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Enhancement Of Oral Bioavailability Of Pentoxifylline By Solid Lipid Nanoparticles

J. Varshosaz, M. Minayian, Elaheh Moazen
Published 2010 · Materials Science, Medicine

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Pentoxifylline (PTX) is a highly water-soluble, hemorheologic drug that undergoes first-pass effect with 20% bioavailability. The solid lipid nanoparticles (SLNs) of PTX were prepared to enhance its oral bioavailability by homogenization, followed by the sonification method. Seven different variables, each at two levels, were studied: lipid type, surfactant type and concentration, speed of homogenizer, acetone:dichloromethane (DCM) ratio, lecithin:lipid ratio, and sonication time. The mean particle size and size distribution, drug entrapment efficiency (EE%), zeta potential, and drug release of the SLNs were investigated. A pharmacokinetic study was conducted in male Wistar rats after oral administration of 10 mg kg−1 PTX in the form of free drug or SLNs. The z-average particle size, zeta potential, and EE% of the SLNs were at least 250 nm, −30.2 mV, and 70%, respectively. Among the studied factors, the lipid type, surfactant type, and percentage had a significant effect on the particle size. Zeta potential was more affected by lipid type, acetone:DCM ratio, and sonication time. Speed of homogenizer and acetone:DCM ratio had a significant effect on the EE%. The optimized SLN was prepared by 80 mg of cetyl alcohol, 10 mg of lecithin, acetone:DCM ratio (1:2), 30-second sonication, 3% Tween 20, and a mixing rate of 800 rpm. In vitro drug release lasted for about 5 hours. It was found that the relative bioavailability of PTX in SLNs was significantly increased, compared to that of the PTX solution. SLNs offer a promising approach to improve the oral bioavailability of PTX that is affected by a high first-pass effect.
This paper references
Comparison of Pentoxifylline Pharmacokinetics Between Smokers and Nonsmokers
V. Mauro (1992)
Effect of lipid core material on characteristics of solid lipid nanoparticles designed for oral lymphatic delivery.
Rishi Paliwal (2009)
Pentoxyphylline and propentophylline are inhibitors of TNF-alpha release in Meiners I, monocytes activated by advanced glycation endproducts
S. Hauschildt (2004)
Effect of Excipient and Processing Variables on Adhesive Properties and Release Profile of Pentoxifylline From Mucoadhesive Tablets
Madhu S. Surapaneni (2006)
Solid lipid nanoparticles (SLN) for controlled drug delivery--drug release and release mechanism.
A. Zur Mühlen (1998)
Pentoxyphylline and propentophylline are inhibitors of TNF-α release in monocytes activated by advanced glycation endproducts
Ina Meiners (2004)
Engineering Methods for Robust Product Design
Henry W. Altland (1996)
Body Distribution of Camptothecin Solid Lipid Nanoparticles After Oral Administration
Shicheng Yang (2004)
Duodenal administration of solid lipid nanoparticles loaded with different percentages of tobramycin.
R. Cavalli (2003)
Some considerations about the hydrophilic-lipophilic balance system.
R. Pasquali (2008)
Lipid nanoparticles (SLN, NLC) in cosmetic and pharmaceutical dermal products.
J. Pardeike (2009)
Comparative pharmacokinetic analysis of novel sustained-release dosage forms of pentoxifylline in healthy subjects.
I. Raz (1988)
Examination of the impact of a range of Pluronic surfactants on the in‐vitro solubilisation behaviour and oral bioavailability of lipidic formulations of atovaquone
L. Sek (2006)
Applying the Taguchi robust design to the optimization of the asymmetric reduction of ethyl 4-chloro acetoacetate by bakers' yeast.
J. Y. Houng (2003)
Solid lipid nanoparticles: production, characterization and applications.
W. Mehnert (2001)
Comparison of the Lymphatic Transport of Halofantrine Administered in Disperse Systems Containing Three Different Unsaturated Fatty Acids
R. Holm (2004)
Lipid-based vehicles for the oral delivery of poorly water soluble drugs
A. Humberstone (1997)
Medication vehicles made of solid lipid particles (solid lipid nanospheres sln)
룩크스 스테판 (1992)
Evaluation of surface charge density and surface potential by electrophoretic mobility for solid lipid nanoparticles and human brain-microvascular endothelial cells.
Y. Kuo (2007)
A novel approach based on lipid nanoparticles (SLN®) for topical delivery of α-lipoic acid
E. Souto (2005)
Solid lipid nanoparticles (SLNs) to improve oral bioavailability of poorly soluble drugs
L. Hu (2004)
Pentoxifylline in prevention of radiation-induced lung toxicity in patients with breast and lung cancer: a double-blind randomized trial.
B. Ozturk (2004)
Modulation of intravariceal pressure with pentoxifylline: a possible new approach in the treatment of portal hypertension
E. Eleftheriadis (1998)
PrefaceLipid nanoparticles: recent advances☆
R. Mueller (2007)
Engineering Methods for Robust Product Design: Using Taguchi Methods in Technology and Product Development
W. Y. Fowlkes (1995)
Studies on oral absorption of stearic acid SLN by a novel fluorometric method.
H. Yuan (2007)
Brain and muscle of Wistar rats are the main targets of intravenous dendrimeric sulfadiazine.
M. J. Prieto (2008)
Novel double coated nanocapsules for intestinal delivery and enhanced oral bioavailability of tacrolimus, a P-gp substrate drug.
T. Nassar (2009)
Development and evaluation of nitrendipine loaded solid lipid nanoparticles: influence of wax and glyceride lipids on plasma pharmacokinetics.
V. V. Kumar (2007)
Solid lipid nanoparticles for enhancing vinpocetine's oral bioavailability.
Yifan Luo (2006)
Enhancement the oral bioavailability of praziquantel by incorporation into solid lipid nanoparticles.
Li Yang (2009)
Production of solid lipid nanoparticles (SLN): scaling up feasibilities
A. Dingler (2002)
Solid lipid nanoparticles (SLNs) for controlled drug delivery—a review of the state of the art
R. H. Müller (2000)
Zeta-potential measurement using the Smoluchowski equation and the slope of the current-time relationship in electroosmotic flow.
A. Sze (2003)
Production and optimization of valproic acid nanostructured lipid carriers by the Taguchi design
J. Varshosaz (2010)
Solid lipid nanoparticles (SLN) for controlled drug delivery. I. Production, characterization and sterilization
C. Schwarz (1994)
Solid lipid nanoparticles (SLN) for controlled drug delivery - a review of the state of the art.
R. Mueller (2000)
The importance of gastrointestinal uptake of particles in the design of oral delivery systems
E. Lavelle (1995)
Enhanced oral bioavailability of salvianolic acid B by phospholipid complex loaded nanoparticles.
Q. Peng (2008)
The influence of lipid nanocapsule composition on their size distribution.
B. Heurtault (2003)
Antithrombotic therapy in peripheral arterial disease.
E. Lipsitz (2008)
Drug Treatment of Intermittent Claudication
Douglas S Jacoby (2012)

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Nanodrugs in Medicine and Healthcare: Oral Delivery
A. Sosnik (2016)
Studies concerning the development of lipid nanostructures in bioproducts encapsulation.
C. Dinu-Pîrvu (2012)
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Milad Fathi (2012)
Recent Advances in Lipid Nanoparticle Formulations with Solid Matrix for Oral Drug Delivery
S. Das (2010)
Formulation in vitro and in vivo evaluation of SRMS-based heterolipid-templated homolipid delivery system for diclofenac sodium
Momoh A. Mumuni (2016)
Lipospheres and pro-nano lipospheres for delivery of poorly water soluble compounds.
Anna Elgart (2012)
Solid Lipid Nanoparticles of Dronedarone Hydrochloride for Oral Delivery: Optimization, In Vivo Pharmacokinetics and Uptake Studies.
V. M. Gambhire (2019)
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G. A. Islan (2016)
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Rahul S. Kalhapure (2013)
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Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs): recent advances in drug delivery
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