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Further reading
[1] Aguiló-Aguayo I, Abreu C, Hossain MB, et al. Exploring the effects of pulsed electric field processing parameters
on polyacetylene extraction from carrot slices. Molecules 2015;20(3):3942e54.
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pharmaceutical aspects. Pharmaceutical Research 1995;12:1561e72.
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17 siRNA and corticosteroid for topical treatment of psoriasis. Medical Hypotheses 2020;145:110322.
4. Lipid-based particulate systems for delivery of plant actives and extracts: Extraction, prospective carriers, and safety issues114
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5
Phyto-complexed systems as a
versatile tool for the delivery of
plant-based drugs
Madhuri Baghel
1
, Pooja Yadav
2
, Hemant Badwaik
1
,
Kartik Nakhate
3
and Ajazuddin
2
1
Shri Shankaracharya Institute of Pharmaceutical Sciences and Research, Bhilai, Chhattisgarh,
India;
2
Rungta College of Pharmaceutical Sciences and Research, Bhilai, Chhattisgarh, India;
3
Shri Vile Parle Kelavani Mandal’s Institute of Pharmacy, Dhule, Maharashtra, India
List of abbreviations
CD Cyclodextrin
CHGS Chitooligosaccharide
CM-CD O-Carboxymethyl- b-CD
CME-CD O-Carboxymethyl-O- Ethyl- b-CD
DE-CD 2,6-Di-O-Ethyl-b-CD
DSC Differential Scanning Calorimetry
G-CD Gamma CD
GAS Gas Antisolvent
HP-CD 2-Hydroxypropyl- b-CD
ICs Inclusion Complexes
IR Infrared
NMR Nuclear Magnetic Resonance
Pa Pascal
PHC Phosphatidylcholine
PHL Phospholipid
SAS Supercritical Antisolvent Process
SCF Supercritical Fluid
SEDS Solution-Enhanced Dispersion by SCF
SME-CD Sulfate and Sulfobutylether b-CD
TEM Transmission Electron Microscopy
TM-CD Trimethyl- b-CD
XRD X-ray Powder Diffraction
CHAPTER
115
Phytopharmaceuticals and Herbal Drugs
https://doi.org/10.1016/B978-0-323-99125-4.00005-6 © 2023 Elsevier Inc. All rights reserved.
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1. Introduction
The food, cosmetics, and pharmaceutical industries have all made extensive use of phyto-
chemicals derived from plants [1]. Flavonoids, polyphenolics, alkaloids, terpenoids, tannins,
glycosides, vitamins, carotenoids, phytosterols, oleoresins, and volatile oils are the examples
of secondary plant metabolites that have been shown to have a significant impact in a variety
of industrial and commercial applications such as healthcare, insect repellents, cosmetics, fra-
grances, flavors, and preservatives. Because of the limited safety profile associated with syn-
thetic substances, research into phytochemicals and their usage has exploded in recent years.
Chemical variety ranging from low molecular mass, one or many aromatic ring, and simple
chemicals to complex and massive derivatives is related with their different biological prop-
erties. However, most of them have radical scavenging, antioxidant, and other therapeuti-
cally potential health benefits [2e16].
In the current context, the number of pharmaceutical products based on phytochemicals is
large, and their importance to the global economy is steadily increasing. Phytochemicals have
been adopted as main active ingredients in a large number of health products, nutritional
supplements, and cosmetics. However, the efficacy of these active constituents is highly influ-
enced by preservation of their bioactivity, stability, and bioavailability [17]. Previous re-
searchers [18] found that these compounds’ poor water solubility and quick degradation
pose a significant barrier to their usefulness. For tackling these chal lenges in pharmaceutical
product development, many strategies such as solvent deposition, solid dispersion, micron-
ization, supercritical fluid (SCF) process, use of salt forms, use of surfactants, and complex-
ation have been examined [19e21]. Each of these methods has their own advantages and
disadvantages. The complexation process has been used more widely and accurately to in-
crease the solubility, dissolution, and bioavailability of pharmaceuticals that are poorly water
soluble. Phospholipid (PHL), cyclodextrin (CD), and chito-oligosaccharide (CHGS) complex-
ation are the most widely studied approaches among the complexation techniques. As a
result, this chapter aims to provide an overview of phyto-complex techniques used for the
delivery of plant-based drugs specially phytoconstituents for the treatment of various dis-
eases. Table 5.1 lists the types of phyto-complexes, active ingredients, biological activities,
and particular indications.
2. Complexation
The reversible interaction of a substrate and ligand to produce a new species is known as
complexation. Complexes are divided into two categories based on the type of chemical
bonding: Coordination complexes and molecular complexes. Coordinate bonds form coordi-
nation complexes, in which pair of electrons transfer from one interacting moiety to the other
to some extent. Metaleion coordination complexes between metal ions and bases are the
most prominent examples.
5. Phyto-complexed systems as a versatile tool for the delivery of plant-based drugs116
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TABLE 5.1 Published works regarding phyto-complexes of phospholipids, cyclodextrins, and
Chitooligosaccharides.
Activity Bioactive Phyto-complex References
Phospholipid phyto-complex
Hepatoprotective Curcumin Soy phospholipid [22]
Silymarin Soy phospholipid [23]
Quercetin Hydrogenated soy phosphatidyl choline [24]
Silybin Soy phospholipid [25]
Silybin Phosphatidylcholine [26]
Brain disease Curcumin Soy lecithin [27]
Chronic hepatitis C treatment Silybin Soy phosphatidylcholine [28]
Silybin and vitamin E Phospholipid [29]
ND (improved
pharmacokinetics)
Silybin Phosphatidylcholine [30]
Anticancer Curcumin Phospholipid [31]
[32]
Celastrol Soy phosphatidylcholine [33]
Curcumin Phosphatidylcholine [34]
Silybin Phosphatidylcholine [35]
[36]
Antioxidant Silybin Phosphatidylcholine [37]
Naringenin Phosphatidylcholine [38]
Myricetin Phosphatidylcholine [39]
Antiinflammatory activity Rutin Phosphatidylcholine [40]
Ruscogenin Phosphatidylcholine [41]
Luteolin Soy phosphatidylcholine [42]
Immunomodulator Echinacea Phosphatidylcholine [43]
Cyclodextrin phyto-complex
Antiinflammatory Diosmin b-CD, HP- b -CD [44,45]
Baicalein HP- b -CD [46]
Curcumin b-CD [47]
Arbutin HP-b-CD [48]
b-Caryophyllene M-b
-CD [49]
(Continued)
2. Complexation 117
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