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

Abstract

(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.

Glycerosome of Melissa officinalis L. Essential Oil for Effective Anti-HSV Type 1

“…The experiment was carried out with 1 mL of sample, magnetically stirred in 200 mL of PBS, used as release medium. The temperature was set at 37 • C; 0.5 mL of medium was collected at specified time points (30, 60, 120, 240, 360, 1440 min) and they were replaced by equal volumes of fresh medium, thus maintaining the sink conditions [31]. The collected release medium was analyzed by HPLC-DAD.…”

Development and Percutaneous Permeation Study of Escinosomes, Escin-Based Nanovesicles Loaded with Berberine Chloride

“…Nanovesicles were prepared using the thin layer evaporation method at specific conditions [21,22]. Different liposomes were developed by varying the lipid constituents and loading BRB.…”

Methoxy polyethylene glycol–cholesterol modified soy lecithin liposomes for poorlywater‐solubleanticancer drug delivery

“…Liposomes, artificially spherical vesicles prepared from naturally derived phospholipids, are widely known as the versatile biomedical materials of choice for the successful delivery of poorly water‐soluble anticancer drugs (PWSADs) 1–5 . Comprising at least one lipid bilayer enclosed aqueous core, liposomes have several advantages for delivery of PWSADs, such as enhancing drug solubility, serving as a sustained release system, reducing the toxic effect of drugs and providing protection against drug degradation 6–8 .…”

“…Among the choices available, soy lecithin (SL), a natural and unsaturated phospholipid obtained from soybean, is commonly used for liposomes preparations due to its specific advantages compared to saturated phospholipids derived from animal sources, including better stability with fewer polyunsaturated fatty acids, low risk of contaminating proteins and/or pathogens, abundant availability in both purified and nonpurified forms, and low production cost 9 . Thus, many studies have been performed assessing the efficacy of SL for preparing liposome‐based drug delivery systems 3,10–12 . However, similar to liposomes produced from other phospholipid sources, soy lecithin liposomes (SLPs) are quickly eliminated from the body, tending to leak the entrapped drugs through the lipid boundary and challenging the high loading of PWSADs due to the limited space within the lipid bilayers 13–15 .…”