‫منــارة التعلــيم الصــيدلي فـــي مصــر ومحيطــها اإلقليـــمي‬

‫أول كلية صيدلة معتمدة من الهيئة القومية لضمان جودة التعليم واالعتماد‬

Students working in Groups

Student (1) Name: ‫طارق محمود سعداوى محمد‬

Student (1) ID: 30279

National ID/ Passport number: 29811142403339

Student Email: Tarek.mah.saadawy@std.pharma.cu.edu.eg

Student (2) Name: ‫عبدالرحمن احمد دهشان عبدالعال‬

Student (2) ID: 30281
National ID/ Passport number: 29901092102072

Student Email: abdelrahman.ahm.dahshan@std.pharma.cu.edu.eg

Student (3) Name: ‫عبدالرحمن حسن محمد عبدالرحمن‬

Student (3) ID: 30284

National ID/ Passport number: 30002082102393

Student Email: abdelrahman.has.mohamed@std.pharma.cu.edu.eg

Student (4) Name: ‫عبدالرحمن محمد سعيد عبدالعزيز‬

Student (4) ID: 30286

National ID/ Passport number: 29902060102476

Student Email: Abdelrahman.moh.saeed@std.pharma.cu.edu.eg

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Student (5) Name: ‫عبدالرحمن مصطفى عبدالذاكر احمد‬
Student (5) ID: 30287
National ID/ Passport number: 29908140100731

Student Email: abdelrahman.mou.abdelzakir@std.pharma.cu.edu.eg

Student Level: Third Year

Course Name: Pharmaceutics IV

Course Code: 110

Title of Research: Radiopharmaceuticals diagnostic and therapeutic

applications.

Role of each student:

Student (1): Data summarization.

Student (2): Data summarization & word.

Student (3): Data reviewer.

Student (4): Data collection.

Student (5): Data collection.

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-Radiopharmaceuticals diagnostic and therapeutic applications:

Introduction:

-Radiopharmaceuticals are a group of radioactive drugs composed of

radionuclides which are used in diagnosis and therapy. [11][6]

-Several Radiopharmaceuticals are approved by the FDA and others undergo

clinical trials. [12]

-They are administered mainly by systemic route but they localize in specific
tissues which gives these agents high specificity so quality control aspects and
sterility must be monitored. [11] [12]

-Compounds that are used for diagnosis mainly emit beta particles or gamma
rays while therapeutic compounds mainly emit alpha particles. [11]

Diagnostic applications:

There are many methods or applications for Diagnosis such as [13] [8]:

1-isotope dilution 4-Scanning technique

2-rate of isotope disappearance 5- isotope concentrations

3- metabolic rate 6- Rate of isotope transfer

1-Isotope dilution: One of the most useful radioactive method for diagnosis is
isotope dilution ID.

Procedure of ID [17]:

1-Adding a known amount of radioisotope of the element to the substance.

2- mix with the stable isotope of the element.

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3-analyze the sample and compare between the radioactive isotope and the
stable one.

Application of ID [7]:

IDA can be used in determination of blood volume by using of 51Cr in clinical

practice, and the technique depends on extraction of blood, then mixed with
51
Cr then reinjected, extract the blood labelled with 51Cr again and because of its
stability the blood volume can be measured.

2-Rate of isotope disappearance: rate at which an isotope disappears from the

tissue to determine the circulation in this tissue [9].

Application of disappearance rate [9]:

Determination of disappearance rate of 133Xenon, 4-Iodo-antipyrine-131I

and 131I from Skeletal Muscles in case of rest and hyperaemia.

At rest: the ratio between 133Xe and 131I for [<70 years] is 0.78 and [>70years]
is 0.59.

At hyperaemia: the ratio between removal rates of 133Xe and 131I increased
from 0.94 at rest to 1.98 during hyperaemia.

So at high blood flow the removal rate of 131I decreased.

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3-Metabolic rate [13]: indicates the concentration of radioisotopes in normal
and abnormal case.

Application on metabolic rate [12] [13]:

Since 1954 131I rose Bengal has been used to study liver function, and to
differentiate among various hepatobiliary conditions.

In normal: The ratio 20/5 min of plasma activity after the injection is 0.51

If the ratio is higher than 0.51, that indicates low liver function.

Application 2: determination of thyroid function by rate of 131I deposition.

Procedure [13]:

1-Taking 5-25 mc of 131NaI.

2-After 24 hours measure radioactivity of thyroid against 131NaI standard kept in

vitro.

3-Calculate the 131I uptake

• 1-(15%) indicates hypothyroidism &myxedema

• 2- (35-40%) is normal
• 3-(50%)indicates hyperthyroidism

4-Scan technique:

Radionuclide scan (radioisotope scan) is an imaging technique used to check

parts of the body by injecting a small dose of a radioactive chemical into the
body and using of gamma camera .it can detect cancer, trauma, infection or
other disorders.
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According to the isotope used in diagnosis, this isotope is localised in a target
organ.

Application on scanning technique (brain scanning) [16]:

It is used to determine any abnormality in the brain and it depends on the

tendency of isotope to concentrate in tumours
and lesions.

The isotope is injected or taken orally,

Travels to blood stream to the target organ.

Fig1.Brain scanning technique

Procedure [16]:

1-Injection of a radioactive isotope (such as technetium-99Tc or 131I) into a

blood vessel that supplies the brain.

2-As the substance becomes localized within the brain, it emits gamma rays.

3-Measure the concentration of the rays by movable radiation detection device

which can reveal the presence, the shape, and often the size of the intracranial
abnormality.

Therapeutic applications:

1-Cobalt 60 (60Co): it’s a radioactive isotope which is used to sterilize food

and medical equipment due to its ability to destroy some living organisms when
it’s directed to an area with a particular radiation dose, so this ability is used in
nuclear medicine to treat some types of carcinomas in many parts in the body,
e.g. prostatic carcinoma [5]
-The machine directing 60Co to the body has anterior & posterior portals that
6

radiate 60Co against each other like cross firing [5]

Page
-In case of prostatic carcinoma, these portals are centered in the midline of the
pelvis & start to radiate the dose [5]

2-Gold 198 (198Au): radioactive gold nanoparticles (AuNP) are showing

promising results in the matter of cancer therapy [2]
-There is a variety of methods to use gold nanoparticles in cancer treatment, but
the most common ones are chemotherapy, radiotherapy & hyperthermia method
(injecting a dose of gold nanoparticles to the tumor & the surrounding tissues,
and then exposing the area of the tumor to high temperature to break the bonds
between the gold nanoparticles & this affect the tumor badly) [3]
-These methods have been tested to treat prostate cancer in animals & it showed
promising results which give us a big hope to use them as a new therapy to treat
human cancer [2]
-The dose required to distribute in the tumor & its surrounding tissues is
calculated by Monte-Carlo N-Particle code (MCNP-6.1.1 code) [2]

3-Iridium 192 (192Ir): it’s a radioactive isotope that has destructive abilities to
tumor cells when it’s used by brachytherapy method (branch of radiation
therapy that uses a high dose rate method), so it has been used to help in treating
types of skin cancer by being implanted near the tumor site [10].
-For example, squamous cell carcinomas can be treated better by a combination
of external beam radiation therapy to tumor site & iridium implant near the
tumor site [10]
-The mechanism of implanting iridium is by placing it into flexible plastic tubes
or hard needles & injecting the plastic tubes (or needles) near the tumor site,
and then the iridium will leak out of the plastic tubes (or needles) to deliver the
calculated radiation dose [4].
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4-Iodide 131 (131I): stable iodide ion is very important to the thyroid gland
because it facilitates thyroid hormone biosynthesis [1]
-In case of differential thyroid cancer (DTC), the transporter that transport
iodide ion into the thyroid gland (sodium iodide symporter) is damaged & this
results in abnormal rates of thyroid hormone biosynthesis [1 ]
-The treatment to the DTC was by thyroidectomy surgery & replacement with
thyroid hormone. But recently, the nuclear medicine has proved that supplying
radioactive iodine (131I) after the surgery results in higher cure rate, lower
recurrence & longer survival [15]

5-Phosphorous 32 (32P): it’s one of the earliest known radioactive isotopes.

-It emits high-energy beta particles with a maximum tissue penetration of 8mm
& a half-life of 14.28 days & because of that, it has been used to treat tumors
(e.g. ovarian cancer) & in the treatment of polycythemia vera by being injected
as intraperitoneal infusion [14]
-It’s also can be injected intravenously for palliation of bone pain [14]

Conclusion:

-Radiopharmaceuticals have countless applications whether therapeutic or

diagnostic.

-Diagnostic applications include many techniques such as: isotope dilution, rate
of isotope disappearance, rate of isotope transfer and scanning technique which
can be used to evaluate the body functions such as liver, thyroid, brain, etc…

-Many radioactive elements can be used on purpose of therapy such as Cobalt

for prostatic carcinoma, Gold for different tumors, Iridium for skin cancer,
Iodide for differential thyroid cancer and Phosphorus for polycythemia
8
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References:

1- Al-Rasheed, M. M., Alzahrani, A. S., Macadam, A., Overall, A., Gard, P., &
Dzimiri, N., eds., The potential role of the sodium iodide symporter gene
polymorphism in the development of differentiated thyroid cancer, Gene,
November 2015, volume 572, issue 2, pages163-168.

2- Al-Yasiri, A.Y., White N.E., Katti, K.V., Loyalka, S.K., eds., Estimation of
tumor and local tissue dose in gold nanoparticles radiotherapy for prostate
cancer, Reports of practical oncology & radiotherapy, May-June 2019, volume
24, issue 3, pages 288-293.

3- Beik, J., Khateri, M., Khosravi, Z., Kamrava, S.K., Kooranfir, S., Ghaznavi,
H., Shakeri-Zadeh, A., eds., Gold nanoparticles in combinatorial cancer therapy
strategies, Coordination chemistry reviews, May 2019, volume 387, pages 299-
324.
4- Crook, J., Mazeron, J., Marinello, G., Raynal, M., Huart, J., Leung, S., …
Pierquin, B., eds., Interstitial iridium 192 for cutaneous carcinoma of the
external nose, International Journal of Radiation Oncology*Biology*Physics,
January 1990, volume 18, issue 1, pages 243-248.
5- Dykhuizen, R.F., Sargent, C.R., George, F.W., Kurhara, S.S., eds., The use of
cobalt 60 in the treatment of prostatic carcinoma, the journal of urology,
September 1968, volume 100, issue 3, pages 333-338.
6- Elisa Crestoni, M. (2018) ‘Radiopharmaceuticals for Diagnosis and
Therapy’, in Reference Module in Chemistry, Molecular Sciences and Chemical
Engineering. doi: 10.1016/b978-0-12-409547-2.14205-2.
7- Fassett,J.D., Isotopic and nuclear analytical techniques in biological systems:
A critical study-X. Elemental isotope dilution analysis with radioactive and
stable isotopes (Technical Report),Pure and Applied Chemistry ,Jan 1995

8- Lah, W., Journal of the Pharmaceutical Society of Korea 20 (2), 47-61, 1976

9- Lindbjerg, I. F. Disappearance Rate of 133Xenon, 4-Iodo-antipyrine-131I

and 131I-from Human Skeletal Muscles and Adipose Tissue. Scand. J. clin.
9
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Lab. Invest. 19, 120-128, 1967

10- Mazeron, J.-J., Belkacemi, Y., Simon, J.-M., Pechoux, C. L., Martin, M.,
Haddad, E., … Pierquin, B., eds., Place of iridium 192 implantation in definitive
irradiation of faucial arch squamous cell carcinomas, International Journal of
Radiation Oncology*Biology*Physics, September 1993, volume 27, issue 2,
pages 251-257.
11- Munjal A, Gupta N. Radiopharmaceuticals. [Updated 2020 Feb 1]. In:
StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2020 Jan

12- Nordyke,R.A., Metabolic and physiologic aspects of 131i rose bengal in

studying liver function, Seminars in nuclear medicine 2 (2), 157-166, 1972

13- Pharmaceutics lectures for third year, fopcu, 2019-2020

14- Phosphorus 32. Retrieved May 29, 2020, from

https://www.sciencedirect.com/topics/medicine-and-dentistry/phosphorus-32

15- Ravishankar, U., Pande, S., & Savita, N., eds., I-131 In the Management of
Differentiated Thyroid Cancer – an Update on Current Recommendations and
Practices, Apollo Medicine, December 2009, volume 6, issue 4, pages 347-354.
16- The editors of Encyclopaedia Britannica, Brain scanning, October 16,2015.

17- The editors of Encyclopaedia Britannica, Isotope dilution, [date accessed]

28May,2020.

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