Solid lipid nanopaticle as promising drug


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Solid lipid nanopaticle as promising drug

  1. 1. SOLID LIPID NANOPARTICLE AS PROMISING DRUG DELIVARY SYSTEM DEPARTMENT OF PHARMACEUTICS ANURADHA COLLEGE OF PHARMACY, CHIKHLI. 2011-2012. Seminar on: Recent Trends in Pharmaceutical Sciences Presented by: Gajanan S.Ingole Guided by: Mr. K.B.Charhate 1
  2. 2. Introduction Advantages & disadvantages Aims of SLNs Principal of drug release Methods of Preparation Analytical characterization of SLNs Applications of SLNs Routes of administration References CONTENTS : 2
  3. 3. Solid lipid nanoparticles The solid lipid nanoparticles(SLN’s) are submicron colloidal carriers which are composed of physiological lipid, dispersed in water or in an aqueous surfactant solution. They consist of macromolecular materials in which the active principle is dissolved, entrapped, and or to which the active principle is adsorbed or attached. No potential toxicity problems as organic solvents are not used. SLNs are spherical in shape & diameter range from 10-1000nm. To overcome the disadvantages associated with the liquid state of the oil droplets, the liquid lipid was replaced by a solid lipid shown in fig, 3
  4. 4. The reasons for the increasing interest in lipid based system are : 1. Lipids enhance oral bioavailability and reduce plasma profile variability. 2. Better characterization of lipoid excipients. 3. An improved ability to address the key issues of technology transfer and manufacture scale-up. Fig. 1: Structure of solid lipid nanoparticle (SLN) 4
  5. 5. Advantages of SLN 1) Control and target drug release. 2) Excellent biocompatibility. 3) Improve stability of pharmaceuticals. 4) High and enhanced drug content. 5) Easy to scale up and sterilize. 6) Enhanced bioavailability of entrapped bioactive compounds. 7) Much easier to manufacture than biopolymeric nanoparticles. 8) No special solvent required. 5
  6. 6. 9) Conventional emulsion manufacturing methods applicable. 10) Raw materials essential the same as in emulsions. 11) Can be subjected to commercial sterilization procedures. Disadvantages of SLN 1) Particle growth. 2) Unpredictable gelation tendency. 3) Unexpected dynamics of polymeric transitions Aims of solid lipid nanoparticles 1) Possibility of controlled drug release. 2) Increased drug stability. 6
  7. 7. 3) High drug pay load. 4) No bio-toxicity of the carrier. 5) Avoidance of organic solvents. 6) Incorporation of lipophilic and hydrophilic drugs. Principles of drug release from SLNs The general principles of drug release from lipid nanoparticles are as 1. Crystallinization behaviour of the lipid carrier and high mobility of the drug lead to fast drug release. 2. Higher surface area due to smaller particle size in nanometer range gives higher drug release. 3. Slow drug release can be achieved when the drug is homogenously dispersed in the lipid matrix. It depends on type and drug entrapment model of SLN. 7
  8. 8. Methods of preparation of solid lipid nanoparticles 1. High pressure homogenization A. Hot homogenization B. Cold homogenization 2. Ultrasonication A. Probe ultrasonication B. Bath ultrasonication 3. Solvent evaporation method 4. Solvent emulsification-diffusion method 5. Microemulsion based method 6. Spray drying method 8
  9. 9. 7. Double emulsion method 8. Precipitation technique 9. Film-ultrasound dispersion First method to prepare solid lipid nanoparticle are as 1. High pressure homogenization A. Hot homogenization 9
  10. 10. Fig: Solid lipid nanoparticles preparation by hot homogenization process 10
  11. 11. B. cold homogenization process 11
  12. 12. 2. Ultrasonication/high speed homogenization SLNs are also prepared by ultrasonication or high speed homogenization techniques. For smaller particle size combination of both ultrasonication and high speed homogenization is required Advantages Reduced shear stress. Disadvantages Potential metal contamination. Physical instability like particle growth upon storage. 12
  13. 13. 3. Solvent evaporation 4. Solvent emulsification-diffusion method 13
  14. 14. 5. Microemulsion based method Fig. : Microemulsion method 14
  15. 15. 6. Spray drying method It's an alternative procedure to lyophilization in order to transform an aqueous NLC dispersion into a drug product. It's a cheaper method than lyophilization. But his method can cause particle aggregation due to high temperature, shear forces and partial melting of the particle. 7. Double emulsion method Here the drug is encapsulated with a stabilizer to prevent the partitioning of drug in to external water phase during solvent evaporation in the external water phase of w/o/w double emulsion. 15
  16. 16. 8. Precipitation method The glycerides are dissolved in an organic solvent (e.g. chloroform) and the solution will be emulsified in an aqueous phase. After evaporation of the organic solvent the lipid will be precipitated forming nanoparticles. 9. Film-ultrasound dispersion lipid + drug add in to organic solutions, after decompression, rotation and evaporation of the organic solutions, a lipid film is formed. Then the aqueous solution which includes the emulsions was added, Using the ultrasound with the probe to diffuser at last, the SLN with the little and uniform particle size is formed. 16
  17. 17. 1) Measurement of particle size Static light scattering (SLS) Electron microscopy Acoustic methods. Atomic force microscopy (AFM) DSC Analytical characterization of SLN 17
  18. 18. 2) Measurement of crystallinity & lipid modification X-ray photoelectron spectroscopy Laser doppler anaemometry DSC Gel chromatography Electrophoresis. DSC. IR. X-ray scattering. Raman spectroscopy 3) Co – existence of additional structures 18
  19. 19. Routes of administration 1. Parenteral administration 2. Oral administration 3. Rectal administration 4. Nasal administration 5. Respiratory delivery 6. Ocular administration 7. Topical administration 19
  20. 20. 1. SLN as potential new adjuvant for vaccines. 2. Solid lipid nanoparticles in cancer chemotherapy. 3. Solid lipid nanoparticles for delivering peptides and proteins. 4. Solid lipid nanoparticles for targeted brain drug delivery. 5. Solid lipid nanoparticles for parasitic diseases. 6. Solid lipid nanoparticles for ultrasonic drug and gene delivery. 7. SLN applied to the treatment of malaria. 8. Solid lipid nanoparticles in tuberculosis disease. 9. SLN in cosmetic and dermatological preparations. 10. SLN for potential agriculture applications Applications of SLN 20
  21. 21. Vyas S.P. and Khar R.K. Targeted And Controlled Drug Delivery System, 1stEdition, 2002, CBS Publication; 249 - 277. Jain N. K., Controlled and novel Drug Delivery, 1st edition 2001, CBS Publication; 292 - 301. Mukherjee S., Ray S., Thakur R.S. “ Solid lipid nanoparticles: a modern formulation approach in drug delivery system” Indian journal of Pharmaceutical sciences, 71(2009) 349-358. Heurtault B., Saulnier P., Pech B., Proust J.E., Benoit J.P. “ Physico-chemical stability of colloidal lipid particles’’ Biomaterials 24 (2003) 4283-4300 REFERENCE 21
  22. 22. Feng S., Chien S. “ Chemotherapeutic engineering: application and further development of chemical engineering principles for chemotherapy of cancer and other diseases” Chemical engineering science 58 (2003) 4087-4114. Gasco M.R. “ Lipid nanoparticles: perspectives and challenges”Advanced drug delivery reviews, 59 (2007) 377-378. Muller R.H., Mader K., Gohla S. “ Solid lipid nanoparticles (SLN) for controlled drug delivery – a review of the state of art” European journal of Pharmaceutics & Biopharmaceutics, 50 (2000) 161-177 Kaur I.P., Bhandari R., Bhandari S., Kakkar V. “ Potential of Solid lipid nanoparticles in brain targeting” Journal of Controlled release, 127 (2008) 97-109 22
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