tsp polymer

Tam arind Seed polysaccharide: A s novel excip ient

D epartm ent of Pharm aceutics, SN IO P , Pusad 1

Tamarind Seed Polysaccharide: As novel excipient

Abstract-

The natural polymers always have exceptional properties which make them

distinct from the synthetic polymers and tamarind seed polysaccharide (TSP) is one such example which shows more valuable properties making it a useful excipient for a wide range of applications. TSP is a natural polysaccharide obtained from the seeds of Tamarindus indica, recently gaining a wide potential in the field of pharmaceutical and cosmetic industries. Its isolation and

characterisation involve simple techniques resulting in costeffective yield in its

production. TSP shows uniqueness in its high drug holding capacity, high swelling index and high thermal stability, especially necessary for various novel drug delivery systems. It also plays the role of stabiliser, thickener, binder, release retardant, modifier, suspending agent, viscosity enhancer, emulsifying agent, as a carrier for novel drug delivery systems in oral, buccal, colon, ocular systems, nanofabrication, wound dressing and is also becoming an important part

of food, cosmetics, confectionery and bakery. Various studies and experiments

have been carried out to prove its multifunctional potentiality, from which it can

be concluded that TSP can be a promising natural polysaccharide having enormous applications. This review focuses on the diversity of applications of TSP.

Key words: Drug delivery, excipient, pharmaceutical, sustained release polymer, tamarind seed polysaccharide



Introduction:

Introduction of matrix tablet as sustained release (SR) has given a new breakthrough for novel drug delivery system (NDDS) in the field of Pharmaceutical technology. It excludes complex production procedures such as coating and pelletization during manufacturing and drug release rate from the dosage form is controlled mainly by the type and proportion of polymer used in the preparations. Hydrophilic polymer matrix is widely used for formulating an Sustained Release dosage form.1 The use of natural polymer and their semisynthetic derivatives in drug delivery continues to be an area of active research. Drug-release retarding polymers are the key perform in matrix systems. Various polymers have been investigated as drug retarding agents , each presenting a different approach to the matrix system. Based on the futures of the retarding polymer, matrix systems are usually classified into three main groups: hydrophilic, hydrophobic and plastic. Hydrophilic polymers are the most suitable for retarding drug release and there is growing interest in using this polymers in sustained drug delivery.2 Hydrophilic matrices are an interesting option when developing an oral sustained release formulation. The drug release from such matrices can be controlled through their physical properties. Polysaccharides are

the choice of materials among the hydrophilic polymers used, because they are nontoxic and acceptable by the regulating authorities. Tamarind seed polysaccharide (TSP) obtained from the seed kernel of Tamarindus indica, possesses properties like high viscosity, broad pH tolerance, non-carcinogenicity, muco-adhesive nature, and biocompatibility. It is used as stabilizer, thickener, gelling agent, and binder in food and pharmaceutical industries. The tamarind

seed polysaccharide constitutes about 65% of the tamarind seed components.3

The main component of Tamarindus indica seed has been found as a non-ionic, neutral, branched polysaccharide which consists of a cellulose-like

backbone that carries xylose and galactoxylose substituents.4

Need of natural polymer:5,6



1. Biodegradable: naturally ocuring polymers produced by all living oraganisms. They show no adverse effect on the environment or human being.

2. Biocompatible and non-toxic: chemically, nearly all of these plant materials are carbohydrates in nature and composed of repeating monosaccharide units. Hence they are non-nontoxic.

3. Economic: they are cheaper and there production cost is less than synthetic materials.

4. Safe and devoid of side effects: they are from natural sources and hence, safe and without side effect.

5. Easy availability: in many countries, they are produced due to there applications in many industries.

Disadvantages of natural polymers:

1. Microbial contamination: during production, they are exposed to external environment and hence, there are chances of microbial contamination.5,6

2. Batch to batch variation: synthetic manufacturing is controlled procedure with fixed quantities of ingredients while production of natural

polymers is dependent on environment and various physical factors.5 3. The uncontrolled rate of hydration: due to differences in the collection

of natural materials at different times, as well as differences in region, species and climate conditions. The percentage of chemical constituents present in a given materials may vary.5,6

4. Slow process: as the production rate depents on the environment and many other factors, it cant be changed. So natural polymers have slow rate of production.6,7

5. Heavy metal contamination: there are chances of heavy metal

contamination often associated with herbal excipients.6,7

D epartm ent of P harm aceutics

Structure and composition

Figure 01: tamarind seed polysaccharide.

TSP contains monomers of glucose, galactose and xylose sugars molar ratio of 3:1:2, which constitutes about 65% of the seed components. Various studies identified it as a non

highly branched polysaccharide consisting of a cellulose

carries xylose and galactoxylose substitution at the glucan chain (nearly 80%),chemical residues similar to those of membrane spanning mucin

basis analysis, the major compositions of TSP are72.2), Protein (15.422.7

Isolation of tamarind seed polysaccharide:

Method 1:

Tam arind Seed polysaccharide: A s novel excipient

D epartm ent of Pharm aceutics, SN IO P , Pusad

and composition of tamarind seed polysaccharide:

Figure 01: tamarind seed polysaccharide.

TSP contains monomers of glucose, galactose and xylose sugars molar ratio of 3:1:2, which constitutes about 65% of the seed components. Various studies identified it as a nonionic, neutral, hydrophilic, mucoadhesive,

highly branched polysaccharide consisting of a celluloselike backbone that

ose and galactoxylose substitution at the glucan chain (nearly 80%),chemical residues similar to those of membrane spanning mucin. As per

basis analysis, the major compositions of TSP are Nonfibre carbohydrate (22.7), Oil (3.97.4), Crude fibre (0.78.2), Ash (

Isolation of tamarind seed polysaccharide:9,10


4

of tamarind seed polysaccharide:

TSP contains monomers of glucose, galactose and xylose sugars present in a molar ratio of 3:1:2, which constitutes about 65% of the seed components.

ionic, neutral, hydrophilic, mucoadhesive,

like backbone that

ose and galactoxylose substitution at the glucan chain (nearly 80%), As per the dry

fibre carbohydrate (65.1(2.453.3).8



200 g of tamarind seeds must be soaked in double distilled water and boiled for 5 h to remove the outer dark layer. After removing the outer dark layer, sufficient amount of double distilled water should be added to the inner white portion and

boiled with constant stirring in order to obtain the slurry. Now cool the resultant solution in refrigerator so that most of the un-dissolved portion settles down. The supernatant liquid can be separated out by simple decantation or best by centrifugation at 500 rpm for 20 min. After this, the solution is to be concentrated on a water bath at 60C to reduce the volume to one-third of its initial volume. Now the solution is to be cooled and poured into 3 volumes of acetone by continuous stirring. Precipitates obtained must be washed with

acetone and dried in vacuum at 50-60C.

Method 2:

Tamarind seeds must be collected and dried in sunlight. The kernels should be crushed into fine powder. 20 g of fine kernel powder is to be added to 200 ml of cold distilled water to prepare slurry. The slurry obtained must be poured into 800 ml of boiling distilled water and boiled for 20 min on a water bath to obtain a clear solution which must be kept aside overnight. The thin clear solution was then centrifuged at 5000 rpm for 20 min to separate all the foreign matter. Supernatant liquid was separated and poured into excess of absolute alcohol with continuous stirring. Precipitates obtained were collected by a suitable method

and washed with 200 ml of absolute ethanol and dried at 50C for 10 h. Store the polymer obtained in a dessicator.

Properties of tamarind seed polysaccharide:

TSP is insoluble in organic solvents such as ethanol, methanol, acetone, ether and in cold water, but it gets dissolved completely in hot water at temperatures

above 85C, yielding a highly viscous colloidal solution or a mucilaginous gel showing typical nonNewtonian rheologic behaviour and pseudoplastic

properties. TSP possesses various properties like high viscosity, adhesivity,



noncarcinogenicity, broad pH tolerance and biocompatibility. It is also found to

be a potential emulsifier, nontoxic and nonirritant with haemostatic activity.

Figure 02: tamarind seed and powder

Other distinguishable properties of TSP have also been identified, which include the high drug holding capacity, high swelling index and high thermal stability, making it a suitable excipient for drug delivery system. Apart from this, it is an excellent viscosity enhancer showing mucomimetic, mucoadhesive and bioadhesive activities. Recent studies on TSP for various drug formulations revealed other unique properties with wide applications in the pharmaceutical area, which include its potent antidiabetic activity that reduces blood sugar

level.11

Pharmaceutical application of tamarind seed polysaccharides: 8, 12

Matrix Oral Drug Release Modifiers:

Polysaccharides exhibit a wide choice among the hydrophilic polymers for use as release retardants, since they are nontoxic and most acceptable by the regulating authorities. Matrix tablets are used to make sustained release or controlled release formulations for which they require release modifiers, and according to the need, the release modifiers used are release retardants. Hence, the use of TSP



as a matrix material becomes a promising excipient for oral matrix tablets as it

acts as a release retardant.

Binder in tablet dosage form:

Evaluations of tamarind seed polysaccharide as a binder for tablet dosage forms was taken up for the weight granulation as well as direct compression methods. The results indicated that tamarind seed polysaccharide could be used as binder

for weight granulation and direct compression tabletting methods.

Colon targeting:

The potential use of TSP as a carrier for colonic drug delivery was demonstrated. They prepared matrix tablets by wet granulation methods using ibuprofen as a model drug. In vitro release studies mimicking mouth to colon transit demonstrated the ability of TSP to release the drug at pH 6.8. TSP was remarkably degraded in rat indicating that TSP can be used as a carrier for

colonic drug delivery.

Ocular targeting:

TSP is an adhesive enabling it to stick to the surface of eye longer than other eye preparations. TSP possesses mucomimetic, mucoadhesive, and pseudo plastic properties. Furthermore, the TSP drops did significantly better job of relieving several key subjective symptoms of dry eye syndrome namely trouble blinking, ocular burning, and having sensation of having something in someone eye. It also increases the resident time of the drug to the cornea, e.g. -blockers. The effect of an ophthalmic preparation containing timolol and TSP on intra-ocular

pressure was evaluated in rabbits and found to decrease.

Bioadhesive tablet:

Tablets prepared from the TSP and tamarind gum were evaluated as bioadhesive tablets and was found that the tablets showed longest residence time in oral



cavity as compared to that prepared from xanthan gum and carboxycellulose but

the unpleasant taste of the former gradually developed.

S. No

Dosage form Applications Comments

1 Verapamil HCL As a drug release retardant

TSP can be used as sustained release component

2 Terbutaline sulphate Tablet

As a binder for tablet prepared by wet granulation and direct compression methods

It can be used as binder as well as a polymer for sustained release formulations of low drug loading

3 Diclofenac sodium Spheroids

Polysaccharide hydrogel was used as release modifier

Formulation follows zero order release pattern over 8 hrs with improved bioavailability.

4 Tablet (water soluble & water insoluble drugs)

As a carrier polysaccharide

Anomalous release of water soluble drugs, Zero order drug release for water insoluble drugs

5 Caffeine tablet As a carrier polysaccharide

Anomalous drug release

6 Nifedipine mucoadhesive tablet

As a mucoadhesive and sustained release component

More comfortable to the user to do less erosion, faster hydration rate, and optimum pH of surrounding medium

7 Metronidazole Mucoadhesive buccal Patches

As a mucoadhesive and sustained release component

TSP might be well utilized to develop a buccal drug delivery system with required mucoadhesive strength.

8 Ketoprofen Diclofenac sodium

Assess the release behaviour of drugs, from cross linked tamarind seed polysaccharide

This study confirmed that the crosslinked TSP can be used as an effective release retardant and can be successfully used in commercial products.

Table.1: applications of TSP



Suspending and Emulsifying Agent in Liquid Orals:

Attempts made to study the use of TSP as a suspending agent in the formulation of nimesulide suspension showed that TSP acts as a stable suspending agent that reduced the rate of settling and permitted in the easy redispersion of any settled particulate matter. The comparative studies on castor oil emulsions with TSP and gum acacia have shown that 2% w/v of TSP was more effective than using 10% w/v of gum acacia. TSP was also compared with other natural suspending agents

using a pharmaceutical formulation of paracetamol suspension.

Novel Controlled Release Modifiers:

The polysaccharide isolated from the seeds of tamarind was identified to have hydrogel property, and hence can be used as a release modifier in various formulations. Diclofenac sodium spheroids were prepared with TSP using extrusion spheronisation technique. The process was studied on the effect of variables to achieve spheroids with satisfactory particle shape, size and

sizedistribution, and further characterised for surface morphology, qualitative

surface porosity, friability, bulk density and flow properties. The results were found to be significant and gave evidence for its use as a release modifier, as spheroids showed a good correlation between in vitro dissolution profile, viscosity, the swelling index and surface roughness of the polysaccharide. These

spheroids also showed drug release over 8 h.



Literature review: Rishabha Malviya et al. (2010) Formulation, Evaluation and Comparison

of Sustained Release Matrix Tablets of Diclofenac Sodium Using Natural Polymers as Release Modifier In the this investigation, an attempt was made to formulate sustained release matrix tablets of Diclofenac sodium using gum acacia and tamarind gum as release modifier.and A better sustained drug release (98.7%) was obtained with the matrix tablet of the tamarind gum.13

Bhavin Patel et al.(2009), Evaluation of Tamarind Seed Polysaccharide (TSP) as a Mucoadhesive and sustained release component of nifedipine mucoadhesive tablet & Comparison with HPMC and Na CMC The aim of this study was to evaluate TSP as a mucoadhesive, sustained release polymer and to develop bioadhesive drug delivery for nifedipine with prolonged effect, the TSP is compared with Na CMC in respect of drug release and bioadhesive strength but TSP is better than Na CMC because the erosion of tablets containing Na CMC is more and hence it wont be good feeling for patient in mouth.14

R.deveswaran et al.(2009), design and characterization of diclofenac sodium tablets containing tamarind seed polysaccharide as release retardant, the result of this study demonstrated that the TSP can be used as a drug release retardant, because the drug release was extended over a period of 12 hours and the mechanism of drugwas observed to be following zero order release.3

Ashwini Rajendra et al.(2009), Preparation and Evaluation of Extended Release Matrix Tablets of Diltiazem Using Blends of Tamarind Xyloglucan with Gellan gum and Sodium carboxymethyl cellulose, The present study was carried out to evaluate the tamarind xyloglucan for its



matrix forming ability. Matrix tablets of diltiazem hydrochloride prepared with combination of tamarind xyloglucan with gellan gum and sodium CMC were also found to have good physical properties. During this study,

it was also found that drug: polymer concentration ratio influences the drug release behavior.15



CONCLUSION: Natural polymers such as tamarind seed polysaccharide have advantages over synthetic and semi-synthetic polymers like low cost, natural origin, less side effects, locally available and better patient tolerance. Also it have wide range of applications in pharmaceutical industry. So from this review it can be concluded that the tamarind seed polysaccharide is novel excipient in drug delivery.



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