Hollow microparticles as a superior delivery system over solid microparticles for the encapsulation of peptides

Purpose Peptides are gaining significant interests as therapeutic agents due to their high targeting specificity and potency. However, their low bioavailability and short half-lives limit their massive potential as therapeutics. The use of dense, solid particles of biodegradable polymer as a uni...

Full description

Saved in:
Bibliographic Details
Main Authors: Loo, Joachim Say Chye, Gautam, Archana, Kharel, Sharad, Dickescheid, Andreas
Other Authors: School of Materials Science & Engineering
Format: Article
Language:English
Published: 2019
Subjects:
Online Access:https://hdl.handle.net/10356/82262
http://hdl.handle.net/10220/48032
Tags: Add Tag
No Tags, Be the first to tag this record!
Institution: Nanyang Technological University
Language: English
id sg-ntu-dr.10356-82262
record_format dspace
spelling sg-ntu-dr.10356-822622020-09-21T11:33:52Z Hollow microparticles as a superior delivery system over solid microparticles for the encapsulation of peptides Loo, Joachim Say Chye Gautam, Archana Kharel, Sharad Dickescheid, Andreas School of Materials Science & Engineering Singapore Centre for Environmental Life Sciences and Engineering PLGA Biodegradable DRNTU::Engineering::Materials Purpose Peptides are gaining significant interests as therapeutic agents due to their high targeting specificity and potency. However, their low bioavailability and short half-lives limit their massive potential as therapeutics. The use of dense, solid particles of biodegradable polymer as a universal carrier for peptides also has its challenges, such as inefficient peptide release and low bioactivity. In this paper, it was established that hollow microparticles (h-MPs) instead of solid microparticles (s-MPs), as peptide carriers, could improve the release efficiency, while better preserving their bioactivity. Methods Glucagon like Peptide-1 (GLP-1) was encapsulated as a model peptide. Mass loss, average molecular weight changes, intraparticle pH, polymer-peptide interaction and release studies, together with bioactivity assessment of the peptide for s-MPs and h-MPs were systematically analyzed and evaluated for efficacy. Results The intraparticle pH of s-MPs was as low as 2.64 whereas the pH of h-MPs was 4.99 by day 7. Consequently, 93% of the peptide extracted from h-MPs was still bioactive while only 58% of the peptide extracted from s-MPs was bioactive. Likewise, the cumulative release of GLP-1 by day 14 from h-MPs showed a cumulative amount of 88 ± 8% as compared to 33 ± 6% for s-MPs. Conclusions The cumulative release of peptide can be significantly improved, and the bioactivity can be better preserved by simply using h-MPs instead of s-MPs as carriers MOE (Min. of Education, S’pore) Accepted version 2019-04-16T02:48:22Z 2019-12-06T14:52:01Z 2019-04-16T02:48:22Z 2019-12-06T14:52:01Z 2018 Journal Article Kharel, S., Gautam, A., Dickescheid, A., & Loo, J. S. C. (2018). Hollow microparticles as a superior delivery system over solid microparticles for the encapsulation of peptides. Pharmaceutical Research, 35(10). doi:10.1007/s11095-018-2461-y 0724-8741 https://hdl.handle.net/10356/82262 http://hdl.handle.net/10220/48032 10.1007/s11095-018-2461-y en Pharmaceutical Research © 2018 Springer Science+Business Media [Springer US]. All rights reserved.This is a post-peer-review, pre-copyedit version of an article published in Pharmaceutical Research. The final authenticated version is available online at: https://dx.doi.org/10.1007/s11095-018-2461-y 29 p. application/pdf
institution Nanyang Technological University
building NTU Library
country Singapore
collection DR-NTU
language English
topic PLGA
Biodegradable
DRNTU::Engineering::Materials
spellingShingle PLGA
Biodegradable
DRNTU::Engineering::Materials
Loo, Joachim Say Chye
Gautam, Archana
Kharel, Sharad
Dickescheid, Andreas
Hollow microparticles as a superior delivery system over solid microparticles for the encapsulation of peptides
description Purpose Peptides are gaining significant interests as therapeutic agents due to their high targeting specificity and potency. However, their low bioavailability and short half-lives limit their massive potential as therapeutics. The use of dense, solid particles of biodegradable polymer as a universal carrier for peptides also has its challenges, such as inefficient peptide release and low bioactivity. In this paper, it was established that hollow microparticles (h-MPs) instead of solid microparticles (s-MPs), as peptide carriers, could improve the release efficiency, while better preserving their bioactivity. Methods Glucagon like Peptide-1 (GLP-1) was encapsulated as a model peptide. Mass loss, average molecular weight changes, intraparticle pH, polymer-peptide interaction and release studies, together with bioactivity assessment of the peptide for s-MPs and h-MPs were systematically analyzed and evaluated for efficacy. Results The intraparticle pH of s-MPs was as low as 2.64 whereas the pH of h-MPs was 4.99 by day 7. Consequently, 93% of the peptide extracted from h-MPs was still bioactive while only 58% of the peptide extracted from s-MPs was bioactive. Likewise, the cumulative release of GLP-1 by day 14 from h-MPs showed a cumulative amount of 88 ± 8% as compared to 33 ± 6% for s-MPs. Conclusions The cumulative release of peptide can be significantly improved, and the bioactivity can be better preserved by simply using h-MPs instead of s-MPs as carriers
author2 School of Materials Science & Engineering
author_facet School of Materials Science & Engineering
Loo, Joachim Say Chye
Gautam, Archana
Kharel, Sharad
Dickescheid, Andreas
format Article
author Loo, Joachim Say Chye
Gautam, Archana
Kharel, Sharad
Dickescheid, Andreas
author_sort Loo, Joachim Say Chye
title Hollow microparticles as a superior delivery system over solid microparticles for the encapsulation of peptides
title_short Hollow microparticles as a superior delivery system over solid microparticles for the encapsulation of peptides
title_full Hollow microparticles as a superior delivery system over solid microparticles for the encapsulation of peptides
title_fullStr Hollow microparticles as a superior delivery system over solid microparticles for the encapsulation of peptides
title_full_unstemmed Hollow microparticles as a superior delivery system over solid microparticles for the encapsulation of peptides
title_sort hollow microparticles as a superior delivery system over solid microparticles for the encapsulation of peptides
publishDate 2019
url https://hdl.handle.net/10356/82262
http://hdl.handle.net/10220/48032
_version_ 1681057755170865152