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ORIGINAL/BRIEF
Year : 2012  |  Volume : 4  |  Issue : 5  |  Page : 101-103  

Formulation, optimization and evaluation of sustained release microsphere of ketoprofen


Department of Pharmaceutics and Pharmaceutical Technology, S.K. Patel College of Pharmaceutical Education and Research, Ganpat Vidyanagar, Mehsana-Gozaria Highway, Kherva, Gujarat, India

Date of Web Publication21-Mar-2012

Correspondence Address:
V Chirag Prajapati
Department of Pharmaceutics and Pharmaceutical Technology, S.K. Patel College of Pharmaceutical Education and Research, Ganpat Vidyanagar, Mehsana-Gozaria Highway, Kherva, Gujarat
India
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/0975-7406.94156

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   Abstract 

The objective of this study is to formulate ketoprofen loaded microspheres of Acrycoat S100 by an o/w emulsion solvent evaporation method. It potently inhibits the enzyme cyclooxygenase resulting in prostaglandin synthesis inhibition. Ketoprofen causes an irritation in the gastrointestinal mucous membrane and possesses a bitter taste and aftertaste. The half-life in plasma is about 1-2hrs. This makes ketoprofen a very good candidate for the formulation of controlled release dosage forms. Ketoprofen microspheres help to protect the gastric mucous membrane from drug irritation and to mask its taste. The prepared microspheres were evaluated for micromeritic properties, particle size, effect of surfactant concentration, percentage yield, incorporation efficiency, drug polymer compatibility (IR and DSC study), scanning electron microscopy and in vitro drug release. The microspheres produced exhibited good encapsulation efficiencies and micromeritic properties. Encapsulation efficiency of microsphere is around 78%. The mean diameters of microspheres were found in required micrometer range. The results of optimized formulations showed a narrow size distribution and smooth surface. The DSC and the FTIR analysis showed the absence of any potent incompatibility between the drug and the polymer. In-vitro release showed 86.4% drug release after 12 hours. Results of present study suggest that Acrycoat S100 loaded microsphere of ketoprofen can be successfully designed to develop sustained drug delivery system. The solvent evaporation method is a suitable technique for the preparation of Acrycoat S100 microspheres for controlling the release of Ketoprofen for a prolonged duration.

Keywords: Ketoprofen, Acrycoat S100, solvent evaporation method


How to cite this article:
Prajapati V C, Patel P R, Prajapati G B. Formulation, optimization and evaluation of sustained release microsphere of ketoprofen. J Pharm Bioall Sci 2012;4, Suppl S1:101-3

How to cite this URL:
Prajapati V C, Patel P R, Prajapati G B. Formulation, optimization and evaluation of sustained release microsphere of ketoprofen. J Pharm Bioall Sci [serial online] 2012 [cited 2020 Sep 21];4, Suppl S1:101-3. Available from: http://www.jpbsonline.org/text.asp?2012/4/5/101/94156

Ketoprofen, (RS) 2-(3-benzoylphenyl)-propionic acid is one of the propionic acid class of non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic effects. It potently inhibits the enzyme cyclooxygenase resulting in prostaglandin synthesis inhibition. It also prevents formation of thromboxane A2 by platelet aggregation. Ketoprofen is readily absorbed from the gastrointestinal tract and peak plasma concentrations occur about 0.5 - 2 h after a dose, but it causes a certain irritation in the gastrointestinal mucous membrane and possesses a bitter taste and aftertaste. This makes ketoprofen a very good candidate for the formulation of controlled release dosage forms. Ketoprofen microspheres help to protect the gastric mucous membrane from drug irritation and to mask its taste.


   Materials and Methods Top


Ketoprofen was obtained from BEC chemicals,Raigad. Acrycoat S 100 was received from Corel Pharm chem, Ahmedabad . All other chemicals and reagents used were obtained from S.D. Fine chem, Mumbai.

Ketoprofen loaded microsphere was prepared by emulsion solvent evaporation technique using Acrycoat S100 as a polymer, Poly vinyl alcohol as a surfactant. Ketoprofen and Acrycoat S100 were dissolved in mixture of ethanol and Dichloromethane. This mixture was poured in a 100 ml water containing PVA maintained at specified temperature with stirring. Stirring was continued for 2 h. to allow the volatile solvent to evaporate. The microspheres formed were filtered, washed with water and dried in oven at temperature of 40°C. The prepared microspheres were characterized for: 1) Particle size, 2) percentage yield, 3) Percentage drug entrapment, 4) DSC study, 5) Scanning electron microscopy and 6) in vitro drug release.


   Results and Discussion Top


Particle size

The smallest particle had a size of 153 μm while the largest particle had 178 μm particle size.

Percentage yield

Percentage yield of all batches ranged from 64.52% to 78.58%.

Percentage drug entrapment efficiency

Percentage drug entrapment efficiency of all batches varied from 62.12% to 67.82%.

DSC study

DSC thermograms of Ketoprofen, physical mixture and formulations were investigated. It revealed that there were no drug excipient incompatability [Figure 1].
Figure 1: DSC thermograph of a: Ketoprofen, b: Physical mixture, c: Formulation

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Scanning electron microscopy (SEM)

The surface morphology and shape were visualized by scanning electron microscopy (SEM). SEM of microsphere revealed that particles were spherical [Figure 2].
Figure 2: SEM of N1 formulation

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In vitro drug release

In vitro drug release were carried out for all formulations using USP dissolution apparatus Type I filled with 900 ml Phosphate buffer 6.8. 2 ml of aliquot was withdrawn at predetermined intervals. The samples were analyzed by UV spectrophotometry. Results were shown in the [Table 1].There was in vitro drug release was highest in batch N1 (86.4%) and lowest in batch N4 (66.72%) [Figure 3]. The decrease in drug release in the N4 batch because of the higher percent of Acrycoat S 100 from which the drug did not diffuse at the desired rate.
Figure 3: % DR vs time (hours)

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Table 1: Result of batches

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   Conclusion Top


Ketoprofen microspheres were successfully prepared by using the emulsion solvent evaporation method. Polymer-drug ratio influences the particle size as well as drug release from microsphere. The % yield and % entrapment efficiency were found higher in batch N1 (1:1). In vitro drug release from all the batches was found sustained over the period of 12 hours. Hence it can be concluded that Ketoprofen loaded Acrycoat S 100 microsphere may be useful to achieve sustained drug release profile suitable for oral administration to reduce GI side effects. [4]

 
   References Top

1.Ghodake JD, Vidhate JS, Shinde DA, Kadam AN. Formulation and evaluation of floating Microsphere containing anti-diabetic (metformin Hydrochloride) drug. Int j pharmtech res. 2010; 2(1): 378-384  Back to cited text no. 1
    
2.Khodairy KA, Eshra AG, Nada AH. Preparation and in vitro evaluation of slow release Ketoprofen microcapsules formulated into tablets and capsules. J Microencapsulation, 2002; 9: 365-373.  Back to cited text no. 2
    
3.Dinnarvand R.,Mirffatahi S, and Atyabi F.,Preparation,characterization and in vitro drug release of Isosorbide Dinitrate Microspheres. J. Microencap. 2002,19,73-81.  Back to cited text no. 3
    
4.I. Biswal, A. Dinda, D. Das, A. Chowdary. Encapsulation protocol for highly hydrophilic drug using nonbiodegradable polymer, International Journal of Pharmacy and Pharmaceutical Sciences, 2011,3, 256-259.  Back to cited text no. 4
    


    Figures

  [Figure 1], [Figure 2], [Figure 3]
 
 
    Tables

  [Table 1]


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