitive to high temperatures. 29 After formulation, the recovery of the decitabine was over 95%, confirming the protection of decitabine from high temperatures during the formulation process. Decitabine-loaded THP-LNCs had a size of 33.6±1.6 nm and a drug payload of 44±16 µg/mL, which was too low for therapeutic efficacy.…”

mentioning

confidence: 69%

Development and in vitro evaluations of new decitabine nanocarriers for the treatment of acute myeloid leukemia

Briot

Roger

Lautram

et al. 2017

IJN

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mentioning

confidence: 69%

Development and in vitro evaluations of new decitabine nanocarriers for the treatment of acute myeloid leukemia

Briot

Roger

Lautram

et al. 2017

IJN

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“…In fact, as the proteins contained in the plasma are negatively charged, they can interact nonspecifically with cationic elements [3]. To illustrate the importance of the charge surface, neutral and anionic nanoparticles, such as mesoporous nanoparticles designed by Tanaka and coworkers, lipoprotein formulations proposed by Shahzad and coworkers, (both with a global charge around -3 mV) and LNCs (charge around +7 mV) were tested [163][164][165]. A siRNA LNCs for systemic administration was obtained presenting a 65% siRNA encapsulation efficiency [163].…”

Section: Biodistribution and Elimination Of Synthetic Vectorsmentioning

confidence: 99%

“…To illustrate the importance of the charge surface, neutral and anionic nanoparticles, such as mesoporous nanoparticles designed by Tanaka and coworkers, lipoprotein formulations proposed by Shahzad and coworkers, (both with a global charge around -3 mV) and LNCs (charge around +7 mV) were tested [163][164][165]. A siRNA LNCs for systemic administration was obtained presenting a 65% siRNA encapsulation efficiency [163]. Tumors were found to capture high density lipoprotein (HDL) molecules through the scavenger receptor type B1 (SR-B1), with HDL being necessary for cellular proliferation.…”

Section: Biodistribution and Elimination Of Synthetic Vectorsmentioning

confidence: 99%

Synthetic vectors for gene delivery: An overview of their evolution depending on routes of administration.

Belmadi

Midoux

Loyer

et al. 2015

Biotechnology Journal

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Nucleic acid delivery constitutes an emerging therapeutic strategy to cure various human pathologies. This therapy consists of introducing genetic material into the whole body or isolated cells to correct a cellular abnormality or disfunction. As with any drug, the main objective of nucleic acid delivery is to establish optimal balance between efficacy and tolerance. The methods of administration and the vectors used are selected depending on whether the goal of treatment is the production of an active protein; the replacement of a missing or inactive gene; or the combat of acquired diseases, such as cancer or AIDS. In that sense, synthetic vectors represent a valuable solution because they are well characterized, their structure can be fine tuned, and their potential toxicity can be reduced, since toxicity depends on the composition of the formulations. Here we review various synthetic vectors for gene delivery and address the question of their biodistribution as a function of the route of administration. We highlight the modifications to vectors structure and formulations necessary to overcome the major hurdles limiting the effectiveness of nucleic acid therapies.

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“…Therefore, PEG-NC prepared at pH 9 showed a controlled release profile, in contrast with the uncontrolled behavior of PEG-NC prepared at pH 7. Sustained release profiles have been also observed from some lipid nanocarriers upon deprotonation of doxorubicin [40] and etoposide [27].…”

Section: In Vitro Drug Releasementioning

confidence: 80%

PEGylated Lipid Nanocapsules with Improved Drug Encapsulation and Controlled Release Properties

Hervella¹,

Alonso-Sande²,

Lédo³

et al. 2014

CTMC

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Drugs with poor lipid and water solubility are some of the most challenging to formulate in nanocarriers, typically resulting in low encapsulation efficiencies and uncontrolled release profiles. PEGylated nanocapsules (PEG-NC) are known for their amenability to diverse modifications that allow the formation of domains with different physicochemical properties, an interesting feature to address a drug encapsulation problem. We explored this problem by encapsulating in PEG-NC the promising anticancer drug candidate F10320GD1, used herein as a model for compounds with such characteristics. The nanocarriers were prepared from Miglyol®, lecithin and PEG-sterate through a solvent displacement technique. The resulting system was a homogeneous suspension of particles with size around 200 nm. F10320GD1 encapsulation was found to be very poor (<15%) if PEG-NC were prepared using water as continuous phase; but we were able to improve this value to 85% by fixing the pH of the continuous phase to 9. Interestingly, this modification also improved the controlled release properties and the chemical stability of the formulation during storage. These differences in pharmaceutical properties together with physicochemical data suggest that the pH of the continuous phase used for PEG-NC preparation can modify drug allocation, from the external shell towards the inner lipid core of the nanocapsules. Finally, we tested the bioactivity of the drug-loaded PEG-NC in several tumor cell lines, and also in endothelial cells. The results indicated that drug encapsulation led to an improvement on drug cytotoxicity in tumor cells, but not in non-tumor endothelial cells. Altogether, the data confirms that PEG-NC show adequate delivery properties for F10320GD1, and underlines its possible utility as an anticancer therapy. Graphical Abstract:!

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siRNA LNCs – A novel platform of lipid nanocapsules for systemic siRNA administration

Cited by 29 publications

References 9 publications

Development and in vitro evaluations of new decitabine nanocarriers for the treatment of acute myeloid leukemia

Development and in vitro evaluations of new decitabine nanocarriers for the treatment of acute myeloid leukemia

Synthetic vectors for gene delivery: An overview of their evolution depending on routes of administration.

PEGylated Lipid Nanocapsules with Improved Drug Encapsulation and Controlled Release Properties

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