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FORMULATION AND EVALUATION OF
SUSTAINED RELEASE MICROSPHERES
OF FENOFIBRATE
Done by
Mini Mol.P.V
Reshma Fathima.K
Under the Guidance of
Ms.Sreethu K Sreedharan
CONTENTS
 Introduction
 Literature Review
 Objective And Plan of Study
 Materials And Equipments
 Methodology
 Results And Discussion
 Summary And Conclusion
 References
2
INTRODUCTION
 A well designed controlled drug delivery system can
overcome some of the problems of conventional
therapy and enhance the therapeutic efficacy of a
given drug. To obtain maximum therapeutic efficacy,
it becomes necessary to deliver the agent to the
target tissue in the optimal amount in the right
period of time there by causing little toxicity and
minimal side effects.
3
 There are various approaches in delivering a therapeutic
substance to the target site in a sustained controlled
release fashion.
 One such approach is using microspheres as carriers for
drugs.
 Microspheres are characteristically free flowing powders
consisting of proteins or synthetic polymers which are
biodegradable in nature and ideally having a particle size
less than 200 μm.
 This is the important approach in delivering therapeutic
substance to the target site in sustained and controlled
release fashion.
4
 Microspheres are sometimes referred to as
microparticles. Microspheres can be manufactured
from various natural and synthetic materials.
 Polyethylene, polystyrene and expandable
microspheres are the most common types of
polymer microspheres.
 Polystyrene microspheres are typically used in
biomedical applications due to their ability to
facilitate procedures such as cell soeting and
immunio precipitation
5
Mechanism of Drug Release
 Most of the drug delivery through micro particles
inhibits a matrix type internal solid dispersion
morphology structure.
 The drug may be insoluble in the polymeric matrix
and the drugs are released by erosion. Initially water
diffuses into the matrix dissolving the resulting
adjacent to the surface of the device.
 The resulting osmotic pressure is relieved by forming
a channel to the surface releasing a defined amount
of drug in the initial drug burst.
6

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Formulation and evaluation of sustained release microspheres of

  • 1. FORMULATION AND EVALUATION OF SUSTAINED RELEASE MICROSPHERES OF FENOFIBRATE Done by Mini Mol.P.V Reshma Fathima.K Under the Guidance of Ms.Sreethu K Sreedharan
  • 2. CONTENTS  Introduction  Literature Review  Objective And Plan of Study  Materials And Equipments  Methodology  Results And Discussion  Summary And Conclusion  References 2
  • 3. INTRODUCTION  A well designed controlled drug delivery system can overcome some of the problems of conventional therapy and enhance the therapeutic efficacy of a given drug. To obtain maximum therapeutic efficacy, it becomes necessary to deliver the agent to the target tissue in the optimal amount in the right period of time there by causing little toxicity and minimal side effects. 3
  • 4.  There are various approaches in delivering a therapeutic substance to the target site in a sustained controlled release fashion.  One such approach is using microspheres as carriers for drugs.  Microspheres are characteristically free flowing powders consisting of proteins or synthetic polymers which are biodegradable in nature and ideally having a particle size less than 200 μm.  This is the important approach in delivering therapeutic substance to the target site in sustained and controlled release fashion. 4
  • 5.  Microspheres are sometimes referred to as microparticles. Microspheres can be manufactured from various natural and synthetic materials.  Polyethylene, polystyrene and expandable microspheres are the most common types of polymer microspheres.  Polystyrene microspheres are typically used in biomedical applications due to their ability to facilitate procedures such as cell soeting and immunio precipitation 5
  • 6. Mechanism of Drug Release  Most of the drug delivery through micro particles inhibits a matrix type internal solid dispersion morphology structure.  The drug may be insoluble in the polymeric matrix and the drugs are released by erosion. Initially water diffuses into the matrix dissolving the resulting adjacent to the surface of the device.  The resulting osmotic pressure is relieved by forming a channel to the surface releasing a defined amount of drug in the initial drug burst. 6
  • 7. Materials Used  Microspheres used usually are polymers. They are classified into two types 1. Synthetic polymers 2. Natural polymers Synthetic Polymers: a)Non biodegradable polymers: Polymethyl methacrylate (PMMA), Acrolein, Glycidyl methacrylate, Epoxypolymers 7
  • 8. b) Biodegradable polymers:  Lactides, their glycolides and their copolymers, PolyalkylCyano Acrylate. Natural polymers  These are obtained from different sources like proteins, carbohydrates and chemically modified carbohydrates.  Proteins: Albumin, Gelatin, And Collagen, Carbohydrates: Agarose, Carrageenan, Chitosan, Starch. 8
  • 9. Methods  Single emulsion technique  Double emulsion technique  Polymerization  Phase separation/ Coacervation  Spray drying  Solvent extraction  Emulsion Solvent Evaporation  Wet emulsion technique  Hot Melt Microencapsulation 9
  • 10. Pharmaceutical Applications  Ophthalmic Drug Delivery Polymer  Gene delivery Gene delivery systems  Intratumoral and local drug delivery  Oral drug delivery  Nasal drug delivery  Buccal drug delivery  Gastrointestinal drug delivery:  Peroral drug delivery  Vaginal drug delivery  Transdermal drug delivery  Colonic drug delivery  Multiparticulate delivery system 10
  • 11. LITERATURE REVIEW  Naeem. M, Kiran. B et al., 2013 developed the fenofibrate loaded liposphere system. An attempt was made to improve aqueous solubility of FNO by aid of stearic acid and Paraffin oil. Significant improvement in the aqueous solubility of the drug in the FNO lipospheres supports the applicability of lipospheres as a tool for improving aqueous solubility of the BCS class-II drugs10. 11
  • 12.  Modi, Tayade et al 2006., developed the Solid dispersion (kneading) technique for the enhancement of the dissolution profile of valdecoxib using solid dispersion with PVP and the preparation of fast-dissolving tab- lets of valdecoxib by using a high amount of superdisin- tegrants. A phase solubility method was used to evaluate the effect of various water-soluble polymers on aqueous solu- bility of valdecoxib. Polyvinyl pyrrolidone (PVP K- 30) was selected and solid dispersions were prepared by the method of kneading14. 12
  • 13. Drug Profile  DRUG : Fenofibrate  CATEGORY : Hypolipidaemic drug  MOLECULAR STRUCTURE :  MOLECULAR FORMULA : C20 H21ClO4  DESCRIPTION: white crystalline solid, odourless.  MELTING POINT: 79-82°C 13
  • 14.  SOLUBILITY: Soluble in organic solvents such as ethanol, methanol, DMSO, and DMF. Sparingly soluble in aqueous buffers.  MECHANISM OF ACTION: it is a fibrate class hypolipidaemic drug. It enhances activity of the enzyme lipoprotein lipase, which degrades VLDL level resulting in lowering of triglycerides. They also increase HDL levels. Fibrates also inhibits coagulation and promote thrombolysis, which also accounts for their beneficial effects.  ADVERSE EFFECTS: GI upsets, skin rashes, headache, muscle cramps blurred vision.Adverse events occurs in about 1% of the patients treated with fenofibrate. Skin rashes were the most frequent event causing discontinuation of therapy. 14
  • 15.  PHARMACOKINETICS: pharmacokinetics significantly affected by food intake. The high fat breakfast will significantly affecting the rate of absorption of fenofibrate more than the standard breakfast and fasted conditions specifically AUC from zero to infinity and peak plasma concentration (Cmax) is increased.  DOSE: Orally available as 140mg, 160 mg and 200mg tablets and capsules.  STORAGE: Store below 30ºC. 15
  • 16. OBJECTIVE AND PLAN OF STUDY  The sustained release dosage forms are designed to achieve a prolonged therapeutic effect by continuously releasing medication over extended periods of time after administration of a single dose.  The ideal drug delivery system will possess two main properties »It will be a single dose for the whole duration of treatment. »It will deliver the active drug delivery at the site of action. 16
  • 17. MATERIALS AND EQUIPMENTS USED SL.N O MATERIALS SUPPLIED BY 1 Fenofibrate Alkem pharmaceuticals Pvt Ltd,mumbai 2 Gelatin Nice chemicals,Banglore 3 Methanol Nice chemicals,Banglore 4 Tween 20 Prowess lab chemicals 5 Liquid paraffin Prowess lab chemicals 6 Formaldehyde Nice chemicals,Banglore 7 Hydrochloric acid Nice chemicals,Banglore 8 Monosodium phosphate Nice chemicals,Banglore 9 Disodium phosphate Nice chemicals,Banglore SL.N O INSTRUMENTS MANUFACTURER 1 Electronic weighing balance Shimadzu BL220H,Japan 2 Magnetic stirrer Remiequipments Pvt Ltd 3 Optical microscope Dolar US 4 4 UV-Spectroscopy Shimadzu 1600,Japan 5 FTIR Shimadzu 8400,Japan 6 Dissolution test apparatus Electro Lab,TDT 08L (USP) 7 Differential Scanning Calorimetry Shimadzu D.S.C TA60 WS Thermal Analyzer 8 Scanning Electron Microscopy DSC-823e, Mettler Toledo 17
  • 18.  Preformulation Studies  Identification of drug FTIR (fourier transforms infrared spectra) DSC Analysis Physical Appearance Melting point  Drug excepient compatability studies  Spectrophotometric Scanning of fenofibrate and polymer Preparation of standard stock solution Construction of calibration curve METHODOLOGY 18
  • 19. • Formulation  Preparation of Drug Polymer phase  Preparation of Oily Phase  Preparation of Gelatin microspheres of fenofibrate Formulation Drug(mg) Polymer(mg) Tween20( ml) F1 200 1000 1 F2 200 1500 1 19
  • 20. • Evaluation Studies  Bulk characterization  angle of repose θ = tan−1 h r  bulk density Bulk Density = weight of sample in gm volume occupied by the sample  tapped density Tapped Density = weight of sample in gm volume occupied by the sample after tapping 20
  • 21.  Carr´s Index (CI) Carr’s Index = tapped density−bulk density tapped density  Percentage yield (%Y) % Yield = practical yield theoretical yield ×100  Percentage Drug Entrapment(%DE) % Drug Entrapment = practical drug content theoretical drug content × 100 21
  • 22.  Morphology By using SEM analysis  Invitro Cumulative Percentage Drug Release Study The FNO release from the microspheres was evaluated by using the US Pharmacopoeia Dissolution Apparatus-II Paddle (XVIII) in 900ml mixture of PBS pH 6.8 with 1% SLS in 9:1 at 37°C ± 0.5 temperature. The rotational speed of dissolution apparatus was maintained at 100rpm. Each run was carried out in triplicates. Accurately weighed 243mg of microspheres were filled in a “0” size capsule to get the final weight of 475mg each of the capsules was transformed into dissolution media. The 5ml samples were withdrawn at predetermined time intervals with dissolution media replacement and were filtered through 0.45µm whatman filter paper. The drug content was determined spectrophotometrically at 290nm on shimadzu UV/ Vis- spectrophotometer. 22
  • 23. RESULTS AND DISCUSSION IR spectrum of Fenofibrate IR spectrum of Gelatin 23
  • 24. IR spectrum of Fenofibrate + Gelatin Frequency (cm-1) FNO Frequency (cm-1) Physical mixture Interpretation 3036 3039 Alkanes 3220 3211 Monosubsituted benzene ring 3437 3439 Phenols 3526 3514 1,4-Disustituted phenol 1416 1417 -CH3 group 1622 1625 Carboxylic group 1796,1224 1796,1225 Aromatic ester 1220 1225 -CH2Cl IR Spectral peaks of Fenofibrate and physical mixture 24
  • 25. SEM Analysis of fenofibrate and microspheres 25
  • 26. DSC analysis of prepared microspheres DSC Curve of Fenofibrate 26
  • 27. Standard curve CONCENTRATION ABSORBANCE 0 0.00 10 0.553 20 0.996 30 1.545 40 2.015 50 2.497 27
  • 28. Bulk characterization Sl.no Parameter Fenofibrate microspheres F1 F2 1 Angle of repose 24.11 25.22 2 Bulk density 0.26 0.31 3 Tapped density 0.33 0.39 4 Carr’s index 20 22 5 Hausner’s ratio 1.25 1.30 28
  • 29.  Percentage yield The percentage yield was calculated as per the equation and it was found to be 74 % and 76% in formulation F1 and F2 respectively.  Percentage Drug Entrapment % Drug entrapment of drug entrapped within the polymer matrices were in the range of 70-97 %. An entrapment efficiency depends on the drug solubility in the solvent system used for processing.  In-vitro drug release study: The drug release from microspheres in phosphate buffer pH 6.8 has been shown in Figure . Cumulative % drug release from F1and F2, were in the range of 60 and 68% within 12hours respectively. No formulation is showing burst release which indicates the absence of free particles on the surface of microspheres which further confirmed by SEM study. The trail revealed that low level of gelatin (25%) failed to produce microsphere with acceptable physical characteristic where as high level of stearic acid (100%) resulted in liposphere that exhibited high percentage of drug release. As the level of paraffin oil increases the particle size of liposphere increases due to tackiness which in turn decrease the % drug release from the liposphere 29
  • 30. Dissolution values of F1 Dissolution Values of F2 Sl.n o Time (hr) Absorbanc e Concentrati on (µg/ml) Amount of drug released % drug release Cumulativ e % drug release 1 0 0 0 0 0 0 2 0.5 0.009 0.0611 0.0611 4.07 4.07 3 1 0.020 0.1919 0.1919 12.79 12.87 4 2 0.038 0.4058 0.4058 27.05 27.31 5 3 0.045 0.4890 0.4890 32.60 33.14 6 4 0.052 0.5722 0.5722 38.15 38.79 7 5 0.060 0.6673 0.6673 44.49 45.25 8 6 0.067 0.7506 0.7506 50.04 50.93 9 7 0.072 0.8099 0.8099 53.99 54.99 10 8 0.073 0.8219 0.8219 54.79 55.87 11 10 0.075 0.8456 0.8456 56.37 57.47 12 12 0.079 0.8932 0.8932 59.15 60.17 Sl.n o Time (hr) Absorban ce Concentrati on (µg/ml) Amount of drug released % drug releas e Cumulati ve % drug release 1 0 0 0 0 0 0 2 0.5 0.009 0.0574 0.0574 5.45 5.45 3 1 0.013 0.1068 0.1068 7.25 7.29 4 2 0.019 0.1962 0.1962 14.41 14.49 5 3 0.028 0.2869 0.2869 19.13 19.34 6 4 0.035 0.3702 0.3702 24.68 25.06 7 5 0.050 0.5485 0.5485 36.57 37.06 8 6 0.062 0.6911 0.6911 46.07 46.80 9 7 0.074 0.8338 0.8338 55.59 56.51 10 8 0.081 0.9169 0.9169 61.13 62.24 11 10 0.086 0.9764 0.9764 64.09 65.26 12 12 0.090 1.0239 1.0239 66.26 67.39 30
  • 31. 31
  • 32. SUMMARY AND CONCLUSION Following concclusions have been drawn from the present study:  In the preformulation studies, it was found that Fenofibrate is having poor flow property. Hence in the present study, the resulting microsphere considerably improved flow properties.  The analytical mehod used in the present study was found to be suitable for the estimation of Fenofirate, which was indicated by the high regression values obtained in the standard plot.  The yellowish white microspheres were obtained by using emulsion – coacervation method and the percentage yield was found to be 74% for F1 and 76 % for F2.  Scanning electron microscopy of Fenofibrate microsphere was also performed and the surface morphology were studied. 32
  • 33.  Sustained release property of microsphere were also enhanced by incorporating the microsphere in enteric coated capsules.  The percentage drug entrapment were in the range of 70- 97%.  The invitro drug release study showed that the microspheres were released 60 and 67% of drug at 12 hrs in formulation F1 and F2 respectively.  Gelatin can be effectively used for the preparation of sustained release Fenofibrate microsphere. In conclusion, the present study demonstrated the successful preparation of once daily sustained release microsphere of Fenofibrate. 33
  • 34. REFERENCES  Ramteke. K. H, Jadhav.V. B, Dhole. S. N, [2012], Microspheres as carriers used for novel drug delivery system, IOSRPHR, 2(4), 44-48.  Sahil, Akanksha, Premjeet, Bilandi, Kapoor, [2011], Microsphere a review, IJRPC, 1(4).  Prabus. L, Shirwaikar A, Kumar, [2009], Formulation and evaluation of sustained release microspheres of rosin containing aceclofenac, ARS Pharm, vol 50, 51-62.  Gangadhar.C. B, Sunder. R, Varma. M, Raju. M, Saikiran. M, [2010], Formulation and evaluation of indomethacin microspheres using natural and synthetic polymers as controlled release dosage forms, International journal of drug discovery, 2(1), 8-16.  Barhate. D, Rupnar. S, Sonvane. M, Pawar. R, Rahane. D, [2009], Formulation and evaluation of floating microspheres of ketorolac trometSSSamol, International journal of pharmaceutical research and development online,1 (9), ISSN: 0974-9446. 34