| PLGA Microparticles Encapsulating Prostaglandin E(1)-Hydroxypropyl-β-cyclodextrin (PGE (1)-HPβCD) Complex for the Treatment of Pulmonary Arterial Hypertension (PAH). | |
| | |
MedLine Citation:
|
PMID: 21626061 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
|
PURPOSE: To test the efficacy and viability of poly (lactic-co-glycolic acid) (PLGA) microspheres encapsulating an inclusion complex of prostaglandin E(1) (PGE(1)) and 2-hydroxypropyl-β-cyclodextrin (HPβCD) for pulmonary delivery of PGE(1) for treatment of pulmonary arterial hypertension (PAH), a disease of pulmonary circulation. METHODS: PLGA-based microparticulate formulations of PGE(1)-HPβCD inclusion complex or plain PGE(1) were prepared by a double-emulsion solvent evaporation method. HPβCD was used as a complexing agent to increase the aqueous solubility of PGE(1), act as a porosigen to produce large porous particles, and promote absorption of PGE(1). Particles were characterized for micromeritic properties, in vivo absorption, metabolic degradation, and acute safety. RESULTS: Incorporation of HPβCD in the microparticles resulted in development of large particles with internal pores, which, despite large mean diameters, had aerodynamic diameters in the inhalable range of 1 to 5 μm. HPβCD incorporation also resulted in a significant increase in the amount of drug released in vitro in simulated interstitial lung fluid, showing a desirable burst release profile required for immediate hemodynamic effects. Compared to plain PLGA microparticles, entrapment efficiency was decreased upon complexation with HPβCD. In vivo absorption profile indicated prolonged availability of PGE(1) in circulation following pulmonary administration of the optimized microparticulate formulations, with an extended half-life of almost 4 hours. Metabolic degradation and acute toxicity studies suggested that microparticulate formulations were stable under physiological conditions and safe for the lungs and respiratory epithelium. CONCLUSIONS: This study demonstrates the feasibility of PGE(1)-HPβCD complex encapsulated in PLGA microparticles as a potential delivery system for controlled release of inhaled PGE(1). |
| | |
Authors:
|
Vivek Gupta; Marauo Davis; Louisa J Hope-Weeks; Fakhrul Ahsan |
Publication Detail:
|
Type: JOURNAL ARTICLE Date: 2011-4-6 |
Journal Detail:
|
Title: Pharmaceutical research Volume: - ISSN: 1573-904X ISO Abbreviation: - Publication Date: 2011 Apr |
Date Detail:
|
Created Date: 2011-5-31 Completed Date: - Revised Date: - |
Medline Journal Info:
|
Nlm Unique ID: 8406521 Medline TA: Pharm Res Country: - |
Other Details:
|
Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
|
Department of Pharmaceutical Sciences, School of Pharmacy, Texas Tech University Health Sciences Center, 1300 Coulter Drive, Amarillo, Texas, 79106, USA. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
|
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Establishing a Link Between Amino Acid Sequences and Self-Associating and Viscoelastic Behavior of T...
Next Document: Isolation and molecular characterization of canine distemper virus from India.