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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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From Synthesis and Biological Application of Polylactic Acid (2020) · cites this paper as [89]
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From Synthesis and Biological Application of Polylactic Acid (2020) · cites this paper as [89]
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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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