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solid lipid_nanonoparticle_

solid lipid nanoparticle

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solid lipid_nanonoparticle_

  1. 1. SOLID LIPID NANOPARTICLE Presented By.. Mr. Wagh Pankaj N. M.Pharm.(IInd Sem) 1 Department Of Pharmaceutics R.C.Patel Institute Of Pharmaceutical Education and Research, Shirpur. 2015-16
  2. 2.  Introduction  Advantages & disadvantages  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. 4) Poor drug loading capacity. 6
  7. 7. 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 3. Solvent evaporation method 4. Microemulsion based method 5. Supercritical method 6. Spray drying method 8
  9. 9. 9 It is a reliable and powerful technique, which is used for the production of SLN. High pressure homogenizers push a liquid with high pressure (100–2000 bar) through a narrow gap (in the range of A few microns). The fluid accelerates on a very short distance to very high velocity (over 1000 km/H). Very high shear stress and cavitations forces disrupt the particles down to the submicron range. Generally 5 -10% lipid content is used but up to 40% lipid content has also been investigated. Two general approaches of HPH are :- Hot Homogenization. Cold Homogenization. 1) High Shear Homogenization:
  10. 10. 10 A) Hot Homogenization technique: Melting of lipid Dissolution of the drug in the melted lipid Mixing of the preheated dispersion medium & drug lipid melt Premix using a stirrer to form a coarse pre-emulsion High pressure homogenization at a temp. above the lipid melting point o/w- nano emulsion Solidification of nano emulsion by cooling down to room temp. Solid lipid nanoparticle
  11. 11. 11 Advantages: Disadvantages: 1) temperature induce drug degradation. 2) partitioning effect. 3) complexity of the crystallization. 1) Easy to handle. 2) High concentration of surfactant and co-surfactant are not required. 3) Organic solvent free method
  12. 12. 12 B) Cold Homogenization Technique: Melting of the lipid Dissolution of the drug in the melted lipid Solidification of the drug loaded lipid in liquid nitrogen or ice Grinding in a powder mill (50-100mm particle) Dispersion of the lipid in the cold aqueous dispersion medium Solid lipid nanoparticle
  13. 13. 13 Advantages: 1)Low capital cost. 2)Demonstrated at lab scale. 1) Larger particle sizes & broader size distribution. 2) does not avoid thermal exposure but minimizes it. Disadvantages:
  14. 14. 2) Ultrasonication or 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: 1) Equipment used is very common 2) No temperature induced drug degradation Disadvantages: 1) Potential metal contamination 2) Broader particle size distribution ranging into micrometer range. 14
  15. 15. 15 3) Solvent emulsification-evaporation technique Drug + lipid are dissolved in water immiscible solvent (toluene, chloroform) Emulsification in aq. Phase o/w emulsion Solvent evaporation at room temp.& reduced pressure. Solid lipid nanoparticle
  16. 16. 16 Advantages: 1) Avoidance of any thermal stress. 2) Continuous process Disadvantages: 1) Use of organic solvents. 2) Extremely energy intensive process.
  17. 17. 17 4) Micro emulsion based method: Melting of lipid Add aq. Solution of drug to melted lipid Add surfactant & co-surfactant at temp.above the melting point of lipid Formation of clear w/o solution Formed w/o micro emulsion is added to mixture of water surfactant,& co-surfactant under mechanical stirring Formation of suspension of lipid particle Wash with dispersion medium by ultra-filtration system Solid lipid nanoparticle
  18. 18. 18 Advantages: 1) Low mechanical energy input. 2) Theoretical stability. Disadvantages: 1) Extremely sensitive to change. 2) Labor intensive formulation work. 3) Low nanoparticle concentration
  19. 19. 19 Can be prepared by Rapid Expansion of Supercritical Carbon dioxide solution methods(RESS) Carbon dioxide with 99.99% is good solvent. 5) By Using Supercritical fluid: Advantage:-  Solvent less processing.
  20. 20. 20 6) By Using Spray Drying Method: Spray drying method is a cheaper method than lyophilization. This method causes particle aggregation due to high temperature, shear forces and partial melting of the particle. The best result by spray drying method was obtained with SLN concentration of 1% in solution of trehalose in water or 20% trehalose in ethanol water mixture(10:90 v/v) Disadvantage:- particle aggregation due to high temperature, shear forces & partial melting of particles.
  21. 21. 21 [I] Measurement of particle size 1) Photon correlation spectroscopy 2) Transmission electron microscopy 3) Scanning electron microscopy [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. Characterization of SLNs:
  22. 22. 22 [III]Molecular weight  Gel chromatography  Atomic force microscopy [IV] Density  Helium compression pychnometry  Contact angle measurement
  23. 23. Routes of administration: 1. Parentral administration 2. Oral administration 3. Rectal administration 4. Nasal administration 5. Respiratory delivery 6. Ocular administration 7. Topical administration 23
  24. 24.  Solid lipid nanoparticle as potential new adjuvant for vaccines.  Solid lipid nanoparticles as a targeted carrier for anticancer drug to solid tumor.  Solid lipid nanoparticles for delivering peptides and proteins.  Solid lipid nanoparticles for targeted brain drug delivery.  Solid lipid nanoparticles for parasitic diseases.  Solid lipid nanoparticles for topical use.  Solid lipid nanoparticle applied to the treatment of malaria.  Solid lipid nanoparticles in tuberculosis disease.  SLN in cosmetic and dermatological preparations. Applications of SLN: 24
  25. 25. 25 Conclusion : Lipid particle drug delivery technology present considerable opportunities for improving medical therapeutics, but the technology potential remains unrealized. Their applicability in the encapsulation of various drug. In the number of research works has been successfully carried out in this area. It would result in a simultaneous improvement in the quality, efficacy, and safety profile of drug.
  26. 26. REFERENCES: 1) S. P. Vyas and R. K. Khar, Targeted and Controlled Drug Delivery System, 1st Edition, 2002, CBS Publication, PP.- 249-277. 2) N. K. Jain, Controlled and Novel Drug Delivery, 1st edition, 2001, Reprint 2003, CBS Publication, PP.- 408-423. 3) K. H. Ramteke, S. A. Joshi & S. N. Dhole, A review on Solid Lipid Nanoparticle, IOSR Journal Of Pharmacy, Vol-2, PP. 34-44. 4) P. Ekambaram, B. Abdul Hasan Sathali and K. Priyanka, Solid Lipid Nanoparticles: A Review, Scientific Review & Chemical Communications, PP.- 80-102. 5) Rahul Nair, K. S. Arun Kumar, K. Vishnu Priya, M. Sevukarajan, Recent Advances in Solid Lipid Nanoparticle Based Drug Delivery System, Journal of Biomedicine Science and research, Volume 3(2), 2011, PP.- 368-384 26
  27. 27. 27 Thank you

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