FORMULATION AND INVITRO EVALUATION OF 5-FLUOROURACIL MICROCAPSULES BY USING DIFFERENT METHODS OF MICROENCAPSULATION

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ABOUT AUTHORS:
S.Shanmugam1, J. Srikanth Reddy*1, T. Vetrichelvan2
Adhiparasakthi College of Pharmacy,
Melmaruvathur, 603 319, Tamilnadu, India.
*srikanthjeedipelly@gmail.com

ABSTRCT:
The present study in formulation and evaluation of 5-fluorouracil microcapsules. 5-fluorouracil which is used as a anti cancer drug to treat cancer. The capsules were prepared by coacervation phase separation and emulsion solvent evaporation by using gelatin, sodium alginate and ethyl cellulose. The prepared microcapsules were evaluated with various evaluation methods such as drug content, in-vitro drug release studies, kinetic studies and stability studies as per ICH guidelines were performed. The formulated extended release microcapsules were prepared by powder layering technique. In these formulations containing 150mg of 5-fluorouracil was loaded in it. The particle size and dissolution study of  F9 formulation was concluded as the best formulation among other formulations, which showing the most desired drug release. It will be considered as optimized formulation. No significant change was observed in the drug content physical properties and dissolution rate of these micro pellets after the storage period of three months at 40±2ºc and 75±5%RH.

REFERENCE ID: PHARMATUTOR-ART-1914

INTRODUCTION
Microcapsules are small particles that contain an active agent or core material surrounded by a coating or shell. (Commercial microcapsules typically have a diameter between 3 & 800 micrometer and 10-90% core).

Microspheres:
Microspheres are solid, spherical particles containing dispersed drug molecules, either in solution or crystalline form, among the polymer molecule.


Fig 1: Microsphere & microcapsules

Microcapsules have an either spherical geometry with a continuous core region surrounded by    a continuous shell or have an irregular geometry and contain a number of small droplets or particles of core.

Reasons for Encapsulation:
There are several reasons why substances may be encapsulated

1. To protect reactive substances from the environment

2. To convert liquid active components into a dry solid system

3. To separate incompatible components for functional reasons

4. To mask undesired properties of the active components

5. To protect the immediate environment of the microcapsules from the active components

1.2 METHOD OF MICROCAPSULE PREPARATION:

(1) Coacervation – phase separation        

(2) Interfacial polymerization      

(3) In-Situ polymerization                                    

(4) Solvent evaporation                

(5) Solvent extraction

(6) Spray drying

(7) Fluidized Bed Coating

(8) MultiorificeCentrifugal process

(9) Pan coating

1. Coacervation – Phase Separation:  (Nitika Agnihotri, et al. 2012)
This process of microencapsulation is generally referred to The National Cash Register (NCR) Corporation and the patents of B.K. Green.

This process consists of three Steps-

  • Formation of three immiscible phases; a liquid manufacturing phase, a core material phase and a coating material phase
  • Deposition of the liquid polymer coating on the core material
  • Rigidizing of the coating material

Step-1: The first step of coacervation phase separation involves the formation of three immiscible chemical phases: a liquid vehicle phase, a coating material phase and a core material phase. The three phases are formed by dispersing the core material in a solution of coating polymer, the vehicle phase is used as a solvent for polymer. The coating material phase consists of a polymer in a liquid phase, is formed by using one of the of phase separation- coacervation method, i.e. .by changing the temperature of the polymer solution, by adding a solution, or by inducing a polymer- polymer interaction.

Step-2: It involves the deposition of the liquid polymer coating upon the core material. This is done by controlled mixing of liquid coating material and the core material in the manufacturing vehicle. Step-3: In the last step rigidizing of the coating material done by the thermal, cross linkingdesolvationtechniques.


Fig 1.4: Coacervation process: (a) Core material dispersion in solution of shell polymer; (b) Separation of coacervate from solution; (c) Coating of core material by micro droplets of coacervate; (d) Coalescence of coacervate to form continuous shell around core particles.

4. Solvent-Evaporation Method: (Hammad Umar, et al. 2011)
(Emulsification- Evaporation Method)

This technique is based on the evaporation of the internal phase of an emulsion by agitation. Initially, the coating polymeric material is dissolved in a volatile organic solvent. The core to be encapsulated is then dispersed in the coating polymer solution to form a suspension or emulsion.

In the next step, this organic solution is emulsified under agitation in dispersing phase, which is immiscible with the organic solvent, which contains the emulsifier. Once the emulsion is stabilized, agitation is maintained and the solvent evaporates after diffusing through the continuous phase. This results in the formation of microcapsule. On the completion of the process, the microcapsules held in suspension in the continuous phase are recovered by filtration or centrifugation and are washed and dried.


MATERIALS AND METHODS

MATERIALS
5-fluorouracil was received as a gift sample from Bindu Pharma Pvt.Ltd., Andhrapradesh. Gelatin, Sodium alginate and Ethyl cellulose were obtained from natco pharma Ltd., andrapradesh.

PREPARATION OF MEBEVERINE MICROCAPSULES
The microcapsules of 5-fluorouracil were prepared by coacervation phase separation by change in pH method and emulsion solvent evaporation. The formulation of sustained release microcapsules of 5-fluorouracil were done by using polymers gelatin, sodium alginate and ethyl cellulose. (Table 1)

EVALUATION OF MICROCAPSULES

APPEARANCE
The microcapsules were visually observed for physical appearance of microcapsules.

PARTICLE SIZE
Particle size distribution of microcapsules was determined by using phase contraction microscopy.

DRUG CONTENT
50 mg capsules were weighed and powdered and was transferred to a 100 ml volumetric flask and 15 ml pH 7.0 is added.  The drug is extracted in pH 7.0 by vigorously shaking the Stoppard flask for 2 hrs.  Then the volume is adjusted to the mark with distilled water and the liquid is filtered.  The drug content was determined by measuring the absorbance at 266 nm after appropriate dilution. The drug content was calculated using the standard calibration curve.  The mean percent drug content was calculated.

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