The imbalance of hydrophilicity and lipophilicity along with a large molecular size (due to a unique chemical structure) of natural compounds or plant actives poses a significant challenge for their absorption through a biological membrane and thus, alters the therapeutic efficacy. Therefore, it is desirable to have a novel approach for such formulation in order to improve the solubility and bioavailability of these phytoconstituents as a phospholipid complexation. Herbal drugs are precisely, embedded and bound by phospholipids to form vesicular structures which are amphoteric in nature. Thus, the phytolipid complex technology is unique, in the respect that it has a higher stability profile owing to its amphoteric nature or owing to its solubility in aqueous as well as oil media. It also exhibits a greater absorption and bioavailability, as the drug molecules are embedded in the pockets of the phytosomal assembly, therefore, with more drug loading capability, protection from the gastric environment, and subsequently inactivation in gastro-intestinal tract (GIT). Phytolipid complexes have a great potential in the field of medicine, pharmaceuticals and cosmetics due to improved pharmacokinetics and pharmacological attributes. The present review explores the various aspects of phytolipid complexes concerning the phospholipids, vesicles, choice of ingredients, phytolipid complexation, advantages, preparation methods and their applications.
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http://dx.doi.org/10.2174/1567201815666180209114103 | DOI Listing |
Int J Mol Sci
March 2019
Program Against Cancer Therapeutic Resistance (ProCURE), Metabolism and Cancer Group, Catalan Institute of Oncology, 17007 Girona, Spain.
An ever-growing number of preclinical studies have investigated the tumoricidal activity of the milk thistle flavonolignan silibinin. The clinical value of silibinin as a bona fide anti-cancer therapy, however, remains uncertain with respect to its bioavailability and blood⁻brain barrier (BBB) permeability. To shed some light on the absorption and bioavailability of silibinin, we utilized the Caco-2 cell monolayer model of human intestinal absorption to evaluate the permeation properties of three different formulations of silibinin: silibinin-meglumine, a water-soluble form of silibinin complexed with the amino-sugar meglumine; silibinin-phosphatidylcholine, the phytolipid delivery system Siliphos; and Eurosil/Euromed, a milk thistle extract that is the active component of the nutraceutical Legasil with enhanced bioavailability.
View Article and Find Full Text PDFCurr Drug Deliv
December 2018
Jawaharlal Nehru Technical University, (JNTU) Hyderabad, Telangana, 500 085, India.
The imbalance of hydrophilicity and lipophilicity along with a large molecular size (due to a unique chemical structure) of natural compounds or plant actives poses a significant challenge for their absorption through a biological membrane and thus, alters the therapeutic efficacy. Therefore, it is desirable to have a novel approach for such formulation in order to improve the solubility and bioavailability of these phytoconstituents as a phospholipid complexation. Herbal drugs are precisely, embedded and bound by phospholipids to form vesicular structures which are amphoteric in nature.
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