← Back to Search
Formulation And Antitumor Activity Evaluation Of Nanocrystalline Suspensions Of Poorly Soluble Anticancer Drugs
E. Merisko-Liversidge, P. Sarpotdar, J. Bruno, S. Hajj, L. Wei, N. Peltier, J. Rake, J. Shaw, S. Pugh, L. Polin, J. Jones, T. Corbett, E. Cooper, G. Liversidge
Published 2004 · Chemistry, Medicine
Download PDFAnalyze on Scholarcy
AbstractPurpose. Determine if wet milling technology could be used to formulate water insoluble antitumor agents as stabilized nanocrystalline drug suspensions that retain biological effectiveness following intravenous injection. Methods. The versatility of the approach is demonstrated by evaluation of four poorly water soluble chemotherapeutic agents that exhibit diverse chemistries and mechanisms of action. The compounds selected were: piposulfan (alkylating agent), etoposide (topoisomerase II inhibitor), camptothecin (topoisomerase I inhibitor) and paclitaxel (antimitotic agent). The agents were wet milled as a 2% w/v solids suspension containing 1 % w/v surfactant stabilizer using a low energy ball mill. The size , physical stability and efficacy of the nanocrystalline suspensions were evaluated. Results. The data show the feasibility of formulating poorly water soluble anticancer agents as physically stable aqueous nanocrystalline suspensions. The suspensions are physically stable and efficacious following intravenous injection. Conclusions. Wet milling technology is a feasible approach for formulating poorly water soluble chemotherapeutic agents that may offer a number of advantages over a more classical approach.
This paper references
Biodegradable long-circulating polymeric nanospheres.
R. Gref (1994)
Acute hypersensitivity reactions to etoposide in a VEPA regimen for Hodgkin's disease.
M. Hudson (1993)
Phase I study of taxol administered as a short i.v. infusion daily for 5 days.
J. Grem (1987)
Particle size reduction for improvement of oral bioavailability of hydrophobic drugs: I. Absolute oral bioavailability of nanocrystalline danazol in beagle dogs
G. Liversidge (1995)
Effects of hydrotropic agents on the solubility, precipitation, and protein binding of etoposide.
I. A. Darwish (1989)
Lipid Emulsions as Drug Delivery Systems
S. Davis (1987)
Design, synthesis and biological activity of protaxols
K. C. Nicolaou (1993)
A method for the preparation of submicron particles of sparingly water-soluble drugs by precipitation in oil-in-water emulsions. II: Influence of the emulsifier, the solvent, and the drug substance.
B. Sjoestroem (1993)
Hypersensitivity reactions induced by etoposide.
O'Dwyer Pj (1984)
Successful re-treatment with taxol after major hypersensitivity reactions.
D. Peereboom (1993)
The clinical pharmacology of etoposide
M. Slevin (1991)
Biology and therapeutic response of a mouse mammary adenocarcinoma (16/C) and its potential as a model for surgical adjuvant chemotherapy.
T. Corbett (1978)
Phase I clinical trial of weekly and daily treatment with camptothecin (NSC-100880): correlation with preclinical studies.
F. Muggia (1972)
A phase II trial of VP 16–213 in adults with refractory acute myeloid leukemia: An Eastern Cooperative Oncology Group study
J. Bennett (1984)
The current status of camptothecin analogues as antitumor agents.
W. Slichenmyer (1993)
Improved oral absorption of a poorly water-soluble drug, HO-221, by wet-bead milling producing particles in submicron region.
N. Kondo (1993)
Midwest Cooperative Group evaluation of piposulfan (A‐20968) in cancer
N. Nelson (1967)
Long-circulating (sterically stabilized) liposomes for targeted drug delivery.
T. Allen (1994)
Polystyrene-Poly (Ethylene Glycol) (PS-PEG2000) Particles as Model Systems for Site Specific Drug Delivery. 2. The Effect of PEG Surface Density on the in Vitro Cell Interaction and in VivoBiodistribution
S. E. Dunn (2004)
Interaction of serum components with poly(methylmethacrylate) nanoparticles and the resulting body distribution after intravenous injection in rats.
G. Borchard (1993)
Clinical experience with 1,4-dihydracryloylpiperazine, dimethanesulfonate (NSC-47774).
J. J. van Dyk (1968)
Nanoparticles as microcarriers for anticancer drugs
P. Couvreur (1990)
This paper is referenced by
Paclitaxel-Nanodiamond Nanocomplexes Enhance Aqueous Dispersibility and Drug Retention in Cells.
Dae Gon Lim (2016)
Morphology and surface States of colloidal probucol nanoparticles evaluated by atomic force microscopy.
K. Moribe (2008)
Herstellung und Charakterisierung nanodisperser Arzneiformen in wässrigen und nichtwässrigen Medien und Kontrolle der Freisetzung
Ansgar Brinkmann (2020)
Designing Paclitaxel Drug Delivery Systems Aimed at Improved Patient Outcomes: Current Status and Challenges
Madhu S. Surapaneni (2012)
Nanosuspension: An Attempt to Enhance Bioavailability of Poorly Soluble Drugs
Sneha B Garasiya (2012)
Can controversial nanotechnology promise drug delivery?
Venkat Ratnam Devadasu (2013)
Liposomal paclitaxel formulations.
Štěpán Koudelka (2012)
Intravenous itraconazole emulsions produced by SolEmuls technology.
A. Akkar (2003)
Design of experiment approach in development of febuxostat nanocrystal: Application of Soluplus® as stabilizer
O. P. Sharma (2016)
Csaba Bartos (2019)
Small-scale systems for in vivo drug delivery
David A. LaVan (2003)
Encapsulation of 9-nitrocamptothecin, a novel anticancer drug, in biodegradable nanoparticles: factorial design, characterization and release kinetics.
K. Derakhshandeh (2007)
Are high drug loading nanoparticles the next step forward for chemotherapy?
Joseph Della Rocca (2012)
SOLUBILITY ENHANCEMENT OF POORLY WATER SOLUBLE DRUG BY USING NANO- SUSPENSION TECHNOLOGY
Mishra Soumya (2013)
Application of formulation technologies in lead candidate selection and optimization
M. Chaubal (2004)
Physical properties of griseofulvin-lipid nanoparticles in suspension and their novel interaction mechanism with saccharide during freeze-drying.
S. Kamiya (2010)
The Use of Nanotechnology in Modern Pharmacotherapy
A. Ostróżka-Cieślik (2017)
Formulation development of small and large volume injections
Madhav Kamat and Patrick P. DeLuca (2016)
Insulin Nanoparticles: A Novel Formulation Approach for Poorly Water Soluble Zn-Insulin
E. Merisko-Liversidge (2004)
Increased antitumor activity, intratumor paclitaxel concentrations, and endothelial cell transport of cremophor-free, albumin-bound paclitaxel, ABI-007, compared with cremophor-based paclitaxel.
N. Desai (2006)
One-step preparation of pharmaceutical nanocrystals using ultra cryo-milling technique in liquid nitrogen.
T. Niwa (2010)
Formulation and in-vitro evaluation of pantoprazole loaded pH-sensitive polymeric nanoparticles
A. Nasef (2017)
Nanoparticle Albumin-Bound Anticancer Agents
N. Desai (2015)
Understanding paclitaxel/pluronic F127 nanocrystals prepared by the stabilization of nanocrystal (SNC) method
Jiexin Deng (2009)
Transformation of Meloxicam Containing Nanosuspension into Surfactant-Free Solid Compositions to Increase the Product Stability and Drug Bioavailability for Rapid Analgesia
Csaba Bartos (2019)
CPT loaded nanoparticles based on beta-cyclodextrin-grafted poly(ethylene glycol)/poly (L-glutamic acid) diblock copolymer and their inclusion complexes with CPT.
F. Du (2014)
Mechanical Particle-Size Reduction Techniques
Javier O Morales (2012)
Formulation and pharmacokinetic evaluation of a paclitaxel nanosuspension for intravenous delivery
Y. Wang (2011)
Supercritical fluid technology for enhanced drug delivery
P. Pathak (2005)
Nanosizing for oral and parenteral drug delivery: a perspective on formulating poorly-water soluble compounds using wet media milling technology.
E. Merisko-Liversidge (2011)
Solid lipid nanoparticles
W. Mehnert (2012)
Developing nanocrystals for cancer treatment.
Yi Lu (2015)See more