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Polymers for Transdermal Delivery Systems

Polymers for Transdermal Delivery Systems. EMAC 276 Brian Cheung, Connie Chien, Corinne Nelson, Michelle Song, Xiaoxin (Shawn) Zhu. History . First approved in 1979 3-day patch for motion sickness in astronauts Became popular in 1990s with nicotine patch

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Polymers for Transdermal Delivery Systems

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  1. Polymers for Transdermal Delivery Systems EMAC 276 Brian Cheung, Connie Chien, Corinne Nelson, Michelle Song, Xiaoxin (Shawn) Zhu

  2. History • First approved in 1979 • 3-day patch for motion sickness in astronauts • Became popular in 1990s with nicotine patch • Currently used for birth control, glucose monitoring, local anesthesia, etc

  3. Mechanism - only a couple hundred Daltons • heavily favor lipids and require doses of milligrams per day or less - hard for hydrophilic drugs to pass through

  4. Components of TDD • Matrix-formers • Permeation enhancers • Rate-controlling membrane • Pressure-sensitive adhesives (PSAs) • Backing laminate • Release liner

  5. Requirements for Rate Controlling Membrane • Biocompatible • Highly dependent on the solubility of drug • Easy control of composition and thickness

  6. Polymeric Materials for Rate Controlling Membrane Ethylene-Vinyl Acetate (EVA) • Permeability can be altered by adjusting vinyl-acetate content • VA group leads to better solubility and diffusivity of polar groups • Cost of Material: $1.6-1.7 per kilogram

  7. Polymeric Materials for Rate Controlling Membrane Silicone Rubber: • Good Biocompatibility, ease of fabrication • Free rotation around silicone rubber backbone induce high permeability • Cost of Material: $4.8-5.5 per kilogram • http://www.pharmtech.com/pharmtech/data/articlestandard/pharmtech/192002/18600/article.pdf

  8. Polymeric Materials for Rate Controlling Membrane Polyurethanes: • Condensation of polyisocyanates and polyols • PU is suitable for hydrophilic polar compounds • Cost of Material: $2.2-2.5 per kilogram http://upload.wikimedia.org/wikipedia/commons/c/ca/Polyurethane.png

  9. Natural Polymer for Rate-Controlling Membranes - Chitosan Natural polymers can potentially reduce the skin irritation or allergic reactions induced by synthetic polymers Formed by deacetylation of chitin Thacharodi, D., and K. P. Rao. "Development and in Vitro Evaluation of Chitosan-based Transdermal Drug Delivery Systems for the Controlled Delivery of Propranolol Hydrochloride." Biomaterials 16 (1995): 145-48. Web. 8 Apr. 2012. <http://ac.els-cdn.com/014296129598278M/1-s2.0-014296129598278M-main.pdf?_tid=e7b31de07a5a1327b75f97ed19d36784&acdnat=1333947017_b278c0e1000399a40ac69074daeac121>.

  10. Requirements for PSAs 1. Adhere easily 2. Permanently tacky 3. Does not cause instability of the a. drug b. enhancer, and c. adhesive 4. Does not leave residue when peeled off

  11. Polymeric Materials in Pressure Sensitive Adhesives Polyisobutylene: • Mix of low and high molecular weights • Fillers are used for reinforcement, reducing viscosity and cost • Cost of Material: $1-100 per kilogram • http://www.pharmtech.com/pharmtech/data/articlestandard/pharmtech/192002/18600/article.pdf

  12. Polymeric Materials in Pressure Sensitive Adhesives Polyacrylates: • Amorphous and water-clear color in solution • Stability toward aging • Great resistance to acidic and alkaline hydrolysis and UV degradation • Cost of Material: $3.2-4.5 per kilogram • http://www.pharmtech.com/pharmtech/data/articlestandard/pharmtech/192002/18600/article.pdf

  13. Polymeric Materials in Pressure Sensitive Adhesives Silicones: • Stable adhesive in throughout a wide range of temperature (-73 to 250C) • Outstanding combination of bicompatibility and ease of fabrication for hydrophilic drugs • Poor solubility, permeability and releasing property • Cost of Material: $6.2-8.3 per kilogram • http://www.pharmtech.com/pharmtech/data/articlestandard/pharmtech/192002/18600/article.pdf

  14. Laminates • Layer of protective material • Chemical Resistance is the most important factor • It keeps the medication from seeping out of the patch • Good chemical resistance: • Low modulus • High flexibility • Good oxygen transmission • High moisture vapor transmission rate

  15. Requirements for Laminates • Relatively Inert • Increase hydration of the skin • Make sure that any polymers used do not irritate the skin

  16. Polymers used for Laminate Polyethylene Vinyl Polyester

  17. Release Liner • Protects the skin contacting adhesive • It is removed immediately before being placed on the skin • More a part of the packaging material than the actual patch itself • Made of Polyethylene or PVC and Silicone or Teflon • Cross linking may occur • Increase force to remove liner from patch

  18. Silicone PVC Teflon

  19. Problems • Only small-sized molecules delivery (very thick stratum corneum) • Difficult balancing the degree of damage and penetration

  20. Future development • Electroporation • Cavitational ultrasound • Thermal ablation • Microdermabrasion • Biochemical enhancer • Chemical enhancer combination • Microneedles http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2700785/

  21. Chemical enhancer combination SLS + phenyl piperazine + http://en.wikipedia.org/

  22. Microneedles S. H. Bariya, M. C. Gohel, T. A. Mehta, and O. P. Sharma, "Microneedles: An Emerging Transdermal Drug Delivery System," Journal of Pharmacy and Pharmacology, 64(1), 11-29 (2012).

  23. Questions?

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