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Controlled drug release technology course

Mid term exam – Chemical Engineering Dept. FTUI


Given on Wednesday April 14. 2021 / Submit Friday April 16. 2021 (Google Classroom before 11.59 AM)
Lecturers: Elsa Krisanti, PhD and Prof. Kamarza Mulia, PhD

First problem
Up to now, your group have learned and discussed topics that belong to one of the following drug delivery
routes:
• transdermal/topical drug delivery
• implant drug delivery
• pulmonary/inhaled drug delivery
Now that you have some pretty good idea about controlled release of drugs and bioactive compounds, it is
the right time to organize the information as a concept map. Your concept map should include concepts/topics
(in boxes) and relationship between the concepts/topics (linking words). A good example is shown below:

Please prepare a concept map that covers all of the important concepts/topics related to the drug delivery
system assigned to your group. You could use a computer software such as Word or Visio to prepare the
concept map. Another option is to draw it manually and then scan the concept map.

Second problem
1. Define “biodegradation” and “biocompatibility” using your own words.
2. What are the advantages and disadvantages of bioactive compounds from herbs compared to synthetic
drugs produced by the pharmaceutical industry?
3. What advantages do controlled release formulations have over standard pharmaceutical drug
formulations? What is burst release? Do you think burst release of drugs as a phenomena that should be
avoided altogether in the treatment of patients? Would your answer depends on whether the patient has
a chronic or an acute disease?
4. Question only for group members 1/2/3: Can you propose the development of a transdermal delivery
system to utilize bioactive compounds that are widely available in Indonesia? State specifically the bioactive
compounds that will be used and their application. What should the skin-release system formulation
characterize you prefer?

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5. Question only for group members 4/5/6: Would you like to obtain a chitosan nanoparticle inhaler
formulation containing extracts of bioactive compounds to treat chronic obstructive pulmonary disease
(COPD). What are the important factors that need to be considered in order for your formulation to have
high efficacy?
6. Question only for group members 7/8/9: You would like to obtain implantable cardiovascular stents so
that cardiovascular surgery patients do not react with resistance, What are the properties you would expect
of the polymers used in controlled release formulations to combat inflammation caused by installation?

Third problem: Please choose only one option and then answer the given questions

Option 1: “Drug Release from PLGA Microspheres Attached to Solids Using Supercritical CO2 by Mulia et al.
(http://jba.sagepub.com/content/25/5/401). After reading this paper, please answer the following questions:
a) Could you explain the use of supercritical carbon dioxide as a plasticizer for PLGA?
b) Find data that shows the enhanced solubility of organic solvent organic solvents such as dichloromethane
in supercritical carbon dioxide. Is it similar to enhanced solubility of caffeine in supercritical carbon dioxide?
c) Explain why we need to avoid the present of residual organic solvents in PLGA.
d) Explain the effect of pressure of the supercritical carbon dioxide on the cumulative release of
dexamethasone
e) Do you think the release profile shown in Figure 3 is a zero-order release? Provide comments if such curves
already satisfy a sustained release conditons.
f) List the factors that affect the hydrolytic degradation of PLA and PLGA. Write down the reactions involved
in the degradation of PLA and PLGA.
g) What would happen if PLGA (50:50) used in this study were substituted by PLA (90:10)?

Option 2: “Nanoparticles that do not adhere to mucus provide uniform and long-lasting drug delivery to
airways following inhalation by Schneider et al. (https://advances.sciencemag.org/content/3/4/e1601556).
After reading this paper, please answer the following questions:
a) What are the research objectives stated in the paper?
b) Compare the characteristics of MAP against MPP. Provide the polymer/molecular structure of MAP and
MPP in your explanation.
c) Examine Figure 3 and explain if there is a significant finding based the data.
d) Examine Figure 4 and explain if there is a significant finding based the data.
e) In vivo efficacy comparison was carried out using DP-loaded biodegradable MPP and MAP. The authors
used F127 and F68 to produce MPP and MAP, respectively. Explain why, include the molecular structure of
F127 and F68 in your explanation
f) What do you think is the most important cintribution of the paper? Write down just one sentence using
your own words.

Option 3: “Design and evaluation of a novel transdermal patch containing diclofenac and teriflunomide for
rheumatoid arthritis therapy” Zhang et al, http://ees.elsevier.com/ajps/default.asp. After reading this paper,
please answer the following questions:
a) How do explain about Rheumatoid Arthritis, Non-steroidal anti-inflammatory drugs (NSAIDs) and how
NSAID help relieve RA pain?
b) Explain the background idea of transdermal delivery of NSAID such as Diclofenac (DIC) in this article?
c) What is the goal stated in this article? And explain the results of Amine-drug formation was detected by
DSC-FTIR analysis as shown in Figure 1 & 2.
d) How do you explain the cummulative permeation profile of DA-salts as shown in Figure 3? What is the
role of lipophilic enhancers added to this DA-salt as shown in Figure 4. Does the enhancer added
significantly improve the cumulative permeation amount Q24?
e) How do you explain the effect of addition of TEF on DA drug on anti-inflammatory activity using
transdermal patch? Does the matrix patch give effect on the adjuvant arthritis? When the use of this
transdermal show the reduced swelling.

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