Online citations, reference lists, and bibliographies.
← Back to Search

Formulation Parameters Of Crystalline Nanosuspensions On Spray Drying Processing: A DoE Approach.

S Kumar, Xiaoming Xu, R. Gokhale, D. Burgess
Published 2014 · Materials Science, Medicine

Save to my Library
Download PDF
Analyze on Scholarcy
Nanocrystalline suspensions offer a promising approach to improve dissolution of BCS class II/IV compounds. Spray drying was utilized as a downstream process to improve the physical and chemical stability of dried nanocrystals. The effect of nanocrystalline suspension formulation variables on spray-drying processing was investigated. Naproxen and indomethacin nanocrystalline formulations were formulated with either Dowfax 2A1 (small molecule) or HPMC E15 (high molecular weight polymer) and spray drying was performed. A DoE approach was utilized to understand the effect of critical formulation variables, i.e. type of stabilizer, type of drug, ratio of drug-to-stabilizer and drug concentration. The powders were analyzed for particle size, moisture content, powder X-ray diffraction and dissolution. A dialysis sac adapter for USP apparatus II was developed which provided good discrimination between aggregated and non-aggregated formulations. Nanocrystal aggregation was dependent on the drug-to-stabilizer ratio. The glass transition temperature and the charge effect played a dominant role on spray-dried powder yield. Those formulations with low drug-to-excipient ratios were less aggregating and showed faster dissolution compared to those formulations with high drug-to-excipient ratios. All stable (less aggregated) formulations were subjected to accelerated storage stability testing. The Flory-Huggins interaction parameter (between drug and excipients) correlated with the spray-dried nanocrystal formulations stability.
This paper references
Microcrystalline cellulose, a useful alternative for sucrose as a matrix former during freeze-drying of drug nanosuspensions - a case study with itraconazole.
B. Van Eerdenbrugh (2008)
Nanosizing: a formulation approach for poorly-water-soluble compounds.
E. Merisko-Liversidge (2003)
Formulation and drying of miconazole and itraconazole nanosuspensions.
Ana M Cerdeira (2013)
Prediction of dexamethasone release from PLGA microspheres prepared with polymer blends using a design of experiment approach.
Bing Gu (2015)
Theoretical and Practical Approaches for Prediction of Drug–Polymer Miscibility and Solubility
Patrick J. Marsac (2006)
The rate of solution of solid substances in their own solutions
A. A. Noyes (1897)
Poor aqueous solubility-an industry wide problem in drug discovery
C. Lipinski (2002)
Drying of crystalline drug nanosuspensions-the importance of surface hydrophobicity on dissolution behavior upon redispersion.
B. Van Eerdenbrugh (2008)
Principles of polymer chemistry
P. J. Flory (1953)
Inhibition of sulfathiazole crystal growth by polyvinylpyrrolidone.
A. Simonelli (1970)
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
C. Lipinski (1997)
Conversion of Nanosuspensions into Dry Powders by Spray Drying: A Case Study
M. Chaubal (2008)
A comparative study of top-down and bottom-up approaches for the preparation of micro/nanosuspensions.
S. Verma (2009)
The role of solid nanoparticle technology in the parenteral delivery of poorly water-soluble drugs.
J. Kipp (2004)
Alternative matrix formers for nanosuspension solidification: Dissolution performance and X-ray microanalysis as an evaluation tool for powder dispersion.
B. Van Eerdenbrugh (2008)
Estimation of Drug–Polymer Miscibility and Solubility in Amorphous Solid Dispersions Using Experimentally Determined Interaction Parameters
Patrick J. Marsac (2008)
Drug-like properties and the causes of poor solubility and poor permeability.
C. Lipinski (2000)
DissoCubes—A Novel Formulation for Poorly Soluble and Poorly Bioavailable Drugs
R. Müller (2002)
Drug nano- and microparticles processed into solid dosage forms: physical properties.
J. Lee (2003)
Drug Nanoparticles: Formulating Poorly Water-Soluble Compounds
E. Merisko-Liversidge (2008)
High-throughput drug discovery: what can we expect from HTS?
P. Gribbon (2005)
Carboxymethyl Hyaluronan-Stabilized Nanoparticles for Anticancer Drug Delivery
J. Woodman (2015)
Crystallization of polymers
L. Mandelkern (2002)

This paper is referenced by
Binary Amorphous Solid Dispersion:Method and Application
Kedar Asmita Khandu (2020)
Vicissitudes of liquid crystals for solubility enhancement of poorly soluble drugs
A. Shoaib (2021)
Formulation and performance of Irbesartan nanocrystalline suspension and granulated or bead-layered dried powders - Part I.
Saikishore Meruva (2019)
Advantages and challenges of the spray-drying technology for the production of pure drug particles and drug-loaded polymeric carriers.
A. Sosnik (2015)
Selection of a Nanoparticle Stabilizer for a Calcium Phosphate Drug Delivery System
J. Woodman (2014)
Novel Application of Twin Screw Extruder on Production of Diverse Formulations
Xingyou Ye (2018)
Spray-dried nanocrystals for a highly hydrophobic drug: Increased drug loading, enhanced redispersity, and improved oral bioavailability.
Y. Hou (2017)
Preparation, Physicochemical Characterisation and DoE Optimisation of a Spray-Dried Dry Emulsion Platform for Delivery of a Poorly Soluble Drug, Simvastatin
Mitja Pohlen (2020)
In Vitro and In Vivo Performance of Different Sized Spray-Dried Crystalline Itraconazole.
S Kumar (2015)
Multi Criteria Decision Making to Select the Suitable Method for the Preparation of Nanocrystals Using an Analytic Hierarchy Process
Venkatesh Kyavars (2017)
Optimization and evaluation of cyclosporine A nanosuspension stabilized by combination stabilizers using high pressure homogenization method
Sıla Gülbağ Pinar (2019)
Bumping UBM metal residue defect analysis and improvement using techniques of design of experiment (DOE)
L. Chen (2017)
Production of nano-solid dispersions using a novel solvent-controlled precipitation process - Benchmarking their in vivo performance with an amorphous micro-sized solid dispersion produced by spray drying.
Íris Duarte (2016)
Design and synthesis of a novel multifunctional stabilizer for highly stable dl-tetrahydropalmatine nanosuspensions and in vitro study
B. Yan (2018)
Sugars as bulking agents to prevent nano-crystal aggregation during spray or freeze-drying.
S Kumar (2014)
Role of Wetting Agents and Disintegrants in Development of Danazol Nanocrystalline Tablets.
Saikishore Meruva (2020)
Optimization and dissolution performance of spray-dried naproxen nano-crystals.
S Kumar (2015)
Development of PLGA Microsphere/PVA Hydrogel Composite Coatings for Long-Term Biosensor Functioning
B. Gu (2016)
The dispersion releaser technology is an effective method for testing drug release from nanosized drug carriers
C. Janas (2017)
Formulation of nimodipine nanocrystals for oral administration
Jianwen Li (2016)
Downstream Processing of Irbesartan Nanocrystalline Suspension and Mini-Tablet Development - Part II.
Saikishore Meruva (2019)
Development and solidification of multifunction stabilizers formulated self-assembled core-shell Deacetyl mycoepoxydience nanosuspensions
Y. Ma (2020)
Menetelmiä nanokiteiden liukenemisnopeuden tutkimiseksi
Anu Piipponen (2016)
Investigation of Formulation and Process Parameters of Wet Media Milling to Develop Etodolac Nanosuspensions
A. Karakucuk (2020)
Nanosuspension drug delivery system: preparation, characterization, postproduction processing, dosage form, and application
Jiuhong Zhang (2017)
Dissolution of Nanoparticle Drug Formulations
John L. Bullock (2017)
Nanosuspensions of poorly water-soluble drugs prepared by bottom-up technologies.
J. Du (2015)
Carboxymethyl Hyaluronan-Stabilized Nanoparticles for Anticancer Drug Delivery
J. Woodman (2015)
Analyzing drug load and release from pharmaceutical nanocarriers for the treatment of inflammatory bowel diseases
A. Guillot (2014)
A recent trend of drug-nanoparticles in suspension for the application in drug delivery.
Gurpreet S. Suri (2016)
Prediction of dexamethasone release from PLGA microspheres prepared with polymer blends using a design of experiment approach.
Bing Gu (2015)
Optimization of the Büchi B-90 spray drying process using central composite design for preparation of solid dispersions.
Bing Gu (2015)
See more
Semantic Scholar Logo Some data provided by SemanticScholar