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Cited by 55Advanced Drug Delivery SystemsMicroencapsulation and Drying ProcessesNanoparticle-Based Drug Delivery

Ultrasonic atomization and subsequent polymer desolvation for peptide and protein microencapsulation into biodegradable polyesters

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Felder, Ch. B., Blanco-Príeto, M. J., Heizmann, J., Merkle, H. P., Gander, B.·2003·Journal of Microencapsulation
DOI 10.3109/02652040309178346
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Abstract

Peptide and protein microencapsulation into poly(lactide) (PLA) and poly(lactide-co-glycolide) (PLGA) microspheres continues to represent a technological challenge in terms of product sterility and up-scaling. The primary objective of this study was to examine the feasibility of a novel method for peptide and protein entrapment into PLA and PLGA microspheres, particularly suitable for up-scaling and aseptic processing. The method involves ultrasonic atomization of an organic polymer solution combined with subsequent organic solvent extraction by a hardening agent. The study evaluated the critical atomization conditions, the required molecular cohesion parameters of polymer solvents and hardening agent for particle preparation as well as the quality of entrapment and release as a function of polymer and peptide/protein type. Suitable polymer solvents and hardening agents were restricted to defined domains of fractional cohesion parameters: fp = 0.2–0.35 and fh = 0.2–0.4 for the polymer solvents, and fp = 0-0.1 and fh = 0-0.25 for the hardening agents. Microsphere size (0.1–100 μm) was largely controlled by the viscosity of the atomized solution. Microencapsulation of the freely water-soluble bovine serum albumin and tetrapeptide thymocartin yielded modest efficiencies of 12–35%, whereas the slightly water-soluble octapeptide vapreotide pamoate was entrapped with 63–93% efficiency. Drug release was mainly governed by the polymer type, lasting over 100 days for BSA entrapped in PLA microspheres and ∼ 20 days for vapreotide pamoate in PLGA 50:50 and for thymocartin in PLA. Very importantly, the novel method was readily accommodated within a laminar air-flow cabinet. Under aseptic conditions, sterile microspheres could be prepared. In conclusion, the novel method described may have potential in industrial environments.

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  • Several new methods for manufacturing PLGA or PLA particles have been reported, including ultrasonic atomization, electrospray, microfluidic, pore-closing/thermoreversible-gel, and microfabrication.

    “Recently, several new methods to manufacture PLGA or PLA particles have been reported, such as the ultrasonic atomization method [14,15], the electrospray method [16], the microfluidic method [17,18], the pore-closing and thermoreversible-gel method [19,20], and the microfabrication method [21].”

    From Use of lectin-functionalized particles for oral immunotherapy (2012) · cites this paper as [14]

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Authors
Felder, C. B., Blanco-Príeto, M. J., Heizmann, J., Merkle, H. P., & Gander, B.
Affiliations
  • ETH Zurich (CH)
  • Institute of Pharmaceutical Sciences, ETH Zurich, Winterthurerstrasse 190, 8057, Zurich, Switzerland
  • F. Hoffmann-La Roche AG (CH)
Corresponding author
Gander, B.
ORCID
Gander, B.
Venue
Journal of Microencapsulation
Publisher
Informa UK Limited
Published
2003-01
Volume
20
Issue
5
Pages
553-567
ISSN
  • 0265-2048 (ISSN-L)
  • 1464-5246
DOI
10.3109/02652040309178346
OpenAlex
W4232908226
Cited by
55
References
30
Citations by year
2026: 1 · 2023: 3 · 2022: 1 · 2021: 2 · 2020: 4 · 2018: 5 · 2016: 2 · 2015: 5 · 2014: 2 · 2012: 2
FWCI
3.38
Type
journal article
Language
en
Open access
Licence
other-oa
Locations
  • Journal of Microencapsulation (publishedVersion)
  • PubMed (publishedVersion)
  • Deposito Adademico Digital Universidad De Navarra (University of Navarra) (submittedVersion, other-oa)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Life Sciences › Agricultural and Biological Sciences › Food Science › Microencapsulation and Drying Processes
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Keywords
protein microencapsulation, polylactic acid, poly(lactic-co-glycolic acid), ultrasonic atomization, solvent extraction, hardening agents, cohesion parameter, bovine serum albumin, drug release, aseptic processing, biodegradable polyesters
MeSH terms
Polylactic Acid-Polyglycolic Acid Copolymer, Biocompatible Materials, Biodegradation, Environmental, Drug Carriers, Drug Compounding, Microspheres, Particle Size, Peptide Fragments, Peptides, Polyesters, Polyglycolic Acid, Polymers, Proteins, Serum Albumin, Bovine, Solubility, Solutions, Solvents, Somatostatin, Thymopoietins, Ultrasonics, Viscosity, Lactic Acid

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