PHYTOSOME

Objective: This study aims to develop and evaluate the phytosome of Phyllanthus emblica L. fruit extract. Methods: The formation of phytosome was performed by using three methods, namely solvent evaporation, antisolvent, and thin layer formation method. The phytosome was evaluated for its entrapment efficiency, particle size, polydispersity index, Fourier Transform Infra-Red (FTIR), and Transmission Electron Microscope (TEM) methods. The phytosome was made into cream with a concentration of 1%. The cream stability was evaluated at a room temperature of 40 °C for 28 d. The permeation of the total phenolic content of cream-containing phytosome and cream-containing extract without phytosome technology was evaluated by diffusion studies. Results: The best method to prepare phytosome was an antisolvent method with the efficiency of entrapment, particle size, and polydispersity index equal to 66.99±0.01%, 298.53 nm±12.04, and 0.323±0.01 respectively. Evaluation by using TEM and FTIR spect...

The usage of phytochemical supplements over past two decades has steadily increased worldwide. Popularity of these products has been especially notable among people in western countries, where almost 20% of consumers report regular usage of such supplements. Supramolecular interventions are being viewed with tremendous research inputs. Supramolecular chemistry refers to the area of chemistry beyond the molecules and focuses on the chemical systems made up of discrete number of assembled molecular subunits or components. The forces responsible for the spatial organization may vary and include mainly (intermolecular forces, electrostatic or hydrogen bonding). While traditional chemistry focuses on the covalent bond, supramolecular chemistry examines the weaker and reversible non-covalent interactions between molecules. In spite of the popularity of these phytochemical supplements, the actual efficacy has remained elusive for many of these supplements due to poor bioavailability. To improve the efficacy of these agents, researchers and manufacturers have been adopting novel drug formulation technologies to enhance phytochemical bioavailability. Cyclodextrins, cyclic oligosaccharides obtained from the degradation of starch, can be viable as an encapsulant for the plant bioactive compounds. Solubility and oral bioavailability of rutin (Flavanoid glycoside) was improved by complexation with HP-β-CD (2-hydroxypropyl-β-cyclodextrin). Phytosome ® has been reported as an improved delivery system for oral bioavailability of polyphenolics through enhancement of rate and extent of solubility into aqueous intestinal fluids and capacity to cross bio membranes. Liposomes are extremely versatile supramolecules being developed and used as efficient carriers for drug delivery. Thus, improved phytochemical delivery through supramolecule chemistry may open up a new phase of operations in the "drug war" between humans and plants.

Sinigrin is a major glucosinolate present in plants of the Brassicaceae family. Recently, sinigrin and its phytosome formulations have been investigated for its wound-healing actions, by our research group. The aim of this study was to demonstrate sinigrin drug release from its phytosome complex and also to determine whether the phytosome complex enhances the delivery of sinigrin into the skin when compared to free sinigrin. In vitro Franz cell diffusion studies were performed on human abdominal skin. The morphology of the phytosome complex was examined by transmission electron microscopy. The in vitro drug release was determined using dialysis sacks. The in vitro drug release indicated a controlled and sustained release of sinigrin from the phytosome complex. Tape stripping results showed that the sinigrin-phytosome complex (0.5155 μg/ml) statistically significantly enhanced the delivery of sinigrin into the stratum corneum-epidermis when compared to the free sinigrin (0.0730 μg/ml...

The aim of the present study was performed, Extraction of plant material using hydroalcoholic extract, Phytochemical analysis of Swertia perennis L and Formulation, development and evaluation of phytosomes. The phytochemical screening of this investigation attested the presence of several secondary metabolites with known biological antioxidant activities. Hydroalcoholic extract of aerial parts of Swertia perennis was possessing antioxidant activity due to the presence of flavonoids constituent. Flavonoids content was expressed as milligrams equivalent of Quercetin per 100 milligrams of dry extract (mg QE/100mg). Total flavonoid contents are shown in Table 7.4. From these results, Hydro-alcoholic extract showed flavonoid compounds (1.021 mg QE/100mg). Different formulation of Phytosomes were prepared using different amount of phospholipids: cholesterol and extract and were evaluated for Drug Excipient compatibility study, Entrapment efficiency and particle size analysis, In vitro dru...

In the arena of solubility enhancement, several problems are encountered. A novel approach based on lipid drug delivery system has evolved, pharmacosomes. Pharmacosomes are colloidal, nanometric size micelles, vesicles or may be in the form of hexagonal assembly of colloidal drug dispersions attached covalently to the phospholipid. They act as befitting carrier for delivery of drugs quite precisely owing to their unique properties like small size, amphiphilicity, active drug loading, high entrapment efficiency, and stability. They help in controlled release of drug at the site of action as well as in reduction in cost of therapy, drug leakage and toxicity, increased bioavailability of poorly soluble drugs, and restorative effects. There has been advancement in the scope of this delivery system for a number of drugs used for inflammation, heart diseases, cancer, and protein delivery along with a large number of herbal drugs. Hence, pharmacosomes open new challenges and opportunities ...

Cell death (apoptosis) in the hippocampus is related to impaired memory functions. Gotu kola (Centella asiatica) contains asiatic acid and asiaticoside, which act as antioxidants and improve memory function. This study was intended to determine the effects of gotu kola extracts on Bcl-2 gene expression and spatial memory in rats with impaired memory functions due to trimethyltin (TMT) injection. The rats were subdivided into six groups, each group consisting of 10. The normal group was given sodium carboxymethyl cellulose (CMC-Na); the TMT group was given CMC-Na; the positive group was given 200 mg/kg bw citicoline; the extract groups were given a variation of gotu kola extract at 100 (P100), 200 (P200), and 400 mg/kg bw (P400) doses, respectively. These treatments were conducted for 35 days. TMT was injected intraperitoneally on Day 8 of treatment at a dose of 8 mg/kg bw in all groups except the normal group. On Days 29-35, the Morris water maze (MWM) spatial memory test was conduc...

Objective: This study aims to develop and evaluate the phytosome of Phyllanthus emblica L. fruit extract. Methods: The formation of phytosome was performed by using three methods, namely solvent evaporation, antisolvent, and thin layer formation method. The phytosome was evaluated for its entrapment efficiency, particle size, polydispersity index, Fourier Transform Infra-Red (FTIR), and Transmission Electron Microscope (TEM) methods. The phytosome was made into cream with a concentration of 1%. The cream stability was evaluated at a room temperature of 40 °C for 28 d. The permeation of the total phenolic content of cream-containing phytosome and creamcontaining extract without phytosome technology was evaluated by diffusion studies. Results: The best method to prepare phytosome was an antisolvent method with the efficiency of entrapment, particle size, and polydispersity index equal to 66.99±0.01%, 298.53 nm±12.04, and 0.323±0.01 respectively. Evaluation by using TEM and FTIR spectroscopy also confirmed the formation of spherical phytosome. There were no significant changes in the cream's organoleptic, pH, and viscosity during storage at room temperature. The permeation test through skin snake and Spangler's membrane showed that cream containing phytosome had a better diffusion percentage than cream containing extract without phytosome technology. Conclusion: The results of this study showed that the antisolvent method was a potential method to develop phytosome of Phyllanthus emblica L. fruit extract and cream containing phytosome was effective in increasing the permeation.

Phytosomes are novel form of herbal formulations which contains the bioactive phytoconstituent(s) of herb extract complexed with phospholipid to produce lipid compatible molecular complexes. Since phytoconstituents are obtained from natural resources, fewer side effects and lower phytochemical costs are added advantages for their utilization in treatment of various diseases. Unfortunately, despite the wide therapeutic potentials of poly phenolic phytoconstituents such as flavonoids, glycosides, terpenoids etc. still they suffer with poor aqueous solubility, absorption and bioavailability problems when administered orally or by topical applications. The effectiveness of any herbal product is dependent upon delivering an effective level of active compounds. The phytosome technology meets this challenge by markedly enhancing the solubility, absorption and bioavailability of the phytomedicines for better drug delivery and clinical action. It exhibit better pharmacokinetic and pharmacody...

Traditional medicine which rely on plant resources to treat various diseases and ailment remains an important (in some case, the only) form of treatment in many developing countries and its use is increasing worldwide. 1 According to the world Health Organization (WHO), 75% of world population still rely on plant based traditional medicines for their primary healthcare of which 85% is based on the use of plant extracts. 2 Similarly, it is estimated that 39% of 520 new approved drugs (between 1983 and 1994), 5080% of antibacterial and anticancer drugs were derived from natural product. 3 The increased interest in the use of natural products is for a number of reasons, the perception that such products are safe, ecofriendly, low cost, readily available and of little or no side effects. The use of natural products has led in many drug discoveries as they provided chemical building blocks used in their synthesis or used as new drugs in their unmodified state. 4

Objective: Allicin, a natural organosulfur compound, is the main garlic ingredient, which has extensive pharmacological activities. Its unstable under acidic conditions due to alliinase's inactivation causes the need for preparations that delayed-release in the stomach to maximize allicin absorption. This study aimed to prepare and characterize the enteric-coated microsphere of phytosome loading allicin-rich extract to protect it from gastric acid. Methods: The allicin-rich extract phytosome (ArE-Ps) was prepared and evaluated for characteristics. Microsphere was made in three formulas with different molar ratios of ArE-Ps and Eudragit L30D-55 (1:1; 1:1.5 and 1:2) by spray dry. The three microspheres compared to particle size, entrapment efficiency, and dissolution test in acid and 7.4 pH medium. Results: Optimized ArE-Ps has a size of 251.6 nm, polydispersity index 0.466, zeta potential 34.11, entrapment efficiency of 62.62 %, and specific gravity of 1,005 g/ml. The surface topography of the three formulas shows an almost spherical shape with concave surfaces. The particle size of the microsphere ranges from 215±6.27 nm to 548.8±10.15 nm. Entrapment efficiency increases with an increasing number of polymers with a maximum value of 65.44 % at F3. The results dissolution test in vitro showed no drug release in acidic medium, and drug release occurred at a 7.4 pH medium. Drug release of three microsphere formulations followed the Korsmeyer-Peppas model with a k value of 12.7088±0.1769; 17.9322±1.5621; and 12.958±1.2677; respectively. Conclusion: Based on these results, the polymer's increase in three microsphere formulations can affect characteristics and retain drug release under acidic conditions.

Phytosomes are referred to as novel compounds containing lipophiliccomplexes of components of different plants which are composed of glycerophospholipids. In the novel drug delivery system, it is a need of the hour to search for such a novel delivery system that can provide more bioavailability and efficacy for any extract containing phytoconstituents or Phyto extracts. The present study data were collected from extensive literature surveys from different esteemed scientific repositories such as Pubmed, Science direct, Research gate, Cochrane, Google scholar, Willey, Core, 1Library, etc. Many phytoconstituents that are obtained from nature have high biological activities in many chronic diseases and has the best therapeutic efficacy. The main advantage of using phytoconstituents is that it does not have most adverse side effects. Phytosome is used for phytopharmaceutical formulations, herbal formulations, and in Ayurveda. It improves the bioavailability of medicaments and absorption...

The word ”Phyto” means plant, and also sometimes, it can be signified as cell- like. The development of phytosomes produces a little cell by itself, by which the active ingredient of the herbal extracts is protected from the intestinal secretions and instinctive bacteria destruction. The introduction of phyto- somes into herbal formulation is very recent and useful because they have advanced bioavailability, and they are better absorbed. Also, they consume this enhanced ability to cross lipid-rich bio membranes to finally reach the blood. Phytosomes can also be defined as complex chemical mixtures which are formulated by countering more than one mole synthetic or natural phos- pholipids phosphatidyl ethanolamine or phosphatidylserines with the one mole of another component. There are various plants materials which can be merged in the process of phytosomes, such as several herbal extracts includ- ing quercetin, grape seed, Rhein, neem, green tea, aloe vera, marigold and ginseng. The...

Phytosomes, are the tiny structures which serves as intermediate between the conventional and novel drug delivery system. These are the cells, which are able to carry themselves from a hydrophilic to the lipid environment of the cell membrane, which ultimately reaches the blood. The hydrophilic plant constituents, which find their application in skin disorders, anti-ageing possess and different type of carcinomas are difficult in processing into conventional delivery system and hence transformed into phytosomes. Phytosomes are the complexes prepared by mixing polyphenolic phytoconstituents and phosphatidylcholine in molar ratio. Phytosomes are superior to the conventional drug delivery systems in terms of pharmacokinetic and pharmacodynamic properties. Phytosomal delivery of the extracts of Ginkgo biloba, Grape seed, Green tea, Ginseng, etc. has been profitably used. Phytosomes have been refined for therapeutic uses like cardiovascular, anti-inflammatory, immunomodulator, anticancer...

Liposomes are lipid based vesicular systems that offer novel platform for versatile drug delivery to target cell. Liposomes were first reported by Bangham and his co-workers in 1964 (1). Since then, liposomes have undergone extensive research with the prime aim to optimize encapsulation, stability, circulation time and target specific drug delivery. Manipulation of a liposome’s lipid bilayer and surface decoration with selective ligands has transformed conventional liposomes into adaptable and multifunctional liposomes. Development of liposomes with target specificity provide the prospect of safe and effective therapy for challenging clinical applications. Bioresponsive liposomes offer the opportunity to release payload in response to tissue specific microenvironment. Incorporation of novel natural and synthetic materials has extended their application from stable formulations to controlled release targeted drug delivery systems. Integration and optimization of multiple features int...

Liposomes are lipid based vesicular systems that offer novel platform for versatile drug delivery to target cell. Liposomes were first reported by Bangham and his co-workers in 1964 (1). Since then, liposomes have undergone extensive research with the prime aim to optimize encapsulation, stability, circulation time and target specific drug delivery. Manipulation of a liposome’s lipid bilayer and surface decoration with selective ligands has transformed conventional liposomes into adaptable and multifunctional liposomes. Development of liposomes with target specificity provide the prospect of safe and effective therapy for challenging clinical applications. Bioresponsive liposomes offer the opportunity to release payload in response to tissue specific microenvironment. Incorporation of novel natural and synthetic materials has extended their application from stable formulations to controlled release targeted drug delivery systems. Integration and optimization of multiple features int...

Propolis and lycopene compounds with potent pharmacological activities as anticancer, anti-inflammatory and antioxidant action. Propolis is a unique product produced by honeybees. Lycopene is phytochemical pigment belong to the group of carotenoids and found in different fruits and vegetative, as well as certain algae and fungi. This study was conducted to prepare and characterize phytosomal propolis and lycopene, then evaluate their in vitro anti-proliferative potential on rats prostatic hyperplasia cell line. Size of the nanoparticles determined by scanning electron microscope were 102.1±5.83 nm for phytosome propolis and 110.4±5.77 nm for phytosome lycopene. The encapsulation and loading efficiencies of phytosome formulations were 80.83 ± 4.41% and 64.66 ± 3.52% respectively for phytosome propolis and 75.82 ± 5.46% and 60.66 ± 4.37% respectively for phytosome lycopene. In order to ascertain the anti-proliferative activity of the phytosomal formulations, MTT assay was carried out ...

Objective: Present work is aimed at preparation and characterization of phytosomes, one of the, novel drug delivery dosage form used for improving bioavailability of drug, formed from ethanolic, aqueous, dichloromethane and ethyl acetate extract of Citrullus colocynthis fruit. Method: Required phytosomal formulations were developed in the form of different extracts of Citrullus colocynthis fruit from the lecithin and cholesterol, Then characterization involved various parameters, such as: Particle size determination, apparent solubility, entrapment efficiency (EE%), scanning electron microscope (SEM), xrd, FTIR spectroscopy and dissolution study. Result and Conclusion: Particle size varied from 250nm to 0.1μm of different formulations. The mean particle size of phytosome of aqueous extract of CC was scattered in a narrow range of 254±20.0 nm, and polydispersity index was 0.857±0.055, where phytosome of aqueous extract shows better entrapment then other phytosomal formulation. Photom...

Phytosomes, are the tiny structures which serves as intermediate between the conventional and novel drug delivery system. These are the cells, which are able to carry themselves from a hydrophilic to the lipid environment of the cell membrane, which ultimately reaches the blood. The hydrophilic plant constituents, which find their application in skin disorders, anti-ageing possess and different type of carcinomas are difficult in processing into conventional delivery system and hence transformed into phytosomes. Phytosomes are the complexes prepared by mixing polyphenolic phytoconstituents and phosphatidylcholine in molar ratio. Phytosomes are superior to the conventional drug delivery systems in terms of pharmacokinetic and pharmacodynamic properties. Phytosomal delivery of the extracts of Ginkgo biloba, Grape seed, Green tea, Ginseng, etc. has been profitably used. Phytosomes have been refined for therapeutic uses like cardiovascular, anti-inflammatory, immunomodulator, anticancer...

Sinigrin is a major glucosinolate present in plants of the Brassicaceae family. Recently, sinigrin and its phytosome formulations have been investigated for its wound-healing actions, by our research group. The aim of this study was to demonstrate sinigrin drug release from its phytosome complex and also to determine whether the phytosome complex enhances the delivery of sinigrin into the skin when compared to free sinigrin. In vitro Franz cell diffusion studies were performed on human abdominal skin. The morphology of the phytosome complex was examined by transmission electron microscopy. The in vitro drug release was determined using dialysis sacks. The in vitro drug release indicated a controlled and sustained release of sinigrin from the phytosome complex. Tape stripping results showed that the sinigrin-phytosome complex (0.5155 μg/ml) statistically significantly enhanced the delivery of sinigrin into the stratum corneum-epidermis when compared to the free sinigrin (0.0730 μg/ml...

Cell death (apoptosis) in the hippocampus is related to impaired memory functions. Gotu kola (Centella asiatica) contains asiatic acid and asiaticoside, which act as antioxidants and improve memory function. This study was intended to determine the effects of gotu kola extracts on Bcl-2 gene expression and spatial memory in rats with impaired memory functions due to trimethyltin (TMT) injection. The rats were subdivided into six groups, each group consisting of 10. The normal group was given sodium carboxymethyl cellulose (CMC-Na); the TMT group was given CMC-Na; the positive group was given 200 mg/kg bw citicoline; the extract groups were given a variation of gotu kola extract at 100 (P100), 200 (P200), and 400 mg/kg bw (P400) doses, respectively. These treatments were conducted for 35 days. TMT was injected intraperitoneally on Day 8 of treatment at a dose of 8 mg/kg bw in all groups except the normal group. On Days 29-35, the Morris water maze (MWM) spatial memory test was conduc...

Department of Biochemistry and Biotechnology, Moolji Jaitha College, Jalgaon-425002 ABSTRACT An attempt has been made to review some flavonoids rich medicinal plants of Maharashtra with the intention of their use in herbal drug delivery system. In this direction, a list of indigenous medicinal plants have been prepared with respect to the taxonomic name, vernacular names, family, parts used of these plants on the basis of literature. This article includes 181 medicinal plants of Maharashtra belonging to different 67 families. In the present review 27.07% trees, 17.13% shrubs, 48.07% herbs, few climbers, creepers and weeds are noted for the presence of flavonoids. Among the plant parts, mostly leaves contain more flavonoids than roots, stems, seeds, flowers, fruits and barks. The highest content of flavonoid as flavonol is present in Asteraceae family and an auntheticated chemotaxonomic marker of Asteraceae. Usually terpenes, edusmocoides, ginsenoside, flavonoids, epigallocatechi-3-o...

Phytosome is a complex of a natural active ingredient and phospholipids. The term ‘Phyto’ means plant while ‘some’ means cell like structure. It is claimed that phytosome increases absorption of "conventional herbal extracts" or isolated active principles both orally as well as topically. In this era phytosome gain popularity as a potential drug delivery device due to excessive demand and utility of herbs or herb based medicines. This advance technology offers amenities like improved absorption, enhanced delivery & increased bioavailability of herbal extracts. These drug-phospholipid complexes can be fabricated in the form of solution, suspension, emulsion, syrup, lotion, gel, cream, aqueous micro dispersions. Standardized plant extracts, mainly polar phytoconstituents like flavonoids, terpenoids, tannins, xanthones shall be introduced in form of phytosome.

Traumatic brain injury (TBI) is a disorder of the central nervous system due to head trauma. TBI can damage nerve membrane phospholipids and decrease protein synthesis of neuregulin-1 (NRG-1) because of the transcription factor Krox-20. These conditions cause the lowering in nerve re-myelination which contribute to the decline of cognitive function. In Indonesia, citicoline is a neuroprotective drug that widely used to repair and prevent further damage of the nerve cells membrane caused by trauma. Spade leaf (Centella asiatica) extract phytosome (SEP) is a model of drug delivery system which expected to enhance the therapeutic effects as neuroprotective drug. This study aims to demonstrate and compare the effectiveness from SEP and citicoline as a neuroprotective characterized by increasing the activation of Krox-20, the expression of NRG-1, the distribution of phospholipids, and the improvement of cognitive levels on TBI-induced rats. Rats were divided into 5 groups namely: control...

One of the herbs in Indonesia, Gotu Kola (Centella asiatica) contains triterpenoid glycosides, which are ethnomedicine used as neuroprotectors. Phytochemical components of Gotu Kola extract tend to be polar, so it needs an approach to modify the polarity of the extract. The method is to formulate an extract in the form of phytosome as an herbal delivery system so that it can increase the absorption and bioavailability of the active substance. It is suitable for the delivery system of active compounds from plants because it can carry hydrophilic and lipophilic compounds from plants. This paper specifically reviews the potential of the plant extracts for the recovery of nerve cell membranes and improving one's cognitive function.