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suitable polymer suitable drug

Dr. Mohamed Ghobashy (P.hD.)B.SC 1999M.SC 2007P.hD. 2013

Radiation Research of Polymer DepartmentNanotechnology and Hydrogel lab.National Center for Radiation Research and Technology (NCRRT) Atomic Energy Authority

NCRRTAEAE1/3812/25/2016

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polymer

Giulio Natta (Nobel prize 1963)Cellulose acetate

2Charles Goodyear1800-1860

Thomas Hancock (1786-1865)History of polymers12/25/2016History of polymersHistory of polymersHistory of polymersHistory of polymersHistory of polymersHistory of polymers2/38

polyglaspolymer

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Wallace Hume CarothersPolyamides 6,6189619381937

Wallace Hume CarothersPolyamides 6,6189619381937NO RUN(NURON)NILLONNYLON

Polyamides 6,6Wilmington (Delaware)312/25/2016

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sericinpolymer

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412/25/20164/38

Resilin elastin collagenspolymer

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HOW LONG DOES IT TAKE?POLYMERIC MATERIALDEGRADATION TIMECotton rags1-5 months Paper2-5 months Rope 3-14 months Orange peels 6 months Wool socks 1 to 5 years Cigarette butts 1 to 12 years Plastic coated paper milk cartons 5 years Plastic bags 10 to 20 yearsNylon fabric 30 to 40 years Aluminum cans 80 to 100 years Plastic 6-pack holder rings 450 years Glass bottles 1 million years Plastic bottles May be never

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Problem Description 16In recent years, there is increased number of active pharmaceutical ingredients with high therapeutic activity, but very low water solubility. Thus, a great challenge for pharmaceutical technology is to manufacture successful formulations and efficient drug delivery systems to overcome these dissolution problems. In case of poorly water soluble drugs, dissolution is the rate limiting step in the process of drug absorption. So, bioavailability problems are associated with extremely hydrophobic drugs (aqueous solubility < 0.1 mg / ml at 370C) 12/25/2016

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Problem Description 27

Drug levels in the blood with (a) traditional drug dosing and (b) controlled-delivery dosing SUB-ACUTE TOXICITY-

Identify target organs susceptible to drugs toxicityThree doses are used on two animal speciesAnimals maintained at the max. tolerated doses for a minimum period of 4 weeks to a max. period of 3 monthsFinally ,the animals are killed and subjected to histopathological examination.12/25/20167/38

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12/25/2016Polymer chose8/38

Same shape

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globulinpolymer

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Polypeptide nanowire:In a manner, amino acids combinetogether in chain by formation ofpeptide bond.

1012/25/201610/38

DNA double nanowire:Basic building block ofDNA is nucleotide, it isa five member ringdeoxyribose withphosphate group, anucleic acid base R.

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Types of polymerNeutral BasicAcidicAmphiphilic

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Crystanility of polymer13/38

Crystanility of polymer1412/25/201614/38

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Wurster processing (1949)The Wurstur process is essentially a coating process applied after a drug core is formed.The polymer shell is applied via spraying while the drug cores (liquid or solid) is suspended and recirculated in a gas stream

GasDrugPolymer

Drug

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Electrospinning Process12/25/201617

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Electrospinningpolymer

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Surface erosion(e.g., polyanhydrides)When the polymer is exposed to water hydrolysis occursHydrolysis degrades the large polymers into smaller biocompatible compoundsThese small compound diffuse from the interface of the polymerLoss of the small compounds reveals drug trapped withinNote these polymer do not swell.

AddwaterAddtime

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Drug release by diffusionEarly encapsulation and entrapment systems released the drug from within the polymer via molecular diffusionWhen the polymer absorbs water it swells in sizeSwelling created voids throughout the interior polymerSmaller molecule drugs can escape via the voids at a known rate controlled by molecular diffusion (a function of temperature and drug size)

Addwater

Addtime

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Stimuli Responsive22/38

EUDRAGIT Acrylic Drug Delivery Polymerspoly(meth)acrylates for pharmaceutical applications, which are known worldwide in the industry under the trade name EUDRAGIT.UDRAGIT S 100

methacrylic acic and methyl methacrylate.EUDRAGIT E 100

dimethylaminoethyl methacrylate, butyl methacrylate, and methyl methacrylate22

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No drugpolymer interactions were reportedwhen examined using FTIRThe anionic polymer protected the drug by preventing its gelling and clumping in situ, while the nonionic polymer promoted gellingFan et al. (2009)Fan C, Pai-Thakur R, Phuapradit W, Zhang L, Tian H, Malick W, Shah N, Kislalioglu MS (2009) Impact of polymers on dissolution performance of an amorphous gelleable drug from surfacecoated beads. Eur J Pharm Sci 37(1):1102312/25/201624/38

Crushed API beadlets in the pH 7.4 phosphate buffer solution, (a) Eudragit L100beadlets with exposed cores and (b) PVP K30 beadlets exhibiting the characteristic gelling of the amorphous APINo drugpolymer interactions were reported when examined using FTIR, implying that this factor did not play a role in the differences observed in the release profiles. The anionic polymer protected the drug by preventing its gelling and clumping in situ, while the nonionic polymer promoted gelling (Fig). On the other hand, gelling, clumping, and agglomeration were observed on the surface of the particles coated with PVP K30 which resulted in slow and incomplete release of the drug. From the anionic polymer coating, greater than 90% drug was dissolved in 50 min, whereas the nonionic polymer coating released 60% drug in 5 h (Fig.)

2412/25/2016Fan et al. (2009)Fan C, Pai-Thakur R, Phuapradit W, Zhang L, Tian H, Malick W, Shah N, Kislalioglu MS (2009) Impact of polymers on dissolution performance of an amorphous gelleable drug from surfacecoated beads. Eur J Pharm Sci 37(1):11025/38

2512/25/2016Fan et al. (2009)Fan C, Pai-Thakur R, Phuapradit W, Zhang L, Tian H, Malick W, Shah N, Kislalioglu MS (2009) Impact of polymers on dissolution performance of an amorphous gelleable drug from surfacecoated beads. Eur J Pharm Sci 37(1):11026/38

microprecipitated bulk powder polymer

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Shah et al. 2012)Shah N, Sandhu H, Phuapradit W, Pinal R, Iyer R, Albano A, Chatterji A, Anand S, Choi DS, Tang K, Tian H, Chokshi H, Singhal D, Malick W (2012) Development of novel microprecipitated bulk powder technology for manufacturing stable amorphous formulations of poorly soluble drugs. Int J Pharm 438:5360

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Jennifer Dressmanis Professor of PharmaceuticalProf. Dr. Jennifer B. DressmanInstitute of Pharmaceutical TechnologyBiocenterJohann Wolfgang Goethe UniversityMax-von-Laue-Str.. 960438 Frankfurt am Main, GERMANYdressman@em.uni-frankfurt.de

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vitro study29/38

In vitro study

polymer

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self-emulsification29

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Schematic diagramof a multiple-stepin vitrodigestionmodel to simulate the whole of the GI tract.

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My Studies On Drug Release

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12/25/201632(1) Coil (2) Water Inlet (3) Water Outlet (4) Sample (5) Closed Test Tube (6) Water Madium

Apparatuses to Study The Effect of Magnetic Field on Drug Release 33/38

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Drug release amount from Fe3O4/PAAc/PVA loaded with theophylline drug () no magnetic field () magnetic field

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Drug Release Measurement E.F.12/25/201634

(1) Two Carbon Electrodes (2) Spring Wire (3) Gel Spice35/38

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Electro-controlled release of theophylline from AMPS/AAc hydrogel by switching the applied electric field on and off.36/38

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Liner relation between the amount of loss water by deswelling and the amount of drug release under effect of 1 DC volt in water medium for (75-25)AAc-AMPS 36/38

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