Encapsulation of PROLI/NO in biodegradable microparticles
Abstract
Biodegradable hydrophilic polymers poly-lactic-co-glycolic acid (PLGA) and polyethylene oxide-co-lactic acid (PELA) were used to encapsulate a small hydrophilic prodrug (PROLI/NO) as a strategy to deliver nitric oxide (NO) by inhalation. The microparticles were prepared using double emulsion and solvent evaporation, followed by freeze-drying. The NO release kinetics were characterized by three parameters: the maximum concentration of NO per unit weight of microparticles, C(max) (nM mg(-1)); the window of time for which the concentration exceeded 50% of C(max), W(50) (min); and the initial rate of release, R(i) (nM mg(-1) min(-1)). PLGA-based microparticles did not encapsulate PROLI/NO. PELA-based microparticles demonstrated an entrapment efficiency rate of 43%, a mass median diameter of 2.3 micro m, and NO release in a physiological buffer characterized by C(max) = 123, W(50) = 4.11, and R(i) = 78.7. Addition of gelatin as a hydrophilic binding moiety in the first emulsion allowed PLGA-based microparticles to encapsulate PROLI/NO; however, the mass median diameter was too large for inhalation (23.5 micro m). It is concluded that the hydrophilic polyethylene glycol-moiety in PELA allows for efficient encapsulation of PROLI/NO, and PELA-based microparticles might be a strategy to generate a stable inhalable form of NO.
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PELA and PLGA are suitable vehicles for encapsulating NO donors to prolong NO release.
“Biodegradable poly(ethylene oxide-co-lactic acid) (PELA)249 and poly(lactic-co-glycolic acid) (PLGA)206,219,249 have also been shown to be suitable vehicles for encapsulating NO donors to prolong the NO release.”
From Recent advances in thromboresistant and antimicrobial polymers for biomedical applications: just say yes to nitric oxide (NO) (2016) · cites this paper as [249]
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- Authors
- Jeh, H. S., Lu, S., & George, S. C.
- Affiliations
- University of California, Irvine (US)
- Corresponding author
- Jeh, H. S.
- ORCID
- George, S. C.
- Venue
- Journal of Microencapsulation
- Publisher
- Informa UK Limited
- Published
- 2004-02
- Volume
- 21
- Issue
- 1
- Pages
- 3-13
- ISSN
- 0265-2048 (ISSN-L)
- 1464-5246
- OpenAlex
- W2051377530
- Cited by
- 20
- References
- 20
- Citations by year
- 2026: 1 · 2022: 2 · 2021: 1 · 2019: 1 · 2018: 2 · 2016: 5 · 2012: 2
- FWCI
- 0.55
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Microencapsulation (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institutes of Health (5r29hl060636-04)
- National Heart, Lung, and Blood Institute (HL60636)
- Topics
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Inhalation and Respiratory Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Agricultural and Biological Sciences › Food Science › Microencapsulation and Drying Processes
- Keywords
- nitric oxide, prodrugs, biodegradable microparticles, poly(lactic-co-glycolic acid), pulmonary drug delivery, encapsulation efficiency, gelatin binding, double emulsion solvent evaporation, freeze-drying
- MeSH terms
- Polylactic Acid-Polyglycolic Acid Copolymer, Biocompatible Materials, Drug Carriers, Drug Compounding, Gelatin, Glycolates, Humans, Lactates, Microspheres, Nitric Oxide, Nitrogen Oxides, Particle Size, Polyethylene Glycols, Polyglycolic Acid, Polymers, Prodrugs, Proline, Lactic Acid
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