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Article

Stable, Monodisperse, and Highly Cell-Permeating Nanocochleates from Natural Soy Lecithin Liposomes

1
Department of Chemistry, University of Florence, Via U. Schiff 6, 50019 Sesto Fiorentino, Florence, Italy
2
Institute of Applied Physics “N. Carrara” (IFAC-CNR), Via Madonna del Piano 10, 50019 Sesto Fiorentino, Italy
*
Author to whom correspondence should be addressed.
Received: 13 November 2018 / Revised: 7 January 2019 / Accepted: 8 January 2019 / Published: 16 January 2019
(This article belongs to the Special Issue Smart Nanovesicles for Drug Targeting and Delivery)
(1) Background: Andrographolide (AN), the main diterpenoid constituent of Andrographis paniculata, has a wide spectrum of biological activities. The aim of this study was the development of nanocochleates (NCs) loaded with AN and based on phosphatidylserine (PS) or phosphatidylcholine (PC), cholesterol and calcium ions in order to overcome AN low water solubility, its instability under alkaline conditions and its rapid metabolism in the intestine. (2) Methods: The AN-loaded NCs (AN–NCs) were physically and chemically characterised. The in vitro gastrointestinal stability and biocompatibility of AN–NCs in J77A.1 macrophage and 3T3 fibroblasts cell lines were also investigated. Finally, the uptake of nanocarriers in macrophage cells was studied. (3) Results: AN–NCs obtained from PC nanoliposomes were suitable nanocarriers in terms of size and homogeneity. They had an extraordinary stability after lyophilisation without the use of lyoprotectants and after storage at room temperature. The encapsulation efficiency was 71%, while approximately 95% of AN was released in PBS after 24 h, with kinetics according to the Hixson–Crowell model. The in vitro gastrointestinal stability and safety of NCs, both in macrophages and 3T3 fibroblasts, were also assessed. Additionally, NCs had extraordinary uptake properties in macrophages. (4) Conclusions: NCs developed in this study could be suitable for both AN oral and parental administration, amplifying its therapeutic value. View Full-Text
Keywords: soy lecithin liposomes; nanocochleates; andrographolide; freeze-drying; gastrointestinal stability; uptake and safety soy lecithin liposomes; nanocochleates; andrographolide; freeze-drying; gastrointestinal stability; uptake and safety
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MDPI and ACS Style

Asprea, M.; Tatini, F.; Piazzini, V.; Rossi, F.; Bergonzi, M.C.; Bilia, A.R. Stable, Monodisperse, and Highly Cell-Permeating Nanocochleates from Natural Soy Lecithin Liposomes. Pharmaceutics 2019, 11, 34. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics11010034

AMA Style

Asprea M, Tatini F, Piazzini V, Rossi F, Bergonzi MC, Bilia AR. Stable, Monodisperse, and Highly Cell-Permeating Nanocochleates from Natural Soy Lecithin Liposomes. Pharmaceutics. 2019; 11(1):34. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics11010034

Chicago/Turabian Style

Asprea, Martina, Francesca Tatini, Vieri Piazzini, Francesca Rossi, Maria C. Bergonzi, and Anna R. Bilia 2019. "Stable, Monodisperse, and Highly Cell-Permeating Nanocochleates from Natural Soy Lecithin Liposomes" Pharmaceutics 11, no. 1: 34. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics11010034

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