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  1. 1. ABDUL MUHEEMM.Pharm, IInd sem.,Department of PharmaceuticsFaculty of Pharmacy,Jamia Hamdard 1
  2. 2. Content Definition Introduction Colloidal systems Formulation additives Commercial NEs Formulations Advantages Methods of preparation Techniques of preparation  High -pressure homogenization  Microfluidization  Phase inversion temperature technique  Titration method Characterisation of microemulsion Applications of nanoemulsion conclusion 2
  3. 3. Abbreviations NE- nanoemulsion SME-sub-micron emulsion o/w- oil in water w/o- water in oil PCMX –parachlorometaxylenol TEWL- trans epidermal water loss 3
  4. 4. Definition Nanoemulsions can be defined as oil-in-water (o/w) emulsions with mean droplet diameters ranging from 50 to 1000 nm. Synonyms: sub-micron emulsion and mini- emulsion. Usually SMEs contain 10 to 20 per cent oil stabilized with 0.5 to 2 per cent egg or soyabean lecithin. 4
  5. 5. Introduction NEs are a group of dispersed particles used for pharmaceutical and biomedical aids and vehicles that show great promise for the future of cosmetics, diagnostics, drug therapies, and biotechnologies Due to their small droplet size NEs possess stability against sedimentation or creaming with Ostwald ripening forming the main mechanism of NE breakdown. 5
  6. 6. • Internal structures depend on relative component amounts, concentrations and other characteristics.• The relative oil and water domains that form in nanoemulsion systems are usually so small (about 10-20 nm or less in diameter) that they do not scatter light. 6
  7. 7. Nanoemulsion: Lipid Liposome: Lipidmonolayer enclosing bilayer enclosing ana liquid lipid core. aqueous core. 7
  8. 8. Nanoemulsion versus a MicroemulsionMicroemulsion Nanoemulsion•Thermodynamically stable. •Kinetically stable•Comparatively long term stability •Do not possess long-term stability•Higher surfactant concentration •Requires a lower surfactant concentration for its formation•Less expensive then •Nanoemulsions are generallynanoemulsion expensive MJayne Lawrence and Warankanga Warisnoicharoen, Recent Advances in Microemulsions as Drug Delivery Vehicles (p-125), Nanoparticle as Drug Carriers, 2006 by Imperial College Press 8
  9. 9.  Nanoemulsions are transparent and slightly opalescent. 9
  10. 10. Formulation additives 10
  11. 11. A Typical Formulation 11
  12. 12. Advantages NEs have a much higher surface area and free energy than macro emulsions that make them an effective transport system. NEs do not show the problems of inherent creaming, flocculation, coalescence, and sedimentation, which are commonly associated with macroemulsions. NEs can be formulated in variety of formulations such as foams, creams, liquids, and sprays. 12
  13. 13. Advantages NEs are non-toxic and non-irritant, hence can be easily applied to skin and mucous membranes. Since NEs are formulated with surfactants, which are approved for human consumption (GRAS), they can be taken by enteric route. NEs do not damage healthy human and animal cells, hence are suitable for human and veterinary therapeutic purposes. 13
  14. 14. Significance Small droplet size large interfacial areaof smallerdropletSize. Rapid drug release Increased bioavailability Reduction in dose Better profiles of drug absorption Protection of drug(s) from the hostile environment of the body 14
  15. 15. Techniques of preparationa. High -pressure homogenizationb. Micro fluidizationc. Phase inversion temperature technique. 15
  16. 16. High -pressure homogenization This technique makes use of high-pressure homogenizer/pi ston homogenizer to produce NEs of extremely low particle size (up to 1nm) 16
  17. 17. MICROFLUIDIZATION: It involves the use of device that is micro fluidizer It uses high-pressure positive displacement pump of (500-20000)psi, which forces the product through the interaction chamber, which consists of small channels called “micro channels”. The product flows through the micro channels on to an impingement area resulting in very fine particles of submicron range. The two solutions (aq. Phase and oily phase) are combined together and processed to obtain a stable nanoemulsion. 17
  18. 18. Microfluidization 18
  19. 19. Phase Inversion Temperature technique. 19
  20. 20. Characterization of Nanoemulsion transmission electron microscopy, NE droplet size analysis, viscosity determination, refractive index, in vitro skin permeation studies, 20
  21. 21. Characterization ofNanoemulsion skin irritation test, in vivo efficacy study, thermodynamic stability studies, and surface characteristics. 21
  22. 22. Thermodynamic Stability Studies To overcome the problem of metastable formulation Selected formulations were centrifuged at 3500 rpm for 30 minutes Heating and cooling cycle Six cycles between refrigerator temperatures of 4°C and 45°C for 48 hours were done Freeze-thaw cycle test done for the formulations between –21°C and +25°C. 22
  23. 23. Droplet Size Analysis droplet size of the nanoemulsion is determined by photon correlation spectroscopy The formulation (0.1 mL) is dispersed in 50 mL of water Gently mix by inverting the flask. Measurement is done using a Zetasizer 1000 HS. Light scattering is monitored at 25°C at a 90° angle 23
  24. 24. Transmission ElectronMicroscopy The morphology and structure of the nanoemulsion the nanoemulsion formulation is diluted with water (1/100). A drop of the diluted nanoemulsion is directly deposited on the holey film grid and observed after drying 24
  25. 25. Viscosity Determination The viscosity of the formulations (0.5 g) can be determined without dilution using a Brookfield DV III ultra V6.0 RV cone and plate rheometer at 25 ± 0.5°C. one software used for the viscosity calculations is Rheocalc V2.6. 25
  26. 26. Applications of Nanoemulsions Use of nanoemulsions in cosmetics Antimicrobial nanoemulsions Prophylactic in bio-terrorism attack Nanoemulsions as a mucosal vaccines Nanoemulsion as non-toxic disinfectant cleaner 26
  27. 27. Applications ofNanoemulsions Nanoemulsion in the treatment of various other disease conditions Nanoemulsion formulations for improved oral delivery of poorly soluble drugs Nanoemulsions as a vehicle for transdermal delivery Self-nanoemulsifying drug delivery systems 27
  28. 28. Applications ofNanoemulsions Nanoemulsions in cell culture technology Nanoemulsion in cancer therapy and in targeted drug delivery Solid self-nanoemulsifying delivery systems as a platform technology for formulation of poorly soluble drugs 28
  29. 29. Nanoemulsion as non-toxicdisinfectant cleaner The disinfectant formulation is made up of nanospheres of oil droplets #106 mm that are suspended in water to create a NE requiring only miniscule amounts of the active ingredient, PCMX (parachlorometaxylenol). The nanospheres carry surface charges that efficiently penetrate the surface charges on microorganisms membranes-much like breaking through an electric fence. Rather than "drowning" cells, the formulation allows PCMX to target and penetrate cell walls. As a result, PCMX is effective at concentration levels 1-2 orders of magnitude lower than those of other disinfectants; hence, there are no toxic effects on humans, animals, or the environment. 29
  30. 30. Nanoemulsions as a mucosalvaccines Used to deliver either recombinant proteins or inactivated organisms to a mucosal surface to produce an immune response. An influenza vaccine and an HIV vaccine, can proceed to clinical trials. The NE causes proteins applied to the mucosal surface to be adjunted and it facilitates uptake by antigen-presenting cells. This results in a significant systemic and mucosal immune response that involves the production of specific IgG and IgA antibody as well as cellular immunity. 30
  31. 31. Antimicrobialnanoemulsions The NE has a broad-spectrum activity against bacteria (e.g. E. coil, Salmonella, S. aureus), enveloped viruses (e.g. HIV, Herpes simplex), fungi (e.g. Candida, Dermatophytes), and spores (e.g. anthrax). The NE particles are thermodynamically driven to fuse with lipid-containing organisms. 31
  32. 32. Prophylactic in bio-terrorismattack 32
  33. 33. Use of nanoemulsions incosmetics NEs support the skin penetration of active ingredients and thus increase their concentration in the skin. Another advantage is the small-sized droplet with its high surface area allowing effective transport of the API to the skin. Have own bioactive effects. This may reduce the trans- epidermal water loss, indicating that the barrier function of the skin is strengthened. NEs are acceptable in cosmetics because there are no inherent creaming, sedimentation, flocculation, or coalescence that are observed with macroemulsions. 33
  34. 34. Fluorine-containingnanoemulsions for MRI celltracking•cells of interest are labeled in culture using a perfluorocarbon nanoemulsion•Labeled cells are introduced into a subject and tracked using 19F MRI or NMRspectroscopy•widely applied to studies of inflammation, cellular regenerative medicine, andimmunotherapy. 34
  35. 35. Nanoemulsions as a vehicle fortransdermal delivery  Low systemic absorption  Site-specificity and increased drug levels at injured tissues  Reduced toxicity  Improved pharmacological activity 35
  36. 36. Parenteral Delivery In order to increase the solubility of the drug, To reduce drug toxicity, To reduce hypersensitivity, To reduce pain upon injection, Formulated as long circulating vehicles, Control the release rate, As drug targeting agents, Alternative formulation to long circulating vesicles, On the basis of their small size avoiding uptake by the RES, Their stability and their ease of preparation. 36
  37. 37. How the top 10 big pharmaceutical companies rank in termsof number of nano-related patents. 37
  38. 38. Commercial NEs Formulations 38
  39. 39. Conclusion NE formulations offer several advantages for the delivery of drugs, biologicals, or diagnostic agents. Several other products for drug delivery applications such as Diprivan® (propofol, astra zeneca) and Ropion® (flurbiprofen) have also reached the marketplace. NEs are chiefly seen as vehicles for administering aqueous insoluble drugs, as colloidal carriers for targeted delivery of various anticancer drugs, photosensitizers, neutron capture therapy agents, or diagnostic agents. Because of their submicron size, they can be easily targeted to the tumor area. Research with perflurochemical NEs has shown promising results for the treatment of cancer in conjugation with other treatment modalities and targeted delivery to the neovasculature. It is expected that further research and development work will be carried out in the near future for clinical realization of these targeted delivery vehicles. 39
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  42. 42. INTRODUCTION 42
  43. 43. MATERIALS 43
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  51. 51. References:1. Jia Xi, Qi Chang, Chak K. Chan et al, Formulation Development and Bioavailability Evaluation of a Self- Nanoemulsified Drug Delivery System of Oleanolic Acid. AAPS PharmSciTech, Vol. 10, No. 1, March 2009 (# 2009).2. Nicolas Anton & Thierry F. Nano-emulsions and Micro- emulsions: Clarifications of the CriticalDifferences Shah P, Bhalodia D, Shelat P. Nanoemulsion: A pharmaceutical review. Syst Rev Pharm [serial online] 2010 [cited 2011 Mar 16];1:24-32. Available from: 9509 51
  52. 52. Thank You 52