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FORMULATION AND OPTIMIZATION OF PHYTOSOMES: PHYTOSOMAL -ENCAPSULATION FOR INCREASING ITS EFFICACY AND SAFETY

Abstract:
Advanced biochemical and pre-clinical studies have proved the potential of plant flavonoids and other hydrophilic natural compounds for the treatment of skin disorders, different types of carcinoma, anti-aging and many other areas of therapeutics and preventive medicine. The hydrophilic nature and unique chemical structure of these compounds pose major challenge because of their poor bioavailability through the skin or gut. The use of phytosomes is a novel formulation technology which helps to overcome these problems. The paper provides details of the formulation methodology for phytosomes and describes their chemical and biological properties. The characterization and evaluation technologies used for phytosomes offers insight into different techniques helpful in screening various parameters of phytosomes. The advantages of phytosomes over conventional and liposomal drug delivery systems are also discussed. The scientific usefulness of the technology is reviewed together with a list of important patented technologies involving phytosomes. Thus, in this paper, a complete overview of phytosome technology has been provided for the benefit of the researchers interested in this field.

Inroduction:
Phytosomes (Phospholipid-herbal extract complexes) can be considered novel entities. It is better absorbed, utilized, and as a result produce better achievements than conventional herbal extracts. It contains the active ingredients of the herb bounded to phospholipids(phosphatidylcholine). The phospholipid molecular structure includes a watersoluble head and two fat-soluble tails. Because of this dual solubility, the phospholipid acts as an effective emulsifier. By combining the emulsifying action of the phospholipids with the standardized botanical extracts, the phytosome form provides dramatically enhanced bioavailability for lipid soluble drugs explained by faster and improved absorption in the intestinal tract. In addition, not all botanical properties are as bioavailable as others, joining

them to phospholipids produces an effective medium for increased absorption of the active constituents of the herb. Different vegetal derivatives such as flavonoids, terpenes and saponins formed reversible complexes with the phospholipids. Also, they showed antiinflammatory and vasokinetic activities higher and longer lasting than those observed after administration of the same amount of the substances in free form. The longer lasting activity of the complexed substances compared with that of the same substances in free form, could be linked to the increase in lipophilicity achieved through the complexation with the phospholipid. The phytosome process has been applied to many popular herbal extracts of ginkgo biloba, grape seed, hawthorn, milk thistle, green tea, and ginseng root with increasing their biological effect. Since ancient times the therapeutic uses of traditional medicines and phytomedicines have proved very popular for health maintenance by various means. During the last century chemical and pharmacological studies have been performed on many plant extracts in order to investigate their chemical composition and confirm their therapeutic usefulness. Most of the bioactive constituents of phytomedicines are water-soluble molecules (e.g. phenolics, glycosides, and flavonoids). However, water-soluble phytoconstituents are limited in their effectiveness because they are poorly absorbed when taken orally or when applied topically. Many approaches have been developed to improve the oral bioavailability, such as inclusion of solubility and bioavailability enhancers, structural modification and entrapment with the lipophilic carriers. There are many factors which may contribute to the poor bioavailability. For example, many phytoconstituents have multiple rings and, therefore, cannot be absorbed from the intestine into the blood by simple diffusion. Also, some herbal phytomolecules are poorly miscible with oils and other lipids and often fail to pass through the small intestine because of its lipoidal nature. The effectiveness of any herbal product is dependent upon delivering an effective level of the active compounds. The phytosome technology developed by Indena meets this challenge by markedly enhancing the bioavailability of selected phytomedicines. The term "phyto" means plant while "some" means cell-like. The use of phytosomes is a new advanced modern dosage formulation technology to deliver herbal products and drugs by improved better absorption and, as a result, produce better results than those obtained by conventional herbal extracts [8, 9]. This phytosome technology is a breakthrough model for marked enhancement of bioavailability, significantly greater clinical benefit, assured delivery to the tissues, and without compromising nutrient safety. Certain of the water-soluble phyto-molecules (mainly flavonoids and other polyphenols) can be converted into lipid-friendly complexes, by reacting herbal drugs with phospholipids, which are called phytosomes. They are more bioavailable as compared with simple herbal extracts owing to their enhanced capacity to cross the lipid-rich biomembranes and, finally, reach the blood. They have improved pharmacokinetic and pharmacological parameters whichare advantageous in the treatment of acute diseases as well as in pharmaceutical and cosmetic compositions. The phytosome process has been applied successfully to many popular herbal extracts including Ginkgo biloba, grape seed, hawthorn, milk thistle (Silybum marianum), green tea

(Thea sinensis) and ginseng (Panax ginseng). The flavonoid and terpenoid components of these herbal extracts are able to directly bind to phosphatidylcholine.