Phospholipid Complex Technique for Superior Bioavailability of Phytoconstituents

Abstract

Phytoconstituents have been utilized as medicines for thousands of years, yet their application is limited owing to major hurdles like deficit lipid solubility, large molecular size and degradation in the gastric environment of gut. Recently, phospholipid-complex technique has unveiled in addressing these stumbling blocks either by enhancing the solubilizing capacity or its potentiating ability to pass through the biological membranes and it also protects the active herbal components from degradation. Hence, this phospholipid-complex-technique can enable researchers to deliver the phytoconstituents into systemic circulation by using certain conventional dosage forms like tablets and capsules. This review highlights the unique property of phospholipids in drug delivery, their role as adjuvant in health benefits, and their application in the herbal medicine systems to improve the bioavailability of active herbal components. Also we summarize the prerequisites for phytosomes preparation like the selection of type of phytoconstituents, solvents used, various methods employed in phytosomal preparation and its characterization. Further we discuss the key findings of recent research work conducted on phospholipid-based delivery systems which can enable new directions and advancements to the development of herbal dosage forms.

RETRACTED: Optimized Icariin Phytosomes Exhibit Enhanced Cytotoxicity and Apoptosis-Inducing Activities in Ovarian Cancer Cells

“…This type of interaction leaves the fatty acid chains free, so they can further move to encapsulate the polar portion of the complex forming a lipophilic surface [30]. Thus, phytosomes have the potential to enhance the oral bioavailability of plant-derived bioactives [31]. Phytosome use in transdermal drug delivery has also been reported [32].…”

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

“…The plant extracts or its monomers are firmly bound to phosphatidylcholine, a main constituent of phospholipids, resulting in a lipid compatible molecular complex. Phytosomes can significantly improve the pharmacokinetic and pharmacodynamic profiles of phytomedicines compared to the unmodified modalities [ 103 ]. Phytosomes are originally developed for handling the water-soluble phytomedicines with poor oral absorption due to their large molecular size and lack of lipophicity, but now not limited to water-soluble active compounds.…”

“…The in vivo studies showed that the liposomal formulation demonstrated a significant analgesic activity in mice. In recent years, phytosomes (phospholipid complexes) are also being widely used for oral drug delivery [ 103 ]. For example, Freag et al developed self-assembled phytosomal nanocarriers for improving the solubility and oral bioavailability of celastrol [ 151 ], and Telange et al developed apigenin-loaded phytosomes to improve the drug’s aqueous solubility, dissolution, in vivo bioavailability, and antioxidant activity [ 106 ].…”

Vesicle properties and health benefits of milk phospholipids: a review

“…As illustrated in Table 4, phytosome carrier can also deliver bioactive compounds, both lipophilic and hydrophilic, in order to enhance oral bioavailability (Lu et al, 2018). Phytosomes are a durable complexes, with a simple manufacturing process (Gnananath et al, 2017). Complexing reaction of milk phospholipids and encapsulate (molecular ratio 1-5) was realized in either ethanolic or methanolic solution of 55°C.…”