Dr. Mohamed Ghobashy holds a PhD in radiation research of polymers from the National Center for Radiation Research and Technology (NCRRT) at the Atomic Energy Authority in Egypt. The document discusses the history of polymers from cellulose acetate in the 1800s to nylon in the 1930s. It also covers polymer degradation times ranging from months for cotton to over 100 years for glass bottles. The remainder of the document focuses on using suitable polymers to develop drug delivery systems for poorly soluble drugs, including various polymer coating and nanowire approaches as well as stimuli-responsive polymers.
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Suitable Polymer Suitable Drug Release
1. suitable polymer suitable drug
Dr. Mohamed Ghobashy (P.hD.)
B.SC 1999
M.SC 2007
P.hD. 2013
Radiation Research of Polymer Department
Nanotechnology and Hydrogel lab.
National Center for Radiation Research and Technology (NCRRT)
Atomic Energy Authority
NCRRTAEAE
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5. HOWLONGDOESITTAKE? POLYMERIC MATERIAL DEGRADATION TIME
Cotton rags 1-5 months
Paper 2-5 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 years
Nylon 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 512/25/2016
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6. Problem Description 1
6
• In 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)
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7. Problem Description 2
7
Drug levels in the blood with (a) traditional drug dosing and (b) controlled-delivery
dosing
SUB-ACUTE TOXICITY-
• Identify target organs
susceptible to drugs toxicity
• Three doses are used on two
animal species
• Animals maintained at the
max. tolerated doses for a
minimum period of 4 weeks
to a max. period of 3 months
• Finally ,the animals are killed
and subjected to
histopathological
examination.
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10. Polypeptide nanowire:
In a manner,
amino acids
combine
together in
chain by
formation of
peptide bond.
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11. DNA double nanowire:
Basic building block of
DNA is nucleotide, it is
a five member ring
deoxyribose with
phosphate group, a
nucleic acid base R.
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16. 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
Gas
Drug
Polymer Drug
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19. Surface erosion
(e.g., polyanhydrides)
– When the polymer is exposed to water hydrolysis occurs
– Hydrolysis degrades the large polymers into smaller biocompatible compounds
– These small compound diffuse from the interface of the polymer
– Loss of the small compounds reveals drug trapped within
– Note these polymer do not swell.
Add
water
Add
time
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20. Drug release by diffusion
• Early encapsulation and entrapment systems released the drug from within the polymer via molecular
diffusion
– When the polymer absorbs water it swells in size
– Swelling created voids throughout the interior polymer
– Smaller molecule drugs can escape via the voids at a known rate controlled by molecular
diffusion (a function of temperature and drug size)
Add
water
Add
time
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22. EUDRAGIT® Acrylic Drug Delivery
Polymers
poly(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 methacrylate 22
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23. No drug–polymer interactions were reported
when examined using FTIR
The anionic polymer protected the drug by preventing its gelling and clumping in situ, while the
nonionic polymer promoted gelling
Fan 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):1–10
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24. Crushed API beadlets in the pH 7.4 phosphate buffer solution, (a) Eudragit® L100
beadlets with exposed cores and (b) PVP® K30 beadlets exhibiting the characteristic gelling of
the amorphous API
No drug–polymer 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.)
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Fan 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):1–10
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25. 2512/25/2016
Fan 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):1–10
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26. 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 438:53–60
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27. Jennifer Dressman is Professor of
Pharmaceutical
Prof. Dr. Jennifer B. Dressman
Institute of Pharmaceutical Technology
Biocenter
Johann Wolfgang Goethe University
Max-von-Laue-Str.. 9
60438 Frankfurt am Main, GERMANY
dressman@em.uni-frankfurt.de
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(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
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Time(min.)
0 20 40 60 80 100 120
DrugRelase(mg)
0.00
0.05
0.10
0.15
0.20
0.25
0.30
0.35
Drug release amount from Fe3O4/PAAc/PVA loaded with
theophylline drug (○) no magnetic field (●) magnetic field
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34. Drug Release Measurement E.F.
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(1) Two Carbon Electrodes (2) Spring Wire (3)
Gel Spice
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36. 12/25/201636
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-AMPS36/38