NATURAL POLYSACCHARIDES AS PHARMACEUTICAL EXCIPIENTS · The focus should be directed towards the...

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www.wjpr.net Vol 3, Issue 2, 2014. 3776 NATURAL POLYSACCHARIDES AS PHARMACEUTICAL EXCIPIENTS Vilas A. Arsul * 1 , Dr. S. R. Lahoti 2 1 Research Scholar, School of Pharmaceutical Sciences, Jaipur National University, Jaipur, Rajasthan. 2 Professor, Department of pharmaceutics, Y. B. Chavan College of Pharmacy, Aurangabad. ABSTRACT Proper design and formulation of a dosage form requires consideration of the physical, chemical and biologic characteristics of the drug substances and pharmaceutical ingredients to be used in fabricating the product. Excipients facilitate the formulation design and perform a wide range of functions to obtain desired properties for the finished drug product. Polysaccharide hydrocolloids including mucilages, gums and glucans are abundant in nature and commonly found in many higher plants. These polysaccharides constitute a structurally diverse class of biological macromolecules with a broad range of physicochemical properties which are widely used for various applications in pharmacy and medicine. Polysaccharide (Gums and mucilages) functions as versatile excipients such as Suspending Agent, Emulsifying Agent, Binder, Gelling Agent, Disintegrant etc. for pharmaceutical formulations. The polysaccharides can also be modified in different ways to obtain tailor-made materials for drug delivery systems and thus can compete with the available synthetic excipients. KEY WORDS: Natural Polysaccharides, Excipients, Modification, Gums and Mucilages. INTRODUCTION Drug substances are usually not administered as they are in their pure state, but rather as part of a dosage form where they are usually combined with other agents (excipients), which could be non-medicinal. [1] Excipients are the additives used to convert active pharmaceutical ingredients into pharmaceutical dosage form suitable for administration to patients. [2] Excipients were defined as ‘the substance used as a medium for giving a World Journal of Pharmaceutical ReseaRch Volume 3, Issue 2, 3776-3790. Review Article ISSN 2277 – 7105 Article Received on 10 January 2014, Revised on 27 January2014, Accepted on 28 February 2014 *Correspondence for Author VILAS A. ARSUL Research Scholar, School of Pharmaceutical Sciences, Jaipur National University, Jaipur, Rajasthan. [email protected]

Transcript of NATURAL POLYSACCHARIDES AS PHARMACEUTICAL EXCIPIENTS · The focus should be directed towards the...

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NATURAL POLYSACCHARIDES AS PHARMACEUTICAL

EXCIPIENTS

Vilas A. Arsul *1, Dr. S. R. Lahoti 2

1Research Scholar, School of Pharmaceutical Sciences, Jaipur National University, Jaipur,

Rajasthan. 2Professor, Department of pharmaceutics, Y. B. Chavan College of Pharmacy, Aurangabad.

ABSTRACT Proper design and formulation of a dosage form requires consideration

of the physical, chemical and biologic characteristics of the drug

substances and pharmaceutical ingredients to be used in fabricating the

product. Excipients facilitate the formulation design and perform a

wide range of functions to obtain desired properties for the finished

drug product. Polysaccharide hydrocolloids including mucilages, gums

and glucans are abundant in nature and commonly found in many

higher plants. These polysaccharides constitute a structurally diverse

class of biological macromolecules with a broad range of

physicochemical properties which are widely used for various

applications in pharmacy and medicine. Polysaccharide (Gums and

mucilages) functions as versatile excipients such as Suspending Agent, Emulsifying Agent,

Binder, Gelling Agent, Disintegrant etc. for pharmaceutical formulations. The

polysaccharides can also be modified in different ways to obtain tailor-made materials for

drug delivery systems and thus can compete with the available synthetic excipients.

KEY WORDS: Natural Polysaccharides, Excipients, Modification, Gums and Mucilages.

INTRODUCTION Drug substances are usually not administered as they are in their pure state, but rather as part

of a dosage form where they are usually combined with other agents (excipients), which

could be non-medicinal. [1] Excipients are the additives used to convert active

pharmaceutical ingredients into pharmaceutical dosage form suitable for administration to

patients. [2] Excipients were defined as ‘the substance used as a medium for giving a

World Journal of Pharmaceutical ReseaRch

Volume 3, Issue 2, 3776-3790. Review Article ISSN 2277 – 7105

Article Received on 10 January 2014, Revised on 27 January2014, Accepted on 28 February 2014

*Correspondence for

Author

VILAS A. ARSUL

Research Scholar, School of

Pharmaceutical Sciences,

Jaipur National University,

Jaipur, Rajasthan.

[email protected]

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medicament’, that is to say with simply the functions of an inert support of the active

principle or principles. [3]

Reasons for developing new excipients

With the increasing interest in excipients of natural origin, the pharmaceutical world has

compliance to use most of them in their formulations. Moreover, the tremendous orientation

of pharma world towards these naturally derived polysaccharides has become a subject of

increasing interest to discover, extract and purify such compounds from the reported origin.

[4]

The focus should be directed towards the development of the newer excipients, so that they

can enter the pharmaceutical industry and newer formulations could be developed and

formulation problems could be solved. [5]

Polysaccharide in Plant Parts

Polysaccharide hydrocolloids including mucilages, gums and glucans are abundant in nature

and commonly found in many higher plants. These polysaccharides constitute a structurally

diverse class of biological macromolecules with a broad range of physicochemical properties

which are widely used for various applications in pharmacy and medicine. [4]

Gum and Mucilage

Gums are considered to be pathological products formed following injury to the plant or

owing to unfavourable conditions, such as drought, by a breakdown of cell walls (extra

cellular formation; gummosis).

Mucilage’s are generally normal products of metabolism, formed within the cell (intracellular

formation) and/or are produced without injury to the plant. Gums readily dissolve in water,

whereas, mucilage form slimy masses. [3]

Advantages of natural gums and mucilages in pharmaceutical sciences

The following are a number of the advantages of natural plant–based materials.

Biodegradable—Naturally available biodegradable polymers are produced by all living

organisms. They represent truly renewable source and they have no adverse impact on

humans or environmental health (e.g., skin and eye irritation).

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Biocompatible and non-toxic—chemically, nearly all of these plant materials are

carbohydrates composed of repeating sugar (monosaccharide’s) units. Hence, they are

non- toxic.

Low cost—it is always cheaper to use natural sources. The production cost is also much

lower compared with that for synthetic material. India and many developing countries are

dependent on agriculture.

Environmental-friendly processing—Gums and mucilages from different sources are

easily collected in different seasons in large quantities due to the simple production

processes involved.

Local availability (especially in developing countries) —in developing countries,

government promote the production of plant like guar gum and tragacanth because of the

wide applications in a variety of industries.

Better patient tolerance as well as public acceptance— there is less chance of side and

adverse effects with natural materials compared with synthetic one. For example, PMMA,

povidone. Edible sources—Most gums and mucilages are obtained from edible sources.

[7]

Isolation and purification of Polysaccharides

Plant material is dried in sunlight (preferably) or in an oven at 105˚C to retain its properties

unchanged. Generally, chlorophyll or pigments are present in the plant which should be

removed before isolating the mucilage. Plant material must be treated with petroleum ether

and chloroform (to remove pigments and chlorophyll) and then with distilled water. Care

should be taken when drying the final isolated/extracted mucilage. It must be dried at a very

low temperature (not more than 50˚C) or in a vacuum. The dried material is stored carefully

in desiccators to prevent further moisture uptake or degradation. [7]

Characterization / Standardization of Polysaccharides

The characterization of gums and mucilages is initially achieved by only a multiple-technique

approach. For excipient analysis, analytical techniques can be classified according to the type

of information generated. It is necessary to determine the properties of these polysaccharides

before been used as excipients in any formulation in order to achieve the goal intended of the

formulation. [6]

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Table No 1: Preliminary confirmative tests for Polysaccharides

Sr. No Test Observation Inference

1. Molisch’s test: (100 mg dried mucilage powder + Molisch’s reagent + conc. H2SO4 on the side

of a test tube)

Violet green color observed at the junction

of the two layers

Carbohydrate present

2.

Ruthenium test: Take a small quantity of dried mucilage powder, mount it on a slide with

ruthenium red solution, and observe it under microscope

Pink color develops Mucilage present

3. Iodine test: 10 0mg dried mucilage powder +1 ml 0.2 N iodine solution

No color observed in solution

Polysaccharides present(starch is

absent)

4.

Enzyme test: dissolve 100 mg dried mucilage powder in 20 ml-distilled water; add 0.5 ml of

benzidine in alcohol (90%). Shake and allow to stand for few minutes

No blue color produced

Enzyme absent (Distinction

between dried mucilage and

Acacia) Gums and Mucilages as versatile excipients for pharmaceutical formulations

1. Suspending Agent

Some excipients are currently available for the formulation of pharmaceutical suspensions. A

pharmaceutical suspension, like other disperse systems, is thermodynamically unstable, thus,

making it necessary to include in the dosage form, a stabilizer or suspending agent which

reduces the rate of settling and permits easy redispersion of any settled particulate matter both

by protective colloidal action and by increasing the consistency of the suspending medium.

These suspending agent increase sedimentation volume, ease redispersibility, enhance

pourability and prevent compact cake formation. Suspending agents are grouped into three

classes. (i) Synthetic (ii) semi synthetic and (iii) the natural polysaccharides, in which class

Acacia, tragacanth, karaya, Xanthan gum, Hibiscus mucilage etc.

2. Emulsifying Agent

Many of the natural excipient used in the preparation of the emulsion, as emulsion is

thermodynamically unstable, to stabilise it addition of emulsifying agent necessary. Now

days, instead of using the synthetic agent, use of natural emulsifying agent increase due to

low toxicity, low cost, and biocompatibility.

3. Binder

Polysaccharides act as binders by causing aggregation of powders thereby forming granules

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through the process of granulation. They modify the cohesive properties of the granules by

promoting the formation of strong cohesive bonds between such partial. The choice of the

binding agent depends on the binding force required to form granules and its compatibility

with the other ingredients particularly their active drug.

4. Disintegrating agent

Disintegrants are substances that are added to formulations to dissolve more rapidly in

aqueous environment. Polysaccharides extracted have been used as disintegrants due to their

swelling properties. They can display good binding property; both of these properties depend

upon the concentration of mucilage in formulation, generally in the 1 to 10% concentration of

total tablet weight. Polysaccharides can act as base for gel preparation and above it they act

as disintegrant.

5. Sustained Release Polymer

Among various dosage forms, matrix tablets are widely accepted for oral sustained release as

they are simple and easy to formulate. Matrix system is the specific type of release system,

which prolongs and controls the release of drug that is dissolved or dispersed. Various natural

gums and mucilages have been examined as polymer for sustained release formulations.

Mucilage from Aloe barbadensis Miller have been used as a pharmaceutical excipient for

sustained release matrix tablets. Results showed that the dried Abelmoschus esculentus fruit

mucilage can be used as a matrix forming material for controlled release matrix tablets.

Cactus mucilage has been used to prepare a edible coating in pharmaceutical formulation

Table No 2: Pharmaceutical applications or uses of natural gums and mucilages.

Sr. No Common name Botanical name Pharmaceutical Applications

1. Abelmoschus mucilage

Abelmoschus esculentus Sustained release

2. Agar Gelidium amansii Suspending agent, emulsifying agent, gelling agent in suppositories, surgical lubricant, laxative.

3. Aloe mucilage Aloe species Gelling agent, sustained release agent

4. Asario mucilage Lepidum sativum Suspending agent, emulsifying agent, controlled release tablet.

5. Bavchi mucilage Ocimum canum Suspending agent, emulsifying agent

6. Carrageenan Chondrus cryspus Gelling agent, stabilizer in emulsions and suspensions, demulcent and laxative

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7. Cashew gum Anacardium occidentale Suspending agent

8. Fenugreek mucilage

Trigonella foenum graecum

Gelling agent, tablet binder, sustaining agent, emollient and demulcent

9. Guar gum Cyamompsis tetraganolobus

Binder, disintegrant, thickening agent, emulsifier, sustained release agent

10. Gum tragacanth Astragalus gummifer Suspending agent, emulsifying agent, demulcent, emollient in cosmetics.

11. Gum ghatti Anogeissus latifolia emulsifier, suspending agent

12. Hibiscus mucilage Hibiscus esculentus Linn

Emulsifying agent, sustained release agent, suspending agent

13. Hibiscus mucilage Hibiscus rosasinensis Linn Suspending agent, Sustained release agent

12. Ispagol mucilage Plantago psyllium, Plantago ovata

Cathartic, lubricant, demulcent, laxative, sustaining agent, binder, emulsifying and suspending agent

13 Karaya gum Sterculia urens Suspending agent, emulsifying agent, dental adhesive, sustaining agent in tablets, bulk laxative

14. Ocimum seed Mucilage

Ocimum gratissimum Suspending agent, binding agent

15 Satavari mucilage Asparagus racemosus Binding agent and sustaining agent in tablet

16 Leucaena seed gum

Leucaena leucocephata

Emulsifying agent, suspending agent, binder in tablets, disintegrating agent in tablets

17. Xanthan gum Xanthomonas lempestris

Suspending agent, emulsifier, stabilizer in toothpaste and ointments.

18. Gellan gum Pseudomonas elodea Disintegrating agent, Modifications Methods for Polysaccharides

There are various methods for modifying the structures of polysaccharides. The introduction

of hydrophobic, acidic, basic, or other functionality into polysaccharide structures can alter

the properties of materials based on these substances.

1) Physical methods

2) Chemical Methods

1) Physical Modification of Polysaccharides

a) Physical Cross linking

In physical crosslinking, polysaccharides forms crosslinked network with counterion at the

surface. High counterion concentration would require longer exposure times to achieve

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complete crosslinking of the polysaccharides. For physical crosslinking different methods

have been investigated.

i) Cross linking by ionic interaction

ii) Cross linking by Crystallization

iii) Hydrophobised polysaccharides

b) Microwave modification

Microwaves generate electromagnetic radiation in the frequency range of 300 MHz to 300

GHz. On exposure to microwaves, the polar or charge particles tend to align themselves with

electric field component of the microwaves which reverses its direction e.g. at the rate of 2.4

× 109/s at 2.45 GHz microwave frequency. As the charged or polar particles in a reaction

medium fail to align themselves as fast as the direction of the electric field of microwaves

changes, friction is created, which heated the medium

2) Chemical Modification of Polysaccharides

1. Chemical crosslinking:

Chemical crosslinking of polysaccharide is a versatile method with good mechanical stability.

During crosslinking counterions diffused into the polymeric and crosslinking agent reacts

with polysaccharides forming either intermolecular or intramolecular linkages.

i) Crosslinking by radical polymerization

ii) Crosslinking by aldehyde

iii) Crosslinking by addition reaction

iv) Crosslinking by Condensation reaction [17]

2. Graft copolymerization of polysaccharides

Graft copolymers by definition, consists of a long sequence of one polymer with one or more

branches of another polymer. With the help of preformed polymer (polysaccharide in case of

grafted polysaccharides) the synthesis of graft copolymer process will start. The free radical

sites will create on this preformed polymer with the help of external agent. The agent should

be effective enough to create the required free radical sites, at the same time should not be too

drastic to rupture the structural integrity of the preformed polymer chain. Once the free

radical sites are formed on the polymer backbone, the monomer can get added up through the

chain propagation step, leading to the formation of grafted chains.

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i) Vinyl/acryl graft copolymerization

ii) Chemical initiating system

iii) Radically initiating system [18]

The other methods includes

a) Ester and ether formation using saccharide oxygen nucleophiles, including enzymatic

reactions and aspects of regioselectivity

b) The introduction of heteroatomic nucleophiles into polysaccharide chains;

c) The oxidation of polysaccharides, including oxidative glycol cleavage,

d) Chemical oxidation of primary alcohols to carboxylic acids, and enzymatic oxidation of

primary alcohols to aldehydes;

e) Reactions of uronic-acid-based polysaccharides; nucleophilic reactions of the amines of

chitosan; and the formation of unsaturated polysaccharide derivatives. [19]

Many studies have been carried out in fields including food technology and pharmaceuticals

using polysaccharides. The Literature reviles that the extensive effort have been made in

pharmaceutical research laboratory for the development of excipient from natural

polysaccharides. The Literature survey also reviles the use of various physical and chemical

methods for modification of polysaccharides for improving its activity. Some of them are, 1.

Basavaraj et al (2011) designed and characterised sustained release aceclofenac matrix tablets

containing tamarind seed polysaccharide. They extracted tamarind seed polysaccharide (TSP)

from tamarind kernel powder and utilized it in the formulation of matrix tablets containing

Aceclofenac by wet granulation technique and evaluated for its drug release characteristics.

Granules were prepared and evaluated for loose bulk density, tapped bulk density,

compressibility index and angle of repose, shows satisfactory results. Formulation was

optimized on the basis of acceptable tablet properties (hardness, friability, drug content and

weight variations), in vitro drug release and stability studies. All the formulations showed

compliance with pharmacopieal standards. The in vitro release study of matrix tablets were

carried out in phosphate buffer pH 7.4 for 12 hr. Among the formulations, they observed that

F5 shows 98.062% better controlled release at the end of 12 hr. The results indicated that a

decrease in release kinetics of the drug was observed by increasing the polymer

concentration. The drug release of optimized formulations F-5 follows zero order kinetics and

the mechanism was found to be diffusion coupled with erosion (non-Fickian

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diffusion/anomalous). The stability studies were carried out according to ICH guideline

which indicates that the selected formulations were stable. [1]

2. Tushar Deshmukh et al (2011) evaluated the gum obtained from of Butea monosperma as a

tablet binder employing ibuprofen as a model drug. The gum was isolated from bark of Butea

monosperma Lam. Physicochemical characteristics of gum were studied. Different

formulations of tablets using Butea monosperma gum were prepared by wet granulation

method. The binder concentrations in the present tablet were 2, 4, 6, 8, 10 and 12% w/v.

Tablets were prepared and subjected for evaluation of hardness, friability, drug content

uniformity. Preliminary evaluation of granules showed that, 1.75 to 2.06 granule % friability,

30.11 to 33.82º angles of repose and 4.146 to 6.512 compressibility index %. Tablet hardness

was found to be in the range of 2.52 to 4.86 kg/cm2, 155 to 267 sec disintegration time and

more than 90.00% dissolution in 105 min. From their study, it can be concluded that B.

monosperma gum at 8% w/v exhibited good binding properties comparable to that of 10%

starch. Gum can be used as a binding agent for the preparation of tablets. [11]

3. Sandhya P et al (2010), in their work evaluated mucilages obtained from Malva sylvestris

and Pedalium murex as Suspending Agent. The purpose of their study was to search for a

cheap and effective natural excipient that can be used as an effective alternative for the

formulation of pharmaceutical suspensions. The suspending properties of Malva sylvestris

and Pedalium murex mucilage were evaluated comparatively with Acacia at concentrations

of 0.5, 1, 1.5, and 2% w/v in calcium carbonate suspension. Characterization tests were

carried out on purified Malva sylvestris and Pedalium murex mucilage. From the parameters

of sedimentation volume, flow rate, redispersibility abilities, it was observed that suspension

prepared using Pedalium murex mucilage showed better suspendability of all the materials

investigated followed by the suspension prepared using Malva sylvestris. They concluded that

the extracted mucilage from fruits of Pedalium murex and Malva sylvestris has the potential

of a suspending agent even at low concentration and can be used as a pharmaceutical

adjuvant. [14]

4. Olubunmi Olayemi et al., 2011 evaluated Brachystegia eurycoma seed mucilage for use as

a tablet binder in metronidazole formulations in comparison with gelatin. The granules were

formulated by the wet granulation method using the extracted mucilage and gelatin as binder

at 1, 2, 4, 6%w/w concentrations. The granules were found to possess good flow property as

indicated by the angle of repose, Hausner’s ratio and Carr’s index. The formulated tablets

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were evaluated for uniformity of weight, thickness, tablet hardness, friability, disintegration

times, drug assay and dissolution profile. Generally, the tablets formulated from Brachystegia

eurycoma seed mucilage were softer than those of gelatin, had good uniformity of weight and

disintegrated within the official specified times for uncoated tablets. They indicate the

efficacy of Brachystegia eurycoma seed mucilage as a binder where fast release of a drug is

desired. [26]

5. A. S. Mann, et al., 2007 evaluated the suspending properties of Cassia tora (family

Leguminosae) comparatively with those of compound tragacanth, Acacia and gelatin at

concentration range of 0.5 – 4.0% w/v in sulphadimidine suspension. Characterization tests

were carried out on purified Cassia tora mucilage. Sedimentation volume (%), rheology and

particle size analysis were employed as evaluation parameters. The values obtained were

used as basis for comparison of the suspending agents studied. They found that Cassia

mucilage is safe for use as a suspending agent in human and pet foods based on the levels of

use, which are comparable to the use levels of other suspending agents.[27]

6. Mahmud, H S., et al., 2008 investigated the Gum exudates from Khaya senegalensis

(Family Meliaceae) plants for its physicochemical properties such as pH, water sorption,

swelling capacity and viscosities at different temperatures using standard methods. The gum

is slightly soluble in water and practically insoluble in ethanol, acetone and chloroform. It

swells to about 10 times its original weight in water. Water sorption studies revealed that it

absorbs water readily and is easily dehydrated in the presence of desiccants. A 5 %w/v

mucilage concentration gave a viscosity value which was unaffected at temperature ranges

(28 – 40 °C). They found that the swelling ability of Khaya senegalensis gum provides

potentials for its use as a disintegrant in tablet formulation, as a hydro gel in modified release

dosage forms. [6]

7. R. Deveswaran, et al., 2009, studied disintegrant property of mucilage and seed powder of

Isapghula by formulating dispersible tablets of famotidine. Hardness of the tablets was found

to be in the range of 4.0 kg/cm2 for all formulations. The wetting time decreased with the

increase in concentration of seed and mucilage powder. The tablets showed 96.1-99.3% of

the labeled amount of drug, indicating uniformity in drug content. The mucilage powder was

found to have better disintegrating property compared to the seed powder. All the

formulations were found to be within the acceptable limits of official weight variation test

and they exhibited good friability.[12]

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8. Ravi Kumar et al, 2009 investigated the Polysaccharide mucilage, derived from the seeds

of fenugreek, Trigonella foenum-graceum L (family Leguminosae), as disintegrant for use in

mouth dissolving tablet formulations containing metformin hydrochloride. Mucilage

extracted from fenugreek seeds were subjected to toxicity studies, it showed that extracted

mucilage was devoid of toxicity. Fast disintegrating tablet (FDT) of metformin HCl was

formulated using different concentration (2, 4, 6 8 and 10% w/w) of natural disintegrant viz;

isolated mucilage of fenugreek seed and synthetic superdisintegrants like croscarmellose

sodium and were compared. Disintegration time and drug release were taken as the basis to

optimize the rapidly disintegrating tablet. Prepared tablets were evaluated for thickness,

hardness, friability, uniformity of weight, disintegration time, wetting time and dissolution

study. The formulated tablets had good appearance and better drug release properties as

compared to the marketed conventional tablets. Fenugreek mucilage in the concentration of 4

% gives shorter disintegration in 15 sec. and shows 100% drug release within 18 min. is

selected as the optimized formulation (F2). They revealed that fenugreek mucilage showed

better disintegrating property than the most widely used synthetic superdisintegrants like Ac-

di-sol in the formulations of FDTs. Studies indicated that the extracted mucilage is a good

pharmaceutical adjuvant, specifically a disintegrating agent.[18]

9. Phani Kumar G. K et al, 2011, developed sustained release matrix tablets of Lornoxicam

for maintaining therapeutic blood or tissue levels of the drug for extended period of time with

minimized local or systemic adverse effects. Tamarind Seed Polysaccharide (TSP) as a

natural binder and it is source obtained from Tamarindus indica .The tablets were formulated

by wet granulation method by using 10%, 20%, 30%, and 40% Tamarind Seed

Polysaccharide (TSP) as a natural binding agent and its optimized batch was compared with

maximum ratio of various binders (HPMC K4M, Sodium CMC, Guar Gum). Tablets with

highest binder concentration showed maximum hardness (8.0 kg/cm2) and minimum

friability (0.25%). After 24 hours tablets with 20% TSP binder showed maximum drug

release (99.45%) and tablets with 40% TSP binder showed minimum drug release (62.55%).

With increasing the percentage of natural polymer (TSP), release rate decreased, though drug

release pattern was mainly dependent on the type of polymer. Among all the formulations,

formulation LT - 2 which contain 20% TSP binder release the drug which follows Zero order

kinetics via, swelling, diffusion and erosion. The FTIR study revealed that there was no

chemical interaction between drug and excipients.[15]

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10. Anuradha Mishra and Sunita Pal (2007) carried out the synthesis and characterization of

polysaccharide-based material Okra mucilage. A water-soluble food grade polysaccharide

was grafted with polyacrylonitrile (PAN) using ceric ammonium nitrate/nitric acid redox

initiator for modifying their properties for potential industrial applications. Ceric ion initiated

solution polymerization under N2 atmosphere was found to be an efficient method for the

formation of graft copolymers. The effect of variables such as the monomer concentration,

initiator concentration, reaction time and temperature on the grafting efficiency (%GE) and

percent grafting (PG) was discussed. Evidence of grafting was provided by the

characterization of Okra mucilage and its graft copolymers by Fourier transform infrared

spectroscopy (FTIR), scanning electron microscope (SEM), differential scanning calorimetry

(DSC) and X-ray diffraction (XRD) patterns. Grafting of polyacrylonitrile onto Okra

mucilage, a polysaccharide of vegetable origin, offers a new polymeric material with

properties that can be exploited industrially. They concluded that grafting only improves the

properties of mucilage by introducing more reactive sites and without making any change in

the molecular mobility of chelating groups of polysaccharide. [22]

11. Ramana Murthy et al (2002), Evaluated modified gum karaya as carrier for the

dissolution enhancement of poorly water-soluble drug Nimodipine. The advantages of MGK

over the parent gum karaya (GK) were illustrated by differences in the in vitro dissolution

profiles of respective solid mixtures prepared by co-grinding technique. The influence of

process variable, such as polysaccharide concentration and method of preparation of solid

mixture on dissolution rate was studied. They performed solubility studies to explain the

differences in dissolution rate. Solid mixtures were characterized by differential scanning

calorimetry (DSC), X-ray diffraction studies (XRD) and scanning electron microscopy

(SEM). The dissolution rate of NM was increased as the MGK concentration increased and

optimum ratio was found to be 1:9 w/w ratio (NM: MGK). From the study they found that

method of preparation of solid mixtures was significantly effected the dissolution rate of NM

from solid mixtures. The order of method of preparation in according to their Dissolution

Efficiency was physical mixture_co-grinding mixture_swollen carrier mixture_kneading

mixture (water as kneading agent)_kneading mixture (70% v/v ethanol as kneading

agent)_solid dispersion. Though, the solid mixtures prepared by other methods like solid

dispersion, swollen carrier mixture and kneading technique gav faster release, co-grinding

mixture prepared in 1:9 w/w ratio (NM:MGK) was found to exhibit a significant

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improvement in dissolution rate without requiring addition of organic solvents or high

temperatures for its preparation and the process is less cumbersome.[23]

12. Sutar P.B et al (2008) crosslinked polyacrylamide grafted pectin with varying amount of

glutaraldehyde and they observed that the cross-linked product showed better film forming

property and gelling property than pectin. The pH dependent release of salicylic acid was

observed due to pH dependent swelling of the crosslinked hydrogel. [24]

13. Gurpreet Kaur et al evaluated the possible use of inter polymer complexed (IPC) films of

chitosan (CH) and carboxymethyl tamarind kernel powder (CMTKP) for colon release of

budesonide. They found that the results strongly indicate versatility of CH-CMTKP IPC films

to deliver budesonide in the colon. [25]

CONCLUSION In the present review different works on natural polysaccharides were studied in terms of

their use as excipients in various formulations. Gums and mucilages are widely used natural

materials for conventional and novel dosage forms. These natural materials have advantages over

synthetic ones since they are chemically inert, nontoxic, less expensive, biodegradable and widely

available. Recently, much attention has been paid to the modification of natural

polysaccharides in order to obtain novel hybrid materials. These modified polysaccharides

could be applied in the design of various stimuli-responsive controlled release systems such

as transdermal films, buccal tablets, matrix tablets, microsphers/hydrogel bead system and

nanoparticulate system. This contribution is intended to develop other natural sources as well as

with modifying existing natural materials for the formulation of novel drug delivery systems,

biotechnological applications and other delivery systems.

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