The DOI matches its Crossref record; 42 of the 42 references it cites were found in a registry or an index.
Inhibition of Peptide Acylation in PLGA Microspheres with Water-soluble Divalent Cationic Salts
Open accessAbstract
Purpose To test the potential of water-soluble divalent cationic salts to inhibit acylation of octreotide encapsulated in poly(D,L-lactic-co-glycolic acid)-star (PLGA) microspheres.Methods The divalent cationic salts, calcium chloride and manganese chloride, previously shown to disrupt peptide sorption, were introduced in PLGA microspheres prepared by the double emulsion-solvent evaporation method. Peptide stability was monitored by reversed-phase high performance liquid chromatography (RP-HPLC) and identified by liquid chromatography coupled with mass spectrometry (LC-MS) during microsphere degradation under physiological conditions for 4 weeks. Microsphere morphology and salt content were examined by scanning electron microscopy (SEM) and inductively coupled plasma-optical emission spectroscopy (ICP-OES), respectively.Results Addition of divalent cationic salts solely to the organic phase did not provide acylation inhibition. However, addition of the salt inhibitors to both the primary emulsion and the outer water phase resulted in improved drug and salt encapsulation efficiency as well as significantly decreased salt leaching and octreotide acylation. After 28 days, the extent of acylation inhibition afforded by divalent cations was > 58% relative to 13% for the NaCl control group.Conclusions Water-soluble divalent cationic salts represent a suitable class of stabilizer of peptide acylation in PLGA microspheres and this study provides an important formulation approach to maximize stabilizer potency.
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“When using a polylactic acid–polyethylene glycol copolymer, the embedding rate reached 90%.”
From Synthesis and Biological Application of Polylactic Acid (2020) · cites this paper as [89]
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“Su et al. found that, when polylactic acid was used as the membrane material, the embedding rate of hemoglobin was very low, only 7.9%.”
From Synthesis and Biological Application of Polylactic Acid (2020) · cites this paper as [89]
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Jain, R. A. (2000) · Biomaterials · doi:10.1016/s0142-9612(00)00115-0 · Cited by 2,214
Protein Instability in Poly(Lactic-co-Glycolic Acid) Microparticles
van de Weert, M., Hennink, W. E., & Jiskoot, W. (2000) · Pharmaceutical Research · doi:10.1023/a:1026498209874 · Cited by 707
Stabilization of proteins encapsulated in injectable poly (lactide- co-glycolide)
Zhu, G., Mallery, S. R., & Schwendeman, S. P. (2000) · Nature Biotechnology · doi:10.1038/71916 · Cited by 621
Self-citationJiang, W., Rk, G., DESHPANDE, M., & Schwendeman, S. P. (2004) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2004.09.003 · Cited by 480
Self-citationWang, J., Wang, B. M., & Schwendeman, S. P. (2002) · Journal of Controlled Release · doi:10.1016/s0168-3659(02)00137-2 · Cited by 351
Self-citationChemical degradation of peptides and proteins in PLGA: A review of reactions and mechanisms
Houchin, M. L., & Topp, E. M. (2008) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.21176 · Cited by 277
Moisture‐induced aggregation of lyophilized proteins in the solid state
Liu, W. R., Langer, R., & Klibanov, A. M. (1991) · Biotechnology and Bioengineering · doi:10.1002/bit.260370210 · Cited by 263
Protein stability in controlled-release systems
Fu, K., Klibanov, A. M., & Langer, R. (2000) · Nature Biotechnology · doi:10.1038/71875 · Cited by 258
Recent Advances in the Stabilization of Proteins Encapsulated in Injectable PLGA Delivery Systems
Schwendeman, S. P. (2002) · Critical Reviews in Therapeutic Drug Carrier Systems · doi:10.1615/critrevtherdrugcarriersyst.v19.i1.20 · Cited by 235
Self-citationEstey, T., Kang, J., Schwendeman, S. P., & Carpenter, J. F. (2006) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.20625 · Cited by 228
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Synthesis and Biological Application of Polylactic Acid
Li, G., Zhao, M., Xu, F., Yang, B., Li, X., Meng, X., Teng, L., Sun, F., & Li, Y. (2020) · Molecules · doi:10.3390/molecules25215023 · Cited by 492
Metadata
- Authors
- Zhang, Y., Sophocleous, A. M., & Schwendeman, S. P.
- Affiliations
- University of Michigan (US)
- Corresponding author
- Schwendeman, Steven P.
- Venue
- Pharmaceutical Research
- Published
- 2009-06-16
- Volume
- 26
- Issue
- 8
- Pages
- 1986-1994
- ISSN
- 0724-8741 (ISSN-L)
- 1573-904X
- PMC
- PMC4260456
- OpenAlex
- W1993125380
- Cited by
- 49
- References
- 42
- Citations by year
- 2026: 2 · 2025: 2 · 2024: 1 · 2023: 2 · 2022: 3 · 2021: 3 · 2020: 4 · 2019: 7 · 2018: 1 · 2016: 1 · 2015: 6 · 2014: 4 · 2013: 1 · 2012: 1
- FWCI
- 2.70
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Pharmaceutical Research (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Heart, Lung, and Blood Institute (HL68345, R01HL068345)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Agricultural and Biological Sciences › Food Science › Microencapsulation and Drying Processes
- Keywords
- octreotide, PLGA microspheres, calcium chloride, manganese chloride, peptide encapsulation, salt leaching, microsphere degradation, peptide stability, double emulsion solvent evaporation, encapsulation efficiency
- MeSH terms
- Polylactic Acid-Polyglycolic Acid Copolymer, Acylation, Cations, Divalent, Microscopy, Electron, Scanning, Microspheres, Peptides, Polyglycolic Acid, Solubility, Spectrum Analysis, Lactic Acid
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- Zhang, Y., Sophocleous, A. M., & Schwendeman, S. P. (2009). Inhibition of Peptide Acylation in PLGA Microspheres with Water-soluble Divalent Cationic Salts. Pharmaceutical Research. https://doi.org/10.1007/s11095-009-9914-2
