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14.2 Some Industrially Important Pharmaceutical Aids 281
HOOC
HO
HOOC
O
HO
OH
O
HO
OH
O
O
OH
HOOC
O
O
OH
HOOC
O
HO
OH
O
HO
OH
O
HO
OH
OH
O
O
O
O
Figure 14.12 Chemical structure and sugars of tragacanth gum.
are found in Iran, Turkey, India, Afghanistan, and Russia and
belong to the leguminous family. Astragalus plants secrete
sap to protect their tissues from harm, serve as a defensive
tool, and are known as exudate gum. The wounded plant
portion is coated with exudates, solidifying into flakes upon
air exposure and sunshine. The molecular structure of gum
tragacanth is a highly complex polysaccharide consisting of
acidic, heterogeneous, and branching proteoglycans (Figure
14.12). It has a high molecular weight of around 840 kDa and
an elongated form measuring 4500 19A . [140, 141]. Gum tragacanth consists of two distinct components: bassorin, which
makes up 60–70% of the compound, and tragacanthin, which
accounts for 20–30%.
Tragacanthin is a substance that can dissolve in water. It
can be separated into two parts: a component that cannot
dissolve in ethanol, called tragacanth acid, and a part that
can dissolve in ethanol, called arabinogalactan. Both bassorin and tragacanthic acid exhibit hydrophobic properties,
making them water-insoluble. Both fractions have small
amounts of methoxyl groups, and proteinaceous substances combine, forming thick gel-like substances [142]. It
is a naturally occurring material in significant quantities in
the aqueous soluble fractions. Gum tragacanth has found
broad applications as a suspending agent, stabilizer, thickening, and emulsifying agent in numerous culinary and
medicinal formulations. Moreover, it has been extensively
utilized as a well-established pharmaceutical excipient in
various pharmaceutical tablets, acting as a matrix-former
and facilitating prolonged drug release. Its chemical and
physical transformations have contributed significantly to
its widespread usage in the development of diverse drugreleasing hydrogels [143–146].
HOOC
O
HO
OH
O
HO
OH
O
O
O
OH
OH
OH
OH
HOOC
O
HO
O
HOOC
O
O
OH
HOOC
O
HO
OH
O
OH
O
HO
O
OH
O
HO
OH
lies in the presence of β (2 → 1) linkage, which accounts
for its reduced calorific values and the beneficial dietary
fiber effect. As a sought-after ingredient in the food industry, inulin has gained popularity. Recently, inulin and its
derivatives have found extensive applications in the pharmaceutical industry, particularly as excipients. The advantageous suitability of inulin in drug delivery systems stems
from its prompt water solubility, stability, and resilience
against gastric and intestinal enzymes, rendering it a
promising option [147–149].
14.2.16 Lawsone
Lawsone, also known as henna or hennotannic acid, is a
natural dye extracted from the leaves of the Lawsonia iner-
mis plant. While it is widely recognized for its use in traditional body art and hair coloring, lawsone has found
applications beyond cosmetics, making its mark in the
pharmaceutical industry. Lawsone’s unique chemical
properties allow it to form stable complexes with proteins
and enzymes. Its compatibility with different pharmaceutical excipients provides flexibility in formulation design.
Moreover, lawsone has been explored for its potential antioxidant and anti-inflammatory properties, suggesting that
its incorporation into pharmaceutical formulations may
offer additional therapeutic benefits. It is widely used in
the textile and cosmetic industry as a coloring agent. As
research continues to uncover the diverse properties of
lawsone, its role as a natural dye in pharmaceuticals presents an intriguing avenue for enhancing both the aesthetic
and functional aspects of drug delivery systems [150, 151].
14.2.15 Inulin
Inulin, a diverse polysaccharide, is prevalent in several
plants, including chicory, dalia, Jerusalem artichoke,
onion, and garlic. It is comprised of units of β-D-(2 → 1)
fructosyl fructose (fructan), with an initial unit of α–D-
glucose. The molecular length of inulin varies, spanning
from 2 to 60 fructan units. The distinctive feature of inulin
14.2.17 Locust Bean Gum
Carob bean gum is an alternative name for locust bean
gum. The plant-derived seed gum is obtained from the
carob tree seeds (Ceratonia siliqua) [152]. The extracted
locust bean gum is obtainable in a powdered state and
exhibits a whitish to yellowish-white hue. It is a type of
biopolymer with branches and is non-ionic in its properties
[153]. The molecular composition of locust bean gum
282 14 Pharmaceutical Aids of Natural Origin
consists of a heteropolysaccharide of the galactomannan
type, which is made up of interconnected galactose and
mannose residues. These residues are linked together
through glycosidic bonds in a ratio of 1 : 4. The structure is
composed of a β-D-mannopyranose skeleton with (1, 4)
linkages attached to α-D-galactose [154]. Locust bean gum
has low water solubility, necessitating the application of
gentle heat to create aqueous solutions. Locust bean gum is
commonly recognized as a biocompatible, biodegradable
biopolymer that does not harm developing embryos or
cause genetic mutations. It has been employed as prospective medicinal excipients in several pharmacological dosage
regimens [155]. Even at lesser concentrations, locust bean
gum can create very viscous aqueous solutions that are
resistant to changes in salt content, temperature, and pH
[156]. Locust bean gum is commonly used in the preparation of oral medication tablets for release, and it enhanced
bio-mucoadhesive properties in several mucoadhesive drug
delivery systems [14, 157]
14.2.18 Pectins
Pectins are water-soluble, natural complex biopolysaccharides that are non-starch, cheap, non-toxic to neonates,
and found in the cell walls of plants (12). “Natural sources
of pectin encompass citrus fruits, apple pomaces, beetroots, and similar sources. Pectin has been employed as
emulsifiers, gelling agents, stabilizer, and thickening
agents in various applications. Pectins comprise biopolymers with a linear chain of α (1, 4) glycosidic connecting
D-galacturonic acid residues. As depicted in Figure 14.13,
pectin’s molecular structure comprises main chains of
galacturonic acid occasionally interspersed with rhamnose groups. These rhamnose groups disrupt the chain
helix and α-L-rhamnopyranose arrangement through an
α-(1-2) linkage” [158]. In scientific literature, the characterization of pectin molecules is commonly determined by
assessing the extent of esterification of carboxylic acid
groups in pectinic acid, the presence of methoxy groups,
and, in specific instances, evaluating the degree of amidation [159]. Pectins are classified into two distinct types
based on the extent of methoxylation: high methoxy pectins, characterized by a methoxylation degree ranging
from 50–80%, and low methoxy pectins, with a methoxylation degree falling between 25 and 50% [160].
Principal properties of pectins, such as swelling, gelling capacity, and water solubility, are based on the
extent of esterification. A better gelling effect can be
expected with low methoxy pectins due to ionotropic
cross-linking of it with divalent metal cations (e.g. Zn2+,
Ca2+, etc.), and this gelled pectinate matrices are used
as potential sustained releasing carriers [161]. Pectins
have been extensively used as a pharmaceutical aid in
emulsions, suspensions, tablets, granules, beads, microparticles, nanoparticles, gels, hydrogels, films, film coating, scaffolds, matrix-forming, and sustained release
drug delivery [162–164]. Low-methoxy pectin has
recently been used as a buoyant as well as sustainedrelease drug delivery system due to its ionotropic gelling
matrix [111, 129, 165–167]. Owing to their hydrophilic
nature, pectins exhibit limitations in safeguarding drugs
during the transit of pectin-based formulations specifically tailored for delivering or targeting drugs to the
colon [109, 168].
14.2.19 Starch
Starch, a versatile carbohydrate derived from various plant
sources, such as corn, potatoes, and wheat, plays a crucial
role in the pharmaceutical industry as an essential excipient.
Its multifaceted properties make it an ideal choice for various pharmaceutical formulations. Starch is a binder, imparting tablet cohesiveness and ensuring structural integrity
during manufacturing and handling. Additionally, it acts as
O
OH
Figure 14.13 Chemical structure of pectin.
O
OH
COOH
O
OH
O
COOCH
COOCH
O
OH
3
acetylation
methylation
3
O
OH
O
COOH
COOCH
O
3
O
14.2 Some Industrially Important Pharmaceutical Aids 283
a disintegrant, promoting the rapid breakdown of tablets
upon ingestion and facilitating drug release and absorption.
Starch’s mucoadhesive properties make it valuable in oral
formulations, promoting prolonged contact with mucosal
surfaces for controlled drug delivery. Its biocompatibility
and inert nature make it suitable for oral and topical formulations, ensuring patient safety and compliance. Starch is
also utilized as a filler, diluent, and stabilizer in various dosage forms, contributing to pharmaceutical products’ overall
quality and stability. Furthermore, its binding capabilities
extend to granules in wet granulation processes, enhancing
the flow properties of powders and facilitating uniform drug
distribution.
Some of the common chemical forms of starch used in
drug delivery include cross-linked starch, hydroxyethyl
starch (HES), hydroxypropyl starch (HPS), carboxymethyl
starch (CMS), oxidized starch, and starch phosphates.
Cross-linking entails the establishment of covalent
bonds among starch molecules, leading to heightened
resilience against enzymatic breakdown. Cross-linked
starch is commonly employed to improve the stability and
control drug release in formulations. Hydroxyethylation
introduces hydroxyethyl groups to the starch structure,
enhancing solubility and reducing retrogradation. HES is
often used as a plasma volume expander and has been
investigated for its potential in drug delivery systems.
Like HES, hydroxypropylation involves adding hydroxypropyl groups to starch, improving its solubility and filmforming properties [169]. HPS is utilized in different
pharmaceutical formulations for controlled drug release.
Acetylation introduces acetyl groups to starch, resulting
in modified physicochemical properties [170]. Acetylated
starch is known for its improved stability and reduced
susceptibility to enzymatic degradation, making it suitable for drug delivery. Carboxymethylation introduces carboxymethyl groups to starch, enhancing its water
solubility and swelling capacity. For its mucoadhesive
properties, CMS is utilized in oral drug delivery systems,
facilitating prolonged contact with mucosal surfaces.
Oxidation involves the introduction of carbonyl and carboxyl groups to starch molecules. Oxidized starch is utilized to improve starch compatibility with other polymers
and enhance its functional properties in drug delivery.
Phosphorylation introduces phosphate groups to starch,
modifying its properties for specific applications. Starch
phosphates are investigated for their potential as drug
carriers and stabilizers in pharmaceutical formulations
[171–178]. The chemical alterations applied to starch
introduce a spectrum of characteristics that can be customized to align with the distinct demands of various
drug delivery systems, encompassing sustained release,
targeted delivery, and heightened bioavailability. Each
variant of modified starch presents distinct merits, affording formulators the capability to devise pharmaceutical
products endowed with augmented performance and
functionality.
14.2.20 Tamarind Gum
Tamarind gum is a natural substance derived from the
tamarind tree. It is also known as Indian dates, biologically referred to as Tamarindus indica L. (Family:
Leguminosae), also known as imli in Hindi, and its seeds
are the source of tamarind gum [179, 180]. A storage unit
with a cell wall makes up the endosperm of tamarind
seeds, which can be separated from the powdered tamarind seed kernel by several well-established methods [181,
182]. A systematic series of procedures encompassing the
meticulous selection of mature tamarind seeds, subsequent removal of the seed coat, and segregation of the
seed kernel, followed by processes of milling, grinding,
and ultimately sieving, were employed to acquire tamarind seed kernel powder from fully matured and harvested
tamarind seeds. Tamarind gum is a biopolysaccharide that
dissolves in water. It is accurately classified as a galactoxyloglucan. Xylopyranose (α-D) and β-D-galactopyranosyl
(1-2)-α-D-xylopyranose linked (1-6) to glucose residues
make up the backbone of the gum [183, 184]. This pharmaceutical aid exhibits important characteristics like
hydrophilicity, water solubility, biodegradability, chemical
stability in acidic conditions, biocompatibility, and nonirritating properties. Due to its many uses in pharmaceutical formulations, including as a mucoadhesive, matrixformer, suspending agent, thickening agent, gel-producing agent, stabilizer, emulsifier, tablet binder, and filmproducing agent [183–186].
Furthermore, it functions as a component that forms a
matrix in manufacturing extended-release tablets for several medications. Because of its exceptional hydrophilic
and bio-mucoadhesive qualities, tamarind gum creates
several bio-mucoadhesive drug delivery systems. Tamarind
gum has been the subject of numerous recent attempts to
modify it and assess its suitability as a medicinal excipient
in different kinds of treatment [180, 187].
14.2.21 Xanthan Gum
Xanthan gum is a biopolymer produced via the use of the
bacterium Xanthomonas campestris through the fermentation of extracellular polysaccharides in the presence of carbohydrates consisting of sucrose and glucose. The chemical
structure of xanthan gum is composed of pentasaccharide
284 14 Pharmaceutical Aids of Natural Origin
subunits containing D-glucosyl, D-glucuronyl acid, and
14.3 Conclusion
D-mannosyl residues, which are distributed in varying proportions between O-acetyl and pyruvyl residues, retaining a
ratio of 2 : 2 : 1. It is undergoing confirmation changes when
exposed to heat, resulting in a linear, unbranched structure.
Xanthan gum exhibits exceptional water solubility. The
material demonstrates favorable biocompatibility and outstanding biodegradability. Temperature fluctuations, a more
extensive range of ionic strength, and pH variations do not
affect it. Xanthan gum finds widespread application in various culinary and pharmaceutical contexts. As a potential
pharmaceutical excipient, it has been incorporated into
diverse drug delivery systems, spanning oral, buccal, and
topical formulations [143, 188–190].
Table 14.1 Use of some natural pharmaceutical aids in various formulations.
Sr.
Pharmaceutical aid Use References
No.
1. Acacia gum /Gum Arabic Binder, film-coating agent, matrix-forming agent, sustained-
2. Albumin & chitosan Sustained releasing agent, encapsulating agent, matrix-forming
3. Alginate Matrix-forming agent, sustained releasing agent, gelling agent,
4. Curcumin Colorant, antimicrobial, and antioxidant. [93, 94, 97, 99]
5. Gelatin Film-forming agent, matrix-forming agent, sustained releasing
6. Gellan gum Matrix-forming agent, sustained releasing agent, gelling agent,
7. Guar gum Film-forming agent, Matrix-forming agent, sustained releasing
8. Gum tragacanth Binder, Matrix-forming agent, sustained releasing agent,
9. Lawsone Colorant, antimicrobial, and antioxidant. [150, 151]
10. Locust bean gum Superdisintegrant, matrix-forming agent, and sustained
11. Pectin Matrix-forming agent, sustained releasing agent, encapsulating
12. Starch Binder, lubricant, glidant, Sustained release, bioavailability
13. Sterculia gum/ Gum
Karaya
14. Tamarind gum Matrix-forming agent, sustained releasing agent, gelling agent,
15. Xanthan gum Coating agent, matrix-forming agent, sustained releasing agent,
release agent, encapsulating agent, release retardant, osmotic
agent, suspending agent, expanding agent, injectable gelling
agent, and emulsifier.
agent, photoresponsive agent, and film-forming agent.
encapsulating agent, and mucoadhesive agent.
agent, encapsulating agent, mucoadhesive agent, and colon
targeting agent.
encapsulating agent, and mucoadhesive agent.
agent, encapsulating agent, mucoadhesive agent, and colon
targeting agent.
encapsulating agent, and mucoadhesive agent.
releasing agent.
agent, coagulating agent, mucoadhesive agent, buoyant (floate)
imparting agent, and colon targeting agent.
improvement, and film coating.
Colon targeting agent, matrix-forming agent, sustained releasing
agent, encapsulating agent, and mucoadhesive agent.
encapsulating agent, mucoadhesive agent.
encapsulating agent, and mucoadhesive agent.
In conclusion, there has been significant interest among
researchers in utilizing pharmaceutical aids originating
from natural sources to develop a diverse range of traditional dosage forms and NDDS. Recently, chemically
altered versions of natural excipients have been widely
employed to address limitations associated with their original forms. These modified excipients are not only valuable
in the pharmaceutical field but also find relevance in different kinds of industries, such as food, textiles, and paper
(Table No. 14.1).
In pharmaceutical research and development, natural
excipients play a crucial role in formulating various drug
[16–18, 20, 21, 24, 25]
[30, 33, 37, 40, 68, 69, 76, 78,
81, 82]
[43, 46–8, 52, 191]
[64, 101, 102, 105, 118]
[106, 107, 113, 114]
[115, 118–121, 123, 124, 127]
[143, 192–195]
[14, 83, 157, 196, 197]
[75, 129, 164, 166, 198–200]
[169, 172–175]
[132, 133, 137, 139]
[67, 134, 184, 201–204]
[84, 188, 205–209]
References 285
delivery systems, including oral, topical, brain-targeted,
buccal, and other demanding delivery methods. The distinctive attributes of natural pharmaceutical aids, such as
biodegradability, biocompatibility, and nonallergenic properties, position them as promising pharmaceutical excipients. These properties make them suitable for formulating
diverse dosage forms, such as tablets, capsules, pills, pellets, spheroids, beads, microparticles, nanoparticles, films,
gels, hydrogels, scaffolds, and more.
In the pharmaceutical realm, there is an expanding preference for natural excipients over synthetic ones, aiming to
ensure precise and desired drug delivery to specific targets
at the right time. Moreover, these natural excipients contribute to improved bioavailability, stability, and patient
acceptance, and they validate the safety and efficacy of
drug administration. The ongoing and future research on
such kinds of pharmaceutical aids is essential to uncover
their diverse characteristics and potential roles in drug
delivery, ultimately leading to the development of more
effective pharmaceutical formulations. The future outlook
for exploring and harnessing new natural material appears
highly promising, paving the way for further advancements
in pharmaceutical applications.
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