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

(1) Background: Andrographolide (AN), the main diterpenoid constituent of , 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...

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Bibliographic Details
Published in:Pharmaceutics 2019-01, Vol.11 (1), p.34
Main Authors: Asprea, Martina, Tatini, Francesca, Piazzini, Vieri, Rossi, Francesca, Bergonzi, Maria Camilla, Bilia, Anna Rita
Format: Article
Language:English
Subjects:
andrographolide
Bioavailability
Drug delivery systems
Fibroblasts
freeze-drying
gastrointestinal stability
nanocochleates
Oral administration
soy lecithin liposomes
uptake and safety
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Summary:(1) Background: Andrographolide (AN), the main diterpenoid constituent of , 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.
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics11010034