Encapsulation of PROLI/NO in biodegradable microparticles

H. S. Jeh, S. Lu, Steven George

Research output: Contribution to journalArticle

13 Citations (Scopus)

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, Cmax (nM mg-1); the window of time for which the concentration exceeded 50% of Cmax W50 (min); and the initial rate of release, Ri (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 μm, and NO release in a physiological buffer characterized by Cmax = 123, W50 = 4.11, and Ri = 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 μm). 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.

Original languageEnglish (US)
Pages (from-to)3-13
Number of pages11
JournalJournal of Microencapsulation
Volume21
Issue number1
DOIs
StatePublished - Feb 1 2004

Fingerprint

Nitric oxide
microparticles
nitric oxide
Encapsulation
Nitric Oxide
lactic acid
polyethylenes
Lactic acid
Polyethylene oxides
Lactic Acid
oxides
respiration
Emulsions
Inhalation
acids
emulsions
Acids
freeze drying
Biodegradable polymers
entrapment

Keywords

  • Inhalation
  • Microsphere
  • Nitric oxide
  • PELA
  • PLGA
  • Pulmonary hypertension

ASJC Scopus subject areas

  • Bioengineering
  • Pharmaceutical Science
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Colloid and Surface Chemistry

Cite this

Encapsulation of PROLI/NO in biodegradable microparticles. / Jeh, H. S.; Lu, S.; George, Steven.

In: Journal of Microencapsulation, Vol. 21, No. 1, 01.02.2004, p. 3-13.

Research output: Contribution to journalArticle

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