Efficient TGF-β1 Delivery to Articular Chondrocytes In Vitro Using Agro-Based Liposomes

Abstract

The low efficiency in transfecting rat- and human-derived chondrocytes have been hampering developments in the field of cartilage biology. Transforming growth factor (TGF)-β1 has shown positive effects on chondrocytes, but its applications remain limited due to its short half-life, low stability and poor penetration into cartilage. Naturally derived liposomes have been shown to be promising delivery nanosystems due to their similarities with biological membranes. Here, we used agro-based rapeseed liposomes, which contains a high level of mono- and poly-unsaturated fatty acids, to efficiently deliver encapsulated TGF-β1 to rat chondrocytes. Results showed that TGF-β1 encapsulated in nano-sized rapeseed liposomes were safe for chondrocytes and did not induce any alterations of their phenotype. Furthermore, the controlled release of TGF-β1 from liposomes produced an improved response in chondrocytes, even at low doses. Altogether, these outcomes demonstrate that agro-based nanoliposomes are promising drug carriers.

Hop Extract Anti-Inflammatory Effect on Human Chondrocytes Is Potentiated When Encapsulated in Rapeseed Lecithin Nanoliposomes

“…To resolve this possible issue, we also vectorized the extract by using agro-based nanoliposomes from rapeseed lecithin. These systems have been previously employed to protect, carry, and release active molecules to chondrocytes [ 20 ]. Moreover, they are made of fatty acids ( -3), which are known for their anti-inflammatory properties [ 24 , 25 , 26 ].…”

“…Physicochemical characterization revealed no difference between empty and hop-extract-loaded nanoliposomes in terms of size, size distribution, and colloidal stability. As previously described, cell culture conditions with high rapeseed lecithin concentrations (500 and 1000 µg/mL) in empty nanoliposomes or nanoliposomes encapsulating hop extract affected human chondrocyte viability in vitro [ 19 , 20 ]. To assess the effect of empty or loaded nanoliposomes on inflammation, the culture conditions were selected to be harmless to chondrocytes and to include the highest quantities of compounds (250 µg/mL lecithin with or without 75 µg/mL hop extract).…”

“…Rapeseed lecithin obtained from agro-resources can be formulated to make nanoliposomes that are biocompatible systems for chondrocytes [ 19 ]. They have recently shown the promising potential to generate the sustained release and delivery of transforming growth factor (TGF)- 1, a growth factor able to maintain the chondrocyte articular phenotype in vitro [ 20 ]. Therefore, rapeseed lecithin nanoliposomes are delivery systems that can carry anti-inflammatory molecules to prevent joint inflammation [ 21 , 22 , 23 ].…”

Development of Nanomaterials to Target Articular Cartilage for Osteoarthritis Therapy

“…Thus, the mRNA could specifically upregulate the COL2A1 mRNA, modulating COL-II synthesis ( He K et al, 2021 ). In 2022, Velot É et al synthesized agro-based rapeseed liposomes carried transforming growth factor (TGF)-β1 (Lipo@TGF-β1) ( Velot et al, 2022 ). The liposomes encapsulated the TGF-β1, endowing it with biostability, a long half-life, and good penetration in cartilage.…”

Functionalized liposomes for targeted breast cancer drug delivery

“…Liposomes, first introduced in 1965, are rounded vesicles composed of either single or multiple lipid bilayers with an aqueous center [ [48] , [49] , [50] ]. These vesicles can spontaneously form when amphiphilic lipids, such as phospholipids, are dispersed in water and closely resemble our cellular membranes [ 51 , 52 ]. This similarity serves as an immense advantage for drug delivery in terms of biocompatibility and biodegradation.…”