PREPARATION AND EVALUATION OF BIODEGRADABLE ALBUMIN MICROSPHERES OF DICLOFENAC SODIUM

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About Authors:
Renu1*, Shashi Kant2*, Rajendra Yadav3, Amit Kumar Tyagi4
1Faculty of Pharmacy, Shivdan Singh Institute of Technology and Management, Aligarh (U.P)
2Jubilant Chemsys Ltd, Noida,
3Department of Pharmaceutical Sciences, Gurukul Kangri University Haridwar, 
4Department of Chemistry, Meerut College, Meerut (U.P)
*shashi.pharma83@gmail.com

ABSTRACT :
Diclofenac is currently the eighth largest-selling drug and the most frequently used NSAID (Non-steroidal anti-inflammatory drug) in the world, since its introduction in Japan in 1974. Diclofenac is among the better tolerated NSAIDs. Only major adverse effect of Diclofenac is that it causes direct and indirect irritation of the gastrointestinal tract (GIT). To reduce the side effects on gastrointestinal tract (GIT) and to improve therapeutic efficacy of Diclofenac, it can be formulated in polymeric microspheres.
The use of polymeric carriers in formulations of therapeutic drug delivery systems has gained widespread application, due to their advantage of being biodegradable and biocompatible. Among the microparticulate systems, microspheres have a special importance since it is possible to target drugs and provide controlled release. Diclofenac sodium (DS), is a potent drug in the NSAID group having non-steroidal, anti-inflammatory properties, and is widely used in the treatment of rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. In this present study, it was aimed to prepare microsphere formulations of DS using a natural biodegradable polymer as a carrier for administration to extend the duration period of the dosage form. Microsphere formulations of DS which were prepared were evaluated in vitro for particle size, yield value, encapsulation efficiency, surface morphology, and in vitro drug release.

Reference Id: PHARMATUTOR-ART-1413

INTRODUCTION:
Microspheres are the colloidal drug delivery system. Microspheres are characteristically free-flowing powders consisting of proteins/synthetic polymers that are biodegradable in nature and ideally having a particle size less than 200mm. Biodegradable microspheres can be utilized to direct drugs to certain organs through capillary blockade. Its success depends on the size of the microspheres used and on the mode of administration (intravenous/intra-arterial). [1]

Microspheres are reported to possess high specificity and good controlled release properties were exhibited by using biodegradable polymers. [2]

Non-steroidal anti-inflammatory drugs are usually abbreviated as NSAIDs, they reduce Pain, fever and inflammation. During the last few decades, there has been a substantial increase in the number of clinically available NSAIDs in the pharmaceutical market. NSAIDs annually account for 70 million prescriptions and 30 billion over-the-counter (OTC) medications sold in the United States alone. [3]

Diclofenac is a Non-steroidal anti-inflammatory drug (NSAID) which is indicated in relief of signs and symptoms of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and also in relief of migraines, menstrual pain. Diclofenac is used commonly to treat mild to moderate post-operative or post-traumatic pain, particularly when inflammation is also present. [4-6]

Diclofenac is among the better tolerated NSAIDs. The main adverse drug reactions associated with use of Diclofenac relate to direct and indirect irritation of the gastrointestinal tract (GIT).As awareness about this side effects increases so is the increase of research to reduce side effects. To reduce the side effects on gastrointestinal tract (GIT) and to improve therapeutic efficacy of Diclofenac, research is done to formulate Diclofenac in polymeric microspheres and a satisfactory result is found. [7]

 

MATERIALS AND METHODS:
Materials:
Drug: Diclofenac Sodium: Central Drug House New Delhi.
Polymer: Bovine serum albumin: Central Drug House New Delhi.
Chemical: Gluteraldehyde: Central Drug House New Delhi
Toluene : Qualigens Fine Chemical, Mumbai.
Acetone: Qualigens Fine Chemical, Mumbai.
Linseed oil: Qualigens Fine Chemical, Mumbai.

Instruments:
1. Magnetic stirrer: Remi Equipments, 2MLH, and Yamato LT4000.
2. Dissolution apparatus: Electro Lab, TDL- 08 L (USP).
3. U.V. Spectrometer:  Shimajdu Corporation, Japan
4. Microscope: Radical, RM- 3, 20601
5. Oven: Shivaki, T-701

METHODS:
Prepare 2 ml of 25% albumin solution by dissolving 250 mg of serum in purified water. Disperse the drug in the polymer solution. Transfer the aqueous solution into a mixture of 40 ml linseed oil and 10 ml of toluene with continuous stirring at 2400 rpm. Continue stirring for 15 min. observe the particle size distribution under microscope. Add 2ml of gluteraldehyde saturated solution to the albumin solution with continuous stirring for 2 hours. Complete the cross linking process. Wash the suspension of microspheres each with toluene and with acetone. Between each washing discard the supernatant and resuspend the microspheres and at the end of washing with acetone. Suspend the microspheres in 10 ml of acetone and transfer it into a clean petridish.

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