Phytosomes: A Novel approach for improving the efficacy of Herbal Extracts
Vignan Institute of Pharmaceutical Technology, Duvvada, Visakhapatnam, India.
*Corresponding Author E-mail: smedapati@yahoo.com
ABSTRACT:
A phytosome is defined as a combination of a phospholipid and a natural active substance. One of the lipid- based vesicular delivery methods is the phytosome, which can be used to encapsulate drugs and nutraceuticals derived from plants polyphenolic chemicals. Phytosomes are said to boost the absorption of traditional herbal remedies topically and orally. Phytosomes aid in increasing the solubility and bioavailability of polyphenolic substances through the gastrointestinal tract. Phytosomes preparation is simple to make and can be scaled up for business use easily. This article elaborates the concept of phytosome with detailed information regarding its structure, properties, applications preparation, and evaluation methods.
KEYWORDS: Phytosomes, Phospholipids, Polyphenolic compounds, Herbal extracts, Vesicular-system.
INTRODUCTION:
Herbal medicine has a tremendous role in health care system in recent years and widely used in the treatment of various diseases to combat the side effects of allopathic medicine. Some bioactive principles have low bioavailability and gastrointestinal absorption, hence a unique drug delivery mechanism termed phytosomes which enhances bioactive principle uptake and bioavailability is playing a significant role.1 The term "phyto" refers to plants and "some" resembles a construction or a covering. It might be in the form or a product of a polyphenolic phytoconstituent, in a ratio of 1:1 or 1:2.2 This phyto-phospholipid combination has the appearance of a little cell, which has more favourable pharmacokinetic and pharmacodynamic profile than conventional forms.3
A phytosome is created by combining a natural active component and a phospholipid (usually lecithin). It is a lipid-based vesicular delivery method that can be used to encapsulate pharmaceuticals and other substances like polyphenolic chemicals asshown in figure 1, which are plant-derived nutraceuticals.
Interactions between active phyto constituents and phospholipids generate phytophospholipid complexes as shown in figure 2.4 Due to the presence of a surfactant i.e., the phospholipids, phytosome exhibit greater interactions with the cell surface and are shielded from water triggered degradation.
Figure 1: Phytosome
Figure 2: Difference between phytosomes vs liposomes
Materials:5
· Phospholipids: Phosphatidyl ethanolamine, soya phosphatidyl choline, egg phosphatidyl choline, dipalmityl phosphatidyl choline, phosphatidyl choline.
· Aprotic solvent: Dioxane, Acetone, Methylene chloride.
· Non-solvent: n-hexane
· Alcohol:Ethanol, Methanol.
|
S. No |
Plant Source |
Common Name |
Chemical Constituents |
Trade Name |
Applications |
|
1. |
Silibium marianum |
Cardus marianus, milk thistle, Marian thistle |
Silybin |
Silybin Phytosome |
Hepato-protective, Antioxidant |
|
2. |
Panax ginseng |
Korean ginseng |
Ginsenosides |
Ginseng phytosome |
Immunomodulator |
|
3. |
Terminalia Sericea |
Silver Terminalia |
Sericoside |
Sericoside Phytosome |
Skin improver, Anti-wrinkles |
|
4. |
Crataegus Species |
Hawthorn, Quickthorn, Mayflower or hawberry |
Flavonoids |
Hawthorn Phytosome |
Antihypertensive, Cardioprotective |
|
5. |
Gingko biloba |
Maidenhair tree |
Flavonoids |
Gingko select phytosome |
Anti-aging, Protects brain and vascul lining |
|
6. |
Olea europea |
Common Olive |
Polyphenols |
Olea select phytosome |
Anti hyperlipidimea, Antiinflammatory |
|
7. |
Thea sinensis |
Tea plant |
Epigallocatechin |
Green select phytosome |
Anti-Cancer, Antioxidant |
|
8. |
Echinacea angustifolia |
Blacksamson echinacea |
Echinacosides |
Echinacea Phytosome |
Immuno-modulatory, Nutraceuticals |
|
9. |
Centella phytosome |
Gotu kola |
Saponins or Triterpenoids |
Centella phytosome |
Brain tonic, Vein and Skin disorder |
|
10. |
Glycyrrhiza Glabra |
Licorice |
18-𝛽 Glycyrrhetinic acid |
Glycyrrhiza phytosome |
Anti-inflammatory, Soothing |
|
11. |
Vaccinium Myrtilus |
Myrtle blueberry, Myrtle whortleberry |
Polyphenols, Actinoside |
Mertoselect Phytosome |
Antioxidant |
|
12. |
Horse Chestnut bark |
Aesculus hippocastanum |
Proanthocyanidin A2 |
PA2 phytosome |
Anti-Wrinkles, UV Protectant |
|
13. |
Ruscus aculeatus |
Butcher’s broom,knee holly or piaranthus |
Steroid saponins |
Ruscogenin phytosome |
Anti-inflammatory, Improve skin circulation |
|
14. |
Curcurbita pepo seeds |
Pumpkin, Summer squash, Table queen squash |
Curbilene |
Curbilene phytosome |
Skin care, Matting agent |
|
15. |
Zanthoxylum Bungeanum |
Common prickly – ash |
Zanthalene |
Zanthalene Phytosome |
Soothing, Anti irritant, Anti itching |
1. Solvent evaporation8: The herbal extract and phospholipid are mixed in a suitable solvent or mixture of solvents, refluxed for a given duration, and then evaporated using a rota evaporator in this technique. The rota evaporator is used to evaporate the solvent that operates on the premise of lowering the boiling point of water by using vacuum. The solution is then rotated to enhance the heating surface area. The rota evaporator is a popular choice because of its speed and capacity to handle a big volume of solvents and appropriate approach for causing the development of complexes. However, when it comes to evaporating high temperature and high-boiling-point solvents such as DMSO and DMF, a high-pressure vacuum system is required to get the specified boiling point depression.
2. Co-Grinding9: External mechanical force is used to knead the medication and phospholipid together in order to produce a complex. When compared to co-grinding, solvent evaporation resulted in a significant degree of drug complexation.
3. Method of mechanical dispersion10: The phospholipid is dissolved in this approach with the help of a suitable solvent. After that, the samples were subjected to sonication for few minutes. Drop by drop, the medication solution is added to the aforesaid mixture.
4. Super critical fluid process:11 This procedure is carried out at a low temperature and pressure. Carbon dioxide is the most commonly utilized supercritical fluid because it has a critical pressure of 74 bar and a critical temperature of 31 degrees Celsius, allowing it to be employed at low temperatures of 40 to 60 degrees Celsius. However, size and distribution being both within control is one of the drawbacks in this process
5. Co-solvent lyophilization:12 The lyophilization process includes a freezing step, primary drying, and secondary drying, all of which use the sublimation principle. This procedure is carried out at a temperature and pressure that is less than triple point.
6. Precipitation of anti-solvents13: The phospholipid and the medication are placed in RBF and dissolved in a suitable solvent then the complex is generated after refluxing for a particular period of time. Anti-solvent is used to precipitate the substance. Anti-solvent precipitation is a technique that can be used at room temperature and pressure without the use of expensive equipment.
7. Solvent ether-injection process14: The interaction of lipids dissolved in an organic solvent with herbal extracts in an aqueous phase is used in this approach. Phospholipids dissolved in diethyl ether are slowly injected drop by drop into an aqueous solution of phytoconstituents. On subsequent solvent exposure, it results in the creation of cellular vesicles.
1. Transition temperature: The transition temperature of the vesicular lipid system can be determined by differential scanning calorimetry (DSC).15,16
2. Entrapment efficiency:17 The loaded phytosome's entrapment effectiveness can be assessed by diluting 1 part of the preparation in the cooling centrifuge machine after centrifuging at -4°C for 30 minutes with 10ml of solvent at 18000 RPM. The supernatant solution will be collected at this time and analysed using UV/V spectroscopy to assess the amount of free medication.The ultimate value of entrapment efficacy should be computed usingt the following equation:
Entrapment efficacy (%) = (total quantity of drug) - (quantity of free drug) × 100 ÷ (total quantity of drug).
Loaded phytoconstituent computed as a percentage of total using the formula:
% yield = Practical yield x 100 ÷ Theoretical yield
A phytosomal formulation's entrapment efficiency can also be measured using ultra-centrifugation technique.
3. Vesicle size and Zeta potential:18,19 Phytosome particle size and zeta potential can be measured by light scattering, which is determined using a computational system photon correlation spectroscopy.
4. Visualization determination:17 The methods for visualizing phytosomes include transition electron microscopy and scanning electron microscopy.
Scanning Electron Microscopy (SEM): This technique is used to characterise and determine the particle size distribution. Scanning electron microscopy (SEM) and surface morphology of formed complexes. The technique of microscopy is employed, the dry sample should be placed on the brass stub in this approach. In an ion sputter, an electron microscope is coated with gold.The phytosome complex can be photographed digitally Stub scanning at various magnifications of1000, 5000, and 3000X.
Transition electron microscopy: Other than scanning electron microscopy, transition electron microscopy can be utilized to characterise the size of phytosomal vesicle complexes at 1000 times magnification.
5. Measurement of surface tension activity: In an aqueous solution, the drug's surface tension activity, the Du Nouy ring tensiometer is widely accepted to give the accurate results. 19
6. Spectroscopic assessments: 20Interactions of phytoconstituents with phospholipids moiety are validated by the Spectroscopic tests.To assess the concentration of phytosomes, a suitable solvent is used to extract them, which give the amount of drug entrapped using UV-Visible Spectroscopy and high-performance liquid Chromatography.
Stability studies:21,22,23 In vitro and in-vivo evaluations will be based on the properties of medication.Their main phytoconstituents are separated by a phospholipid membrane, based on the animal model that has been chosen for its evaluation.
1. Hepatoprotective effects:24
The fruit of silibummarianum (family steraceae) contains flavonoids known for hepatoprotective effects is involved in the primordial study of the phytosomes.
2. Anti-oxidant properties:17, 25
Phytosomal formulations of Silybum marianum, quercetin, calendula officinalis phytoconstituents exhibit superior anti-oxidant activity compared to their conventional forms.
3. Cancer treatment:17
Herbal medicine containing phytoconstituents such as flavones, isoflavones, flavonoids, anthocyanins, coumarins, Lignin, catechins, and iso-catechins exhibit antioxidant action, contributing to its anti-cancer potential.
4. Transdermal application:17
Ruta graveolens, Panax ginseng M are examples of botanical medicines that can be utilized for conditions such as capillary fragility, hypertension, acne, UV-induced oxidative damage on the skin, liver,blood cholesterol, cataract, cardiovascular illness when they're made into phytosomes. This phytosomes formulation is safe to use on the skin and can be applied transdermally. They have been shown to have high penetration through epidermal barriers such as stratum corneum comparable to their free form.
5. Wound healing: 17
Sinigrin phytosome formulation achieved 100% wound healing and injuries, whereas the sinigrin (in its traditional form) only showed 71% Healing activity.
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Received on 23.05.2022 Modified on 31.12.2022
Accepted on 27.11.2023 © RJPT All right reserved
Research J. Pharm. and Tech 2023; 16(12):6028-6031.
DOI: 10.52711/0974-360X.2023.00978