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Solid lipid nanoparticle

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Colloidal particles ranging in size between 10 & 1000 nm are known as nanoparticles.

SLNs are new generation of submicron sized lipid emulsion where the liquid lipid(oil) has been substituted by a solid lipid.

Example: Capture - Dior

Published in: Health & Medicine
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Solid lipid nanoparticle

  1. 1. Department of Pharmacy (Pharmaceutics)Department of Pharmacy (Pharmaceutics) || Sagar savaleSagar savale Mr. Sagar Kishor SavaleMr. Sagar Kishor Savale Department of Pharmaceutics avengersagar16@gmail.com 2015-016
  2. 2. Content: History Introduction Advantage of SLNs over Polymeric nanoparticles Methods of Preparation Sterilization of SLNs Analytical characterization of SLNs Applications of SLNs Conclusion  References 204/28/16 Sagar Savale
  3. 3. History: 304/28/16 Sagar Savale
  4. 4. Introduction: Colloidal particles ranging in size between 10 & 1000 nm are known as nanoparticles. SLNs are new generation of submicron sized lipid emulsion where the liquid lipid(oil) has been substituted by a solid lipid. Example: Capture - Dior 404/28/16 Sagar Savale
  5. 5. Advantages of SLNs: Control & target drug release Increased drug stability High & enhanced drug content Feasible for carrying both lipophilic & hydrophilic drug Excellent biocompatibility Water based technology Easy to scale up & sterlize Avoid RES 504/28/16 Sagar Savale
  6. 6. Disadvantages:  Drug Loading capacity is limited  High water content  High pressure induce drug degradation  Coexistences of several colloidal species  Lipid crystallization & drug incorporation - supercooled melts - gelation phenomenon  Drug expulsion 604/28/16 Sagar Savale
  7. 7. 704/28/16 Sagar Savale
  8. 8. NLC the more intelligent system…. 804/28/16 Sagar Savale
  9. 9. Advantages of SLNs over polymeric NPs Polymeric Nanoparticles Solid Lipid Nanoparticles Residual contamination Avoid residual contamination Possible toxicity problems No toxicity problems Expensive production & a lack of large scale production method Cost effective methods are available Lack of suitable sterilization method Feasible sterilization method available Not stable as compared to SLNs SLNs formulation stable for even three years have been developed 904/28/16 Sagar Savale
  10. 10. SLNs preparation: General ingredients include solid lipid, emulsifier & water Lipid contains triglycerides, partial glycerides, fatty acids, steroids, waxes Combination of emulsifier might prevent particle agglomeration Emulsifier include soybean lecithin, egg lecithin, poloxmer etc. 1004/28/16 Sagar Savale
  11. 11. Method of preparation: High pressure homogenization - Hot homogenization - Cold homogenization Ultrasonication Solvent emulsification/evaporation Micro emulsion Using Supercritical Fluid  By Spray drying 1104/28/16 Sagar Savale
  12. 12. Hot Homogenization Melting of the lipid & dissolving/dispersing of the drug in the lipid Dispersing of the drug loaded lipid in a hot aqueous surfactant mixture. Premix using a stirrer to form a coarse preemulsion High pressure homogenization at a temperature above the lipid M.P. Hot O/W nanoemulsion Solid Lipid Nanoparticles Disadvantages: 1) temperature induce drug degradation 2) partioning effect 3) complexity of the crystallization 1204/28/16 Sagar Savale
  13. 13. Cold Homogenization Melting of lipid & dissolving/dispersing of the drug in the lipid Solidification of the drug loaded lipid in liquid nitrogen or dry ice Grinding in a powder mill Dispersing the powder in a aqueous surfactant dispersion medium High pressure homogenization at room temperature or below. Solid Lipid Nanoparticles Disadvantages: 1) Larger particle sizes & broader size distribution 2) does not avoid thermal exposure but minimizes it 1304/28/16 Sagar Savale
  14. 14. Ultrasonication: Adv. : 1) Equipment used is very common 2) No temperature induced drug degradation Disadv.: 1) Potential metal contamination 2) Broader particle size distribution 1404/28/16 Sagar Savale
  15. 15. Solvent emulsification:  Lipophilic material is dissolved in a water immiscible organic solvent (e.g.cyclohexane) that is emulsified in an aqueous phase.  Upon evaporation of solvent, a nanoparticle dispersion is formed by ppt of lipid in aq. Medium.  Adv.: Avoidance of any thermal stress  Disadv.: use of organic solvents. 1504/28/16 Sagar Savale
  16. 16. Using Microemulsion: Preparation by stirring optically transparent mixture at 65- 70o c composed of a low melting fatty acid, emulsifier, coemulsifier & water. This hot microemulsion dispersed in cold water (2-3o c) & stirring. 1604/28/16 Sagar Savale
  17. 17. By using Supercritical fluid Can be prepared by Rapid Expansion of Supercritical Carbon dioxide solution methods(RESS) Adv.: 1) Solvent less processing. By Spray drying method  Alternative to lyophilization Disadv.: 1) particle aggregation due to high temp., shear forces & partial melting of particles. 2) Recommended use of lipid with M.P. >700 c for spray drying. 1704/28/16 Sagar Savale
  18. 18. Sterilization of SLNs For parentral & ocular administration SLNs must be sterile. For lecithin stabilized SLNs autoclaving is possible & it is not possible for sterically stabilized polymers. Physical stability during autoclave can not be stated, it depends on composition. SLN dispersion can also be sterilized by filtration 1804/28/16 Sagar Savale
  19. 19. Characterization of SLNs: [I] Measurement of particle size Photon correlation spectroscopy Transmission electron microscopy Scanning electron microscopy Field Flow Fractionation (FFF) X-ray diffraction 1904/28/16 Sagar Savale
  20. 20. [II] Measurement of Zeta Potential Allows predictions about the storage stability of colloidal dispersion Zeta potential under 30 mV are required for full electrostatic stabilization. [III] Molecular weight Gel chromatography Atomic force microscopy [IV] Surface element analysis X-ray photoelectron spectroscopy Electrophoresis Laser doppler anaemometry XRD DSC 2004/28/16 Sagar Savale
  21. 21. [V] DENSITY Helium compression pychnometry Contact angle measurement [VI] Molecular analysis H-NMR Infra red analysis [VI] Measurement of Crystallinity, Lipid modification DSC & X-ray scattering used to investigate status of lipid 2104/28/16 Sagar Savale
  22. 22. [VII] Coexistence of additional colloidal structure NMR & ESR used for this purpose 2204/28/16 Sagar Savale
  23. 23. Applications SLNS/ NLCS aS CoSmeCeutiCaLS  applied in the preparation of sunscreens.  SLN has UV reflecting properties. 2304/28/16 Sagar Savale
  24. 24. oRaL SLN iN aNtituBeRCuLaR tHeRaPY Anti-tubercular drugs such as rifampicin, isoniazide, loaded SLNs able to decrease dosing frequency SLN aS a GeNe VeCtoR CaRRieR Several recent reports of SLN carrying genetic materials such as DNA, plasmid DNA, & other nucleic acid. 2404/28/16 Sagar Savale
  25. 25. Major challenges where nanotech is needed in cancer therapy Cancer comes from our cells – domestic terrorist! Cancers are different from patient to patient Cancers continue to change as they grow 2504/28/16 Sagar Savale
  26. 26. Challenge #1: Cancer comes from our cells – domestic terrorist! Bacteria & viruses = easy to spot Cancer = difficult to detect, difficult to treat 2604/28/16 Sagar Savale
  27. 27. Challenge #2: Cancers are different from patient to patient Each tumor is like a salad from a salad bar They all have a unique combination of ingredients (DNA errors) 2704/28/16 Sagar Savale
  28. 28. Challenge #3: Cancers continue to change as they grow Challenge #3: Cancers continue to change as they grow If a tumor is detected too late, it has probably already won 2804/28/16 Sagar Savale
  29. 29. Rationale of using SLN for anticancer delivery 2904/28/16 Sagar Savale
  30. 30. Tumor Mass SLNs attack blood vesicles which nourish metastatic tumors 04/28/16 Sagar Savale 30
  31. 31. WHY SLN FOR ANTICANCER THERAPY ? Improved stability of cytotoxic compounds by SLN encapsulation Improved pharmacokinetics and drug biodistribution by SLN  Significant anticancer activity of SLN-encapsulated cytotoxic drug. 3104/28/16 Sagar Savale
  32. 32. Changes in biodistribution of antiCanCer drugs delivered by sln Drug Organs with increased drug concentration delivered by SLN Idarubicin Blood, brain Etoposide Blood, brain, tumor, liver, lung, spleen, kidney, bone Doxorubicin Blood, brain Camptothecin Blood, brain, liver, lung, spleen, kidney, heart 3204/28/16 Sagar Savale
  33. 33. Potential of sln in brain targeting SLNs taken up readily by the brain due to their lipidic nature.  high potential to treat brain cancer.  New formulations of neuroactive drugs into SLN are expected to improve their pharmacokinetic profile. 3304/28/16 Sagar Savale
  34. 34. References: 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  Wong H.L., Bendayn R., Rauth A.M., Yongqiang L., Xiao Y.W. “ Chemotherapy with anticancer drugs encapsulated in solid lipid nanoparticles’’ Advanced drug delivery reviews, 59 (2007) 491-504 3404/28/16 Sagar Savale
  35. 35. Mehnert W., Mader K. “ Solid lipid nanoparticles Production, characterization and applications” Advanced drug delivery reviews, 47 (2001) 165-196. Schwarz C., Mehnert W., Lucks J.S., Muller R.H. “ Solid lipid nanoparticles (SLN) for controlled drug delivery Production, characterization and sterilization” Journal of controlled release 30 (1994) 83-96.  Gasco M.R. “ Lipid nanoparticles: perspectives and challenges” Advanced drug delivery reviews, 59 (2007) 377-378. 3504/28/16 Sagar Savale
  36. 36. 3604/28/16 Sagar Savale

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