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