Hollow microparticles as superior carriers for encapsulation and delivery of biomolecules

Bioactive molecules like peptides and proteins have gained significant attention in the field of therapeutics due to their exquisite specificity to their targets resulting in greater effective potency, reduced therapeutic dose and side effects. However, their low systemic stability and short half-li...

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Bibliographic Details
Main Author: Kharel, Sharad
Other Authors: Loo Say Chye Joachim
Format: Thesis
Language:English
Published: 2018
Subjects:
Online Access:http://hdl.handle.net/10356/73864
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author Kharel, Sharad
author2 Loo Say Chye Joachim
author_facet Loo Say Chye Joachim
Kharel, Sharad
author_sort Kharel, Sharad
collection NTU
description Bioactive molecules like peptides and proteins have gained significant attention in the field of therapeutics due to their exquisite specificity to their targets resulting in greater effective potency, reduced therapeutic dose and side effects. However, their low systemic stability and short half-life limits their potential. To overcome these problems, biodegradable polymer microparticles composed of polyester such as PLGA have been extensively used as carriers for delivery. However, they suffer from major limitations such as incomplete release and loss in bioactivity of the encapsulated biomolecules. Therefore, the overall objective of this thesis is to develop a method to fabricate hollow microparticles through an easy one-step method and validate the hollow microparticles as superior carriers for encapsulation and delivery of biomolecules. A method was developed wherein emulsion solvent evaporation technique was modified by adding osmogen into the oil phase before emulsification to fabricate hollow microparticles. The results obtained show conclusive evidence that by simply altering the amounts of osmogen in the formulation, the shell thickness and volume space of hollow cavity could be easily controlled. This was found to be an effective means to control and fine-tune the release kinetics of biomolecules to overcome the issue of incomplete release as observed in solid microparticles. It was found that by changing the particle morphology to hollow, the accumulation of polymer degradation products could be significantly reduced. This helped in reduction of acidic microenvironment in the microparticles, which decreased polymer-biomolecule adsorption. Consequently, the release of biomolecules from the microparticles was improved over solid microparticles. Furthermore, the bioactivity of encapsulated biomolecules was also preserved better in the hollow microparticles. It was thus established that hollow microparticles are superior over solid microparticles for delivery of biomolecules.
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spelling ntu-10356/738642023-03-04T16:46:55Z Hollow microparticles as superior carriers for encapsulation and delivery of biomolecules Kharel, Sharad Loo Say Chye Joachim School of Materials Science & Engineering DRNTU::Engineering::Materials::Biomaterials Bioactive molecules like peptides and proteins have gained significant attention in the field of therapeutics due to their exquisite specificity to their targets resulting in greater effective potency, reduced therapeutic dose and side effects. However, their low systemic stability and short half-life limits their potential. To overcome these problems, biodegradable polymer microparticles composed of polyester such as PLGA have been extensively used as carriers for delivery. However, they suffer from major limitations such as incomplete release and loss in bioactivity of the encapsulated biomolecules. Therefore, the overall objective of this thesis is to develop a method to fabricate hollow microparticles through an easy one-step method and validate the hollow microparticles as superior carriers for encapsulation and delivery of biomolecules. A method was developed wherein emulsion solvent evaporation technique was modified by adding osmogen into the oil phase before emulsification to fabricate hollow microparticles. The results obtained show conclusive evidence that by simply altering the amounts of osmogen in the formulation, the shell thickness and volume space of hollow cavity could be easily controlled. This was found to be an effective means to control and fine-tune the release kinetics of biomolecules to overcome the issue of incomplete release as observed in solid microparticles. It was found that by changing the particle morphology to hollow, the accumulation of polymer degradation products could be significantly reduced. This helped in reduction of acidic microenvironment in the microparticles, which decreased polymer-biomolecule adsorption. Consequently, the release of biomolecules from the microparticles was improved over solid microparticles. Furthermore, the bioactivity of encapsulated biomolecules was also preserved better in the hollow microparticles. It was thus established that hollow microparticles are superior over solid microparticles for delivery of biomolecules. Doctor of Philosophy (MSE) 2018-04-17T07:46:22Z 2018-04-17T07:46:22Z 2018 Thesis Kharel, S. (2018). Hollow microparticles as superior carriers for encapsulation and delivery of biomolecules. Doctoral thesis, Nanyang Technological University, Singapore. http://hdl.handle.net/10356/73864 10.32657/10356/73864 en 156 p. application/pdf
spellingShingle DRNTU::Engineering::Materials::Biomaterials
Kharel, Sharad
Hollow microparticles as superior carriers for encapsulation and delivery of biomolecules
title Hollow microparticles as superior carriers for encapsulation and delivery of biomolecules
title_full Hollow microparticles as superior carriers for encapsulation and delivery of biomolecules
title_fullStr Hollow microparticles as superior carriers for encapsulation and delivery of biomolecules
title_full_unstemmed Hollow microparticles as superior carriers for encapsulation and delivery of biomolecules
title_short Hollow microparticles as superior carriers for encapsulation and delivery of biomolecules
title_sort hollow microparticles as superior carriers for encapsulation and delivery of biomolecules
topic DRNTU::Engineering::Materials::Biomaterials
url http://hdl.handle.net/10356/73864
work_keys_str_mv AT kharelsharad hollowmicroparticlesassuperiorcarriersforencapsulationanddeliveryofbiomolecules