Novel Phytosomes as Drug Delivery Systems and its Past Decade Trials
Aladin Khalaf Alla Elhaj Eltahir1, Hindustan Abdul Ahad1*, Chinthaginjala Haranath2,
Bake Meharajunnisa2, Siriguppa Dheeraj2, Badiginchala Navya Sai2
1Department of Industrial Pharmacy, Raghavendra Institute of Pharmaceutical Education and Research (RIPER)-Autonomous, Ananthapuramu – 515721, Andhra Pradesh, India.
2Department of Pharmaceutics, Raghavendra Institute of Pharmaceutical Education and Research (RIPER)-Autonomous, Ananthapuramu – 515721, Andhra Pradesh, India.
*Corresponding Author E-mail: abdulhindustan@gmail.com
ABSTRACT:
The present afford is to express phytosomes as a tool for aqueous and non-aqueous drug permeation. Phytosomes are prepared by conventional dynamic plant constituents like phospholipid (PL). Phytosomes build the interest of traditionalists in homegrown concentrates, in any case, energetic standards both orally and topically. Extensive literature from reputed journals was gathered and listed various drugs so far tried in the past decade. The phytosomes are capable of being used to induce acute and chronic liver failure due to enhanced pharmacological and pharmacokinetic assets. Phytosomes have successfully entered the market and are not well known as they are in the patent lock period. The study concludes that phytosomes are promising dosage forms for the delivery of plant extracts, which consist of both polar and non-polar constituents.
KEYWORDS: Decade, Delivery, Literature, Novel, Phytosomes.
INTRODUCTION:
Many active constituents from nature are polar and have issues related to bioavailability. This problem can be rectified by many approaches, among them phytosomes (Phyto-Phospholipid complexes), which are gaining the attraction of many industrial formulators in elevating reachability to the bloodstream. Phytosomes mean plant cells like consistency1-3. It is a new patented tactic in which standardized phytoconstituents are complexed with PLs to produce lipid-compatible molecular complexes, resulting in an elevation in absorption and bioavailability4. PTC-containing phytosomes easily traverse the biological layers5.
Phytosomes are made by complex medicaments with PLs that help them pass through the exterior layer of the gut and uniformly reach the blood6. After making PL complexes, membrane permeability is appreciably improved. Thus, phytosomes are freely absorbed and produce greater bioavailability than free drugs7.
STRUCTURE OF PHYTOSOMES:
Phytosomes are formed when medicament interacts with the polar heads of PLs to form a complex. In this structure, two long fatty acid chains do not participate in complex formation, and these condense the polar parts of complexes to form a lipophilic surface. Phytosomes form agglomerates when thinned in water, which looks like liposomes. The difference between phytosomes and liposomes is that they form an essential part of the membrane, the molecules of which overturn through hydrogen bonds to the polar head of the PLs8, 9.
THE DIFFERENCE BETWEEN LIPOSOMES AND PHYTOSOMES:
Phytosomes are distinguished from liposomes, which is illustrated10 in table 1.
Table 1: Differentiation between phytosomes and liposomes
|
Phytosomes |
Liposomes |
|
The fixings are broken down in the center segment of the cavity, with a fragmented chance of atomic contact between the encompassing lipid and a hydrophilic substance. |
A liposome is a strong spread of concentrate in a dietary PL network. The fixing can in some way or other contrast with a basic piece of the lipid layer. |
|
PL ratio 1:1 or 2:1 is preferred for the making of phytosomes. |
Improved the ratio up to 10 times more than the active constituents. |
|
Good bioavailability. |
Poor availability. |
|
It involves chemical bonds. |
No chemical bonds are involved. |
Figure 1: Difference between phytosome and liposome
PREPARATION OF PHYTOSOMES:
The design of phytosomes 11 is exemplified in figure 2.
Figure 2. Phytosomes preparation schematic diagram
.
PROPERTIES OF PHYTOSOMES:
The phytosomes have the following constraints 12.
Physiochemical properties:
· Organized with uniform plant substrate by the stoichiometric quantity of PL.
· The size ranged from 50 to 100 µm.
· Freely soluble in aprotic solvents, quite soluble in fats, and insoluble in water.
Biological properties:
· Increased oral absorption and bioavailability
· Better pharmacokinetic than herbal drugs.
Assets with Phytosomes:
The phytosomes have the following advantages 13.
· Appreciable drug entrapment efficiency
· Good gastric absorption
· Enhanced bioavailability
· No adverse effect on the liver as they are absorbed better in the small intestine.
· They are accepted for pharmaceutical and cosmetic use
· It suits even transdermal drug delivery
· Great stability
· Low-risk profile
· Ease of fabrication
· Ease of making.
Difficulties with phytosomes:
The phytosomes have the following advantages14.
· Phyto-constituents are rapidly eliminated from the dosage forms.
· The duration of action is short.
Classification of vesicles for novel drug delivery
The novel vesicles are classified15 as shown in table 2.
Table 2: Various types of vesicles as drug delivery systems based on size and composition
|
Name of the vesicles |
Particle size (nm) |
Shape |
Composition |
|
Phytosomes |
10–100 |
Spherical |
PL and herbal extract |
|
Niosomes |
100–140 |
Spherical |
Non–ionic surfactant and cholesterol |
|
Transferosomes |
170–230 |
Oval |
Soya phosphatidylcholine surfactant and drug/antigen |
|
Discomes |
16-20 |
Disc-shaped |
Cholesterol and Niosomes |
|
Aquasomes |
60-300 |
Circular |
Ceramics and carbon |
|
Resealed erythrocytes |
6000-9000 |
Oval |
Plasma and protein plates |
|
Ethosomes |
50–100 |
Spherical |
PL and ethanol |
|
Liposomes |
100–1000 |
Spherical |
PLs and cholesterol |
THE PAST DECADE OF WORK ON PHYTOSOMES:
Recent work done on phytosomes is illustrated in table 3.
Table 3: Past work is done on phytosomes
|
Phytosome complexes |
Techniques employed |
Solvents use |
Author and time of publication |
|
Catechin PL complex |
SD |
Anhydrous ethanol |
Athmouni et al., 202016 |
|
Raloxifene PL complex |
Solvent desertion method (SDM) |
Methanol, THF, anhydrous ethanol |
Li et al., 202017 |
|
Ursolic acid PL complex |
Solvent assisted – grinding method |
Methanol |
Wang et al., 201918 |
|
Dihydro myricetin - Hydrogenated soy PTC complexes |
Optimal preparation method |
Methanol and Chloroform |
Zhao et al., 201919 |
|
ATC PL complex |
Spray drying (SD) |
Anhydrous ethanol |
Qin et al., 201820 |
|
Insulin PL complex DNV method |
Thin-film hydration method SDM |
Methanol Trifluoroacetic acid Dichloro methane |
Xu et al., 201821 |
|
Phytosome complex of methanol extract of Terminalia Arjuna |
Salting out |
Methanol (6:1), n-hexane and methylene chloride |
Gnananath et al., 201722 |
|
BaPC – MD |
Discontinuous SDM |
Tetrahydrofuran |
Zhou et al., 2017 23 |
|
Polydatin PL complex (PPC) |
SDM |
Tetrahydrofuran |
Cheng et al., 201724 |
|
PL-based composite of standardized Centella extract |
Salting out |
Ethanol, N-Hexane |
Saoji et al., 201625 |
|
Quercetin PTC complex |
SD |
Anhydrous ethanol |
Zhang et al., 201626 |
|
Oleanolic acid PL compound |
SDM 1:1 molar ratio |
Anhydrous ethanol |
Jiang et al., 201627 |
|
Epigallocatechin gallate PL compound |
SDM |
Ethanol |
Yang et al., 201628 |
|
Pomegranate extract PL |
SD |
An equal volume of methanol and dioxane |
Vora et al., 201529 |
|
Rutin loaded nano Phyto some |
SDM Thin layer hydration method |
A combination of methanol and chloroform (1:4) |
Hooresfand et al., 201530 |
|
Rosmarinic acid – PL compound |
SDM |
Anhydrous ethanol |
Yang et al., 201531 |
|
Phyllanthus emblica extract PL compound |
SDM |
Dichloromethane or methanol as solvent |
Pereira et al., 201532 |
|
Echinoside PL compound |
SDM 1:3 molar ratio |
THF |
Li et al., 2015 33 |
|
Silymarin phospholipid compound |
SDM (1:5) |
Ethanol |
Maryana et al., 201534 |
|
Leutolin phospholipid compound |
SDM by QbD employed |
Ethanol |
Khan et al., 2014 35 |
|
Plain liposomes and Phyto – liposomes |
Reversed-phase evaporation method |
Di ethyl ether |
Angelico et al., 201436 |
|
Soy -lecithin complex |
SDM |
N – Octanol or water |
Yu et al., 201437 |
|
Mangiferin PL complexation |
SD |
Ethanol |
Ma et al., 201438 |
|
Mitomycin C |
SDM |
Tetra hydro furan |
Hou et al., 201339 |
CONCLUSION:
This assessment is a push to introduce an outlining profile according to Phytosome's advantage, concoction properties, physical attributes, strategy for planning, and applications. The poor bioavailability and ingestion of water-dissolvable phytoconstituent could be overwhelmed by the phytosomes approach, as it gives an ideal conveyance of dynamic phytoconstituents. Phytosomes are progressed to liposomes because of their steadiness profile. Phytosomes innovation has a gigantic methodology for use in definition innovation and capacity of hydrophilic plant separate. It is an incredible methodology and inventive detailing for homegrown concentrate which shows better absorption than ordinary natural concentrate.
CONFLICT OF INTEREST:
None.
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Received on 05.04.2021 Modified on 10.03.2022
Accepted on 22.11.2022 ©AandV Publications All Right Reserved
Res. J. Pharma. Dosage Forms and Tech.2023; 15(1):51-54.
DOI: 10.52711/0975-4377.2023.00009