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.
Highlights
The design and production of appropriate drug delivery systems, in particular, nanosized ones, offer an advanced approach to optimised bioavailability and/or the stability of drugs, to control drug delivery and to maintain drug stability during transport to the site of action
(4) Conclusions: NCs developed in this study could be suitable for both AN oral and parental administration, amplifying its therapeutic value
Phospholipids are the main amphiphilic components of the cell membrane and currently represent the main constituents of nanovectors because they can self-assembly in aqueous milieu, generating different supramolecular structures such as micelles and vesicles [1,3]. Their variation in head groups, aliphatic chains and alcohols leads to a wide variety of phospholipids, generally classified as glycerophospholipids and sphingomyelins
Summary
The design and production of appropriate drug delivery systems, in particular, nanosized ones, offer an advanced approach to optimised bioavailability and/or the stability of drugs, to control drug delivery and to maintain drug stability during transport to the site of action. Phospholipids are the main amphiphilic components of the cell membrane and currently represent the main constituents of nanovectors because they can self-assembly in aqueous milieu, generating different supramolecular structures such as micelles and vesicles [1,3]. Their variation in head groups, aliphatic chains and alcohols leads to a wide variety of phospholipids, generally classified as glycerophospholipids and sphingomyelins. The most common natural glycerophospholipids are phosphatidylcholine (PC), phosphatidylinositol, phosphatidylserine (PS), phosphatidylglycerol and phosphatidic acid, having diverse acyl moieties, principally myristoyl, palmitoyl, oleoyl and stearoyl.
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