FORMULATION AND CHARACTERIZATION OF MELOXICAM LOADED MICROEMULSION FOR THE TREATMENT OF RHEUMATOID ARTHRITIS

 

ABOUT AUTHOR:
Verma Siddharth
Sri Ram Institute of Technology,
ITI Jabalpur M.P. 482003
luckyverma84@gmail.com

ABSTRACT
Rheumatoid arthritis (RA) is a chronic, systemic inflammatory disorder that may affect many tissues and organs, but principally attacks synovial joints. The process produces an inflammatory response of the synovium (synovitis) secondary to hyperplasia of synovial cells, excess synovial fluid and the development of pannus in the synovium. Various treatments are available. Non-pharmacological treatment includes physical therapy, orthoses, occupational therapy and nutritional therapy. Analgesia (painkillers) and anti-inflammatory drugs including steroids are used to suppress the symptoms, while disease-modifying antirheumatic drugs (DMARDs) are often required to inhibit or halt the underlying immune process and prevent long-term damage. In recent times, the newer group of biologics has increased treatment options.


REFERENCE ID: PHARMATUTOR-ART-1822

1 INTRODUCTION
1.2 Microemulsion

Microemulsions are transparent fine dispersions of oil and water droplets stabilized by surfactant molecules. Microemulsions are macroscopically monophasic, isotropic and possess a flexible interfacial film which is characterized by ultra low interfacial tension values (10-2 mN/m) (Quemada et al.,1985; Bourrel et al., 1988; De Roni et al., 1989).

Due to their unique physicochemical properties, microemulsion offer advantages over traditional topical and transdermal drug delivery formulation. Microemulsion are homogenous, thermodynamically stable dispersion of water and oil stabilized by relatively large amounts of surfactant(s) frequently in combination with cosurfactant(s) (Schmalfuss et al., 1997; Osborne et al., 1991; Trotta et al., 1996; Aboofazeli et al., 1995; Tenjarla, 1999; Friberg, 1990).

Microemulsion show diverse structural organization due to the use of wide range of surfactant concentration, water-oil ratios, temperature etc (Lawrence et al., 2000). In case of emulsion, it contain three components, namely oil, water and surfactant; whereas microemulsions generally require a forth component, a co-surfactants include linear alcohols of medium chain length that miscible with water. The combination of surfactant and cosurfactant promote the generation of extensive interfaces through the spontaneous dispersion of oil in water, or vice-versa. The large interfacial area between the oil and water consists of a mixed interfacial film containing both surfactant and cosurfactant molecules. The interfacial tension at the oil-water interfaces in emulsions approaches zero, which also contributes to their spontaneous formation. Microemulsions are regarded as micelles extensively swollen by large amounts of solubilized oil (Kreuter, 1994; Ruckenstein, 1978).


3. Preformulation Studies
Preformulation investigations are designed to deliver necessary data (especially physicochemical, physicomechanical and biopharmaceutical properties drug substances, excipients and packaging materials), which may influence formulation design and method of manufacture of drug product.

3.1 Identification Test
3.1.1 Physical Appearance

The drug (Meloxicam) was found as a gift sample from Cipla Pvt. Ltd, Indore. The supplied powder of Meloxicam was Yellow or slightly pale yellow, crystalline, powder without odour.

3.1.2 Melting Point
Melting point of Meloxicam was determined by melting point apparatus (Lab-Hosp Corporation, Mumbai) and found to be 243°C.

3.1.3 Solubility Study
The solubility study of Meloxicam was performed in aqueous and organic solvents. Solubility was determined by making saturated solutions. The drug was gradually added till the solutions turned cloudy, indicating the presence of un-dissolved Meloxicam. The solutions were kept at rest for 24 hr to assist the attainment of equilibrium with the un-dissolved drug particles. The supernatants were decanted and filtered through filter paper (Whatman No.1). The filtrates were suitably diluted to measure the concentrations by UV spectrophotometer (Shimadzu 1700, Japan). The results are given in table 3.1.

Table 3.1 Solubility profile of Meloxicam in various solvents

S. no.

Solvents

Solubility

1

Water

Insoluble

2

Methanol

Slightly soluble

3

Ethanol

Slightly soluble

4

Chloroform

Highly Soluble

5

Acetone

Highly Soluble

6

n-Octanol

Highly Soluble

3.1.4    UV Analysis
A 10 mg of drug was dissolved in small quantity of methanol and volume was made up to 100 ml with distilled water. Then 1 ml of this stock solution produced was pipette into a 10 ml volumetric flask and volume made up to the mark with distilled water. The sample was scanned in the range of 200-400 nm using UV/visible spectrophotometer (Shimadzu 1700, Japan) to determine the lmax. The spectra are shown in Fig. 3.1.

Fig. 3.1 UV spectra of Meloxicam

3.1.5    Calibration Curve of Meloxicam in Phosphate Buffer (pH 7.4) 
Meloxicam stock solution was prepared by weighing 10mg of Meloxicam, transferred in to 10ml volumetric flask (previously calibrated) and dissolve it in 4ml of methanol by shaking for 10 min and volume was made up to 10ml with PBS pH 7.4 to get a concentration of 1000μg/ml (solution A). From this solution an aliquot of 1ml was withdrawn and it was diluted to 10ml with PBS pH 7.4 to get a concentration of 100μg/ml (solution-B). From this aliquots of 0.2ml, 0.4ml, 0.6ml, 0.8ml, 1ml, 1.2ml upto 2ml were pipetted out in to a 10 ml volumetric flask (Previously Calibrated) and diluted to 10ml using PBS pH 7.4 to get concentrations of 2 μg/ml, 4 μg/ml, 6 μg/ml, 8 μg/ml, 10 μg/ml, 12 μg/ml upto 20 μg/ml, respectively. Absorbance of this solution was measured at 363nm using UV Spectrophotometer against blank (Methanol + PBS pH 7.4). The result are given in table 3.2 and shown in fig. 3.2.

Table 3.2 Calibration curve of Meloxicam in PBS (pH 7.4) at 363 nm

S. No

Concentration (μg/ml)

Absorbance

1.

2

0.110

2.

4

0.190

3.

6

0.279

4.

8

0.361

5.

10

0.445

6.

12

0.520

7.

14

0.603

8.

16

0.676

9.

18

0.756

10.

20

0.829


Fig. 3.2 Standard curve of Meloxicam in PBS pH 7.4 at 363 nm

3.1.6 Calibration Curve of Meloxicam in Distilled Water        
Meloxicam stock solution was prepared by weighing 10mg of Meloxicam, transferred in to 10ml volumetric flask (previously calibrated) and dissolve it in 4ml of methanol by shaking for 10 min and volume was made up to 10ml with distilled water to get a concentration of 1000μg/ml (solution A). From this solution an aliquot of 1ml was withdrawn and it was diluted to 10ml with distilled water to get a concentration of 100μg/ml (solution-B). From this aliquots of 0.2ml, 0.4ml, 0.6ml, 0.8ml, 1ml, 1.2ml upto 2ml were pipetted out in to a 10 ml volumetric flask (Previously Calibrated) and diluted to 10ml using distilled water to get concentrations of 2 μg/ml, 4 μg/ml, 6 μg/ml, 8 μg/ml, 10 μg/ml, 12 μg/ml upto 20 μg/ml, respectively. Absorbance of this solution was measured at 363nm using UV Spectrophotometer against blank (Methanol + Distilled water). The result are given in table 3.3 and shown in fig. 3.3.

Table 3.3 Calibration curve of Meloxicam in Distilled Water at 363 nm:

S. No.

Concentration (μg/ml)

Absorbance

1.

2

0.105

2.

4

0.200

3.

6

0.307

4.

8

0.411

5.

10

0.512

6.

12

0.602

7.

14

0.704

8.

16

0.803

9.

18

0.908

10.

20

1.19


Fig.3.3: Standard curve of Meloxicam in PBS pH 5.5 at 265 nm

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