Feasibility study of aerosolized prostaglandin E1 microspheres as a noninvasive therapy for pulmonary arterial hypertension

Gupta, Vivek; Rawat, Amit; Ahsan, Fakhrul

doi:10.1002/jps.21946

Cited by 32 publications

(56 citation statements)

References 42 publications

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“…However, the main limitation of pulmonary delivery of PGE 1 is its very short half-life (3 to 4 minutes) as a result of first-pass metabolism in the lungs. We have shown recently that PLGA microparticles of PGE 1 release the drug over a prolonged period of time, improving the metabolic stability of the drug (19). The extreme hydrophobicity of PGE 1 limits its passage through the air-blood barrier.…”

Section: Introductionmentioning

confidence: 99%

PLGA Microparticles Encapsulating Prostaglandin E1-Hydroxypropyl-β-cyclodextrin (PGE1-HPβCD) Complex for the Treatment of Pulmonary Arterial Hypertension (PAH)

et al. 2011

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Section: Introductionmentioning

confidence: 99%

PLGA Microparticles Encapsulating Prostaglandin E1-Hydroxypropyl-β-cyclodextrin (PGE1-HPβCD) Complex for the Treatment of Pulmonary Arterial Hypertension (PAH)

et al. 2011

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“…A number of new alternative dosage forms of PGE1, such as lipid microspheres (15), inhaled PLGA particles (16)(17)(18) for pulmonary arterial hypertension, and nanoparticles (19)(20)(21)(22), can prevent PGE1 from inactivation in blood and improve the efficacy of PGE1. Among these new dosage forms, PGE1 lipid microspheres (lipo-PGE1) were established by Mizushima (15).…”

Section: Introductionmentioning

confidence: 99%

Development, Optimization, and Characterization of PEGylated Nanoemulsion of Prostaglandin E1 for Long Circulation

Cheng

Liu

Hu³

et al. 2015

AAPS PharmSciTech

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Abstract. Lipo-PGE1 is the most widely used formulation of PGE1 in clinic. However, PGE1 is easier to leak out from lipo-PGE1 and this will lead to the phlebophlogosis when intravenous injection. The stability of lipo-PGE1 in storage and in vivo is also discounted. The aim of this study is to develop a long-circulating prostaglandin E1-loaded nanoemulsion modified with 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000] (DSPE-PEG) to improve the stability and pharmacokinetics profiles of lipo-PGE1. PEGylated PGE1 nanoemulsion was prepared using a dispersing-homogenized method. The stability of nanoemulsion in 1 month was investigated. Pharmacokinetic studies were employed to evaluate the in vivo profile of the optimized nanoemulsion. The optimized nanoemulsion PGE1-PEG2000(1%)-NE showed an oil droplet size <100 nm with a surface charge of −14 mV. Approximately, 97% of the PGE1 was encapsulated in the nanoemulsion. The particle size, zeta potential, and drug loading of PGE1-PEG2000(1%)-NE were stable in 1 month. After PGE1-PEG2000(1%)-NE was intravenously administered to rats, the area under curve (AUC) and half-life of PGE1 were, respectively, 1.47-fold and 5.98-fold higher than those of lipo-PGE1 (commercial formulation). PGE1-PEG2000(1%)-NE was an ideal formulation for prolonging the elimination time of PGE1. This novel parenteral colloidal delivery system of PGE1 has a promising potential in clinic use.

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“…The tapped densities of the particles were determined according to the procedure described previously [28] . An aliquot of particles from each formulation was put to a 10 (±0.05) ml graduated cylinder.…”

Section: Characterization Of Microspheres For Pulmonary Deliverymentioning

confidence: 99%

Preparation and In Vitro Evaluation of Biodegradable Microspheres with Narrow Size Distribution for Pulmonary Delivery

Zhao¹,

Xu²,

Guo³

2017

pharmaceutical-sciences

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Feasibility study of aerosolized prostaglandin E1 microspheres as a noninvasive therapy for pulmonary arterial hypertension

Cited by 32 publications

References 42 publications

PLGA Microparticles Encapsulating Prostaglandin E1-Hydroxypropyl-β-cyclodextrin (PGE1-HPβCD) Complex for the Treatment of Pulmonary Arterial Hypertension (PAH)

PLGA Microparticles Encapsulating Prostaglandin E1-Hydroxypropyl-β-cyclodextrin (PGE1-HPβCD) Complex for the Treatment of Pulmonary Arterial Hypertension (PAH)

Development, Optimization, and Characterization of PEGylated Nanoemulsion of Prostaglandin E1 for Long Circulation

Preparation and In Vitro Evaluation of Biodegradable Microspheres with Narrow Size Distribution for Pulmonary Delivery

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