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Abstract— Herbal drugs are becoming more popular in the
modern world for their application to cure variety of disease with less toxic effects and better therapeutic effect. In recent years, Nanoparticles have been used as potential drug delivery system because of their ability to circulate for a prolonged period of time. The present study is to prepare embelin- chitosan nanoparticle which helps to extend the release so as to reduce the adverse effects. Nanoparticles of the embelin from Embelia ribes were prepared by emulsification cross linking method using chitosan, cross linked with glutaraldehyde. The yield of the dried mass was calculated gravimetrically and the size, morphology of the prepared nanoparticle were examined by scanning electron microscopy analysis.
Keywords— Chitosan, Embelin, Herbal Drugs, Nanotechnology
I. INTRODUCTION RADITIONAL medicines all over the world have advocated the use of herbs to treat diabetes since time
immemorial. Plant drugs are frequently considered to be less toxic and more free from side effects than synthetic ones [1] - [2]. There has been increasing demand for the use of plant products with different pharmacological activity due to low cost, easy availability and lesser side effects. Therefore plant materials are continuously scrutinized and explored for their pharmacological effects. Plant derived medicines are widely used because they are easily available and cheaper.
Embelia ribes is widely used in Indian traditional medicines for various biological activity. Embelin was isolated from Embelia ribes berries and it belongs to the family myrsinaceae. One of the major attractions among researchers towards quinone compounds is their color and biological activities[3]. Among all quinones, benzoquinone and its analogues are most widely used to elicit pharmacological action. Embelin is a natural benzoquinone (2, 5-dihydroxy-3-undecyl-p-benzoquinone), found to be the active principle of
Gnanamani Arumugam is with the Central Leather Research Institute, Adyar, Chennai, Tamilnadu, South India (phone:91-44-24430736;fax:91-44-24911589;email: [email protected])
Chitra Krishnan is with Faculty of Pharmacy, Sri Ramachandra University, Porur,Chennai, Tamilnadu Tamilnadu, South India (email: [email protected])
Mary Babu was with the Central Leather Research Institute, Adyar, Chennai, Tamilnadu, South India (email: [email protected] )
Saba Maanvizhi is with Faculty of Pharmacy, Sri Ramachandra University, Porur, Chennai, Tamilnadu, South India (email: [email protected])
Embelia ribes and reported to possess a wide spectrum of biological activities [4]-[5].
The efficacy of many drugs is often limited by their potential to reach the site of action. In most cases, only a small amount of administered doses reaches the target site, therefore developing a drug delivery system that optimizes the pharmaceutical action of a drug while reducing its toxic side effects is a challenging task. Moreover particulate drug delivery system offer a number of advantages over conventional dosage form. The carrier must be biodegradable, non toxic and stable. One approach is the use of polymeric nanoparticles that can provide targeted drug delivery combined with optimal drug release profile [6]. The present study is to prepare embelin nanoparticles to extend the release so as to reduce the adverse effects using chitosan. Chitosan is a modified natural carbohydrate polymer prepared by partial N- deacetylation of chitin, a natural biopolymer. It is widely used in a variety of pharmaceutical applications because it has a low level of toxicity, physicochemical stability, biodegradability and biocompatibility. Moreover chitosan is lack of irritant and allergic effects [7].
II. MATERIALS AND METHODS Embelin was isolated from Embelia ribes berries. All other
chemicals used were of analytical grade. Magnetic stirrer, Centrifuge, UV spectrophotometer and SEM were the equipment used for the study.
A. Preparation Of Sphere: Emulsification cross linking method is exhaustively used
for the encapsulation of drugs and the same is followed for embelin encapsulation. 0.5 g of chitosan was added to a beaker containing water in a 250ml and is kept for stirring on a magnetic stirrer. Acetic acid was added into the beaker for facilitating the solubilization of chitosan. 0.5 g of embelin was dissolved in DMSO and it was added slowly to the above mixture. 100 ml of sunflower oil was warmed at 60 ̊C for 10min. At room temperature, the warmed oil was added dropwise into the chitosan solution with continuous stirring under an overhead mechanical stirrer. Simultaneously 10 ml of Span 80 was added into the emulsifying mixture. This mixture was homogenized continuously for 4 hours. Then 300 µl of glutaraldehyde was added dropwise into the mixture and kept at stirring overnight at room temperature on a magnetic stirrer .Then the mixture was centrifuged (16000x g , 30 minutes,15⁰C) to remove the oil and several times the
Preparation and Characterization of Embelin Nanoparticle
Gnanamani Arumugam, Chitra Krishnan, Mary Babu, and Saba Maanvizhi
T
2nd International Conference on Chemical, Environmental and Biological Sciences (ICCEBS'2013) March 17-18, 2013 Dubai (UAE)
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sediments was washed with ice cold acetone until it is free from oil globules. The spheres collected were freeze dried, weighed and stored.
B. Characterization Of The Sphere: Percentage Yield: The freeze dried spheres were collected and weighed.
production yield of the dried sphere was calculated gravimetrically.
Percentage Yield (%) = NPs weight / total solids weight (Chitosan +Drug) x100 Drug Entrapment Efficiency:
Weighed quantity of sphere is suspended in DMSO to extract the drug from the sphere. After 24 hours of time, the solution was filtered. Then it was analysed spectrophotometrically at 289nm against DMSO as blank.
Entrapment Efficiency = Actual drug content / theoretical drug content x 100 Swelling Property [8]-[9]:
The swelling of the polymers can be measured by their ability to absorb water and swell. The swelling ability of the spheres in water and physiological media was determined by allowing them to swell to their equilibrium. Accurately weighed amount of spheres (50 mg) were placed on water and simulated gastric and intestinal fluids of pH 1.2 and 7.4 respectively in a glass vial with occasional shaking for 3 hours. The temperature of medium should be maintained at 37±0.5 ◦C throughout the study. After a selected time intervals, the spheres should be withdrawn, blotted to remove excess water and weighed .Change in weight was noted for 3 hours with an interval of 30 minutes. The following formula was used for calculation of degree of swelling.
α = (Ws – Wo) / Ws . . . . . . . . . . . . . . . . . Where, α = Degree of swelling, Wo=Initial weight of
microspheres and Ws = Weight of microspheres after swelling. In vitro drug release:
This study was carried out in USP dissolution test apparatus using phosphate buffer pH 7.4 as dissolution media. Sample was loaded in empty capsule and then suspended in dissolution media. Temperature of the media was kept at 37 ± 2 °C and the rpm was at 50. Samples were filtered, diluted and assayed at each interval for embelin content released at λ max of 289 nm using double beam UV‐ spectrophotometer by keeping phosphate buffer pH 7.4 as blank. Overall three trials were carried out. From this percentage drug release was calculated. Morphological Examination:
Morphological examination of the surface and internal structure of the sphere was carried out using a scanning electron microscope (model Maxim 2000S, CamScan Analytical, UK) at the accelerating voltage of 12 kV. The samples for the SEM analysis were prepared by sprinkling the spheres on one side of a adhesive stub. Then the spheres were coated with gold before microscopy. Then the nanoparticles
size and shape were characterized and photographed. Fig. 1 and 2 depicts the image of empty and drug loaded spheres.
III. CONCLUSION Recently, pharmaceutical scientists have shifted their focus
to designing a drug delivery system for herbal medicines using a scientific approach. Embelin nanoparticle were prepared by emulsification cross linking method. The prepared spheres were subjected to SEM for determining its size and shape.The prepared spheres were free flowing and spherical in shape. The yield was found to be 92% and entrapment efficiency was around 91.5%. The swelling behaviour of the beads at different time intervals was monitored in water and also in solution of pH 1.2 and pH 7.4. Swelling properties of empty sphere was 5 times more than drug loaded sphere. The release was found to be good and sustainable till 6 hours.
ACKNOWLEDGMENT The work was supported by a young faculty research grant
from Sri Ramachandra University and likes to thank SRU management and also CLRI for helping us to carry out this work.
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[3] Nohl H, Jordan W, Youngman RJ, "Quinones in biology: Functions in electron transfer and oxygen activation", Advances in Free Radical Biology and Medicine, vol.2,no.1,pp. 211–279, 1986.
[4] N.Radhakrishnan, Gnanamani A, Mandal AB, “A potential antibacterial agent, Embelin - a natural benzoquinone extracted from Embelia ribes”, Biology and Medicine, vol. 3,no,2,pp.1-7,2011.
[5] N. Radhakrishnan, V. Kavitha, STK. Raja, A. Gnanamani, A.B. Mandal, “Embelin- A natural potential cosmetic agent”, Journal of Applied Cosmetology, vol.29,no.2,pp. 99-107, 2011.
[6] Waree Tiyaboonchai,”Chitosan Nanoparticles: A promising system for drug delivery”,Naresuan University Jn. ,vol.11,no.3,pp.51-66,2003.
[7] Dodane V,Vilivalam VD,”Pharmaceutical applications of chitosan”, PSTT ,vol.1,no.16,pp.246-253,1998.
[8] H. Omidian, K. Park ,”Swelling agents and devices in oral drug delivery”,J. Drug Del. Sci. Tech. ,vol. 18,no.2,pp. 83-93,2008.
[9] Santosh Shep, Sham Dodiya, Sandeep Lahoti, Rahul Mayee,”Swelling System: A Novel Approach Towards Gastroretentive Drug Delivery System”,,Indo-Global Journal of Pharmaceutical Sciences, vol.1,no.3,pp. 234-242,2011
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Fig. 1 Photograph of empty sphere
Fig. 2 Photograph of herbal drug loaded sphere
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