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Optimization And Evaluation Of Cyclosporine A Nanosuspension Stabilized By Combination Stabilizers Using High Pressure Homogenization Method

Sıla Gülbağ Pinar, N. Çelebi
Published 2019 · Materials Science

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The purpose of this study was to develop Cyclosporine A (CsA) nanosuspension by using different stabilizers for oral administration. CsA nanosuspension was prepared by high pressure homogenization technology and HPMC and Soluplus® combination were selected as stabilizers. After Design of Experiment (DoE) analysis, optimum formulation was selected and characterized by particle size (PS), particle size distribution (PDI) and zeta potential (ZP) measurements. Scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction (X-RD), and fourier transform infrared (FTIR) analysis were also performed. Solubility studies were done with optimum lyophilised CsA nanosuspension. The results revealed that appropriate PS, PDI, and ZP results were not obtained with the use of stabilizers separately in preformulation studies. Optimum stabilizers ratio was determined CsA:HPMC:Soluplus® 1:1:0.5 (w/w) in nanosuspension formulation after DoE. It was found to be appropriate with a small particle size of 366.8 ± 9.6 nm, a narrow particle size distribution of 0.48 ± 0.02, and a negative zeta potential value of -14.4 ± 0.4 mV after 30 homogenization cycles. In solubility study, the CsA solubility in the nanosuspension was increased up to 2.1 times in comparison with the coarse CsA. CsA nanosuspension showed a short-term stability over the examined period of one month. CsA nanosuspension can be successfully produced by Microfluidics with HPMC:Soluplus® combination as stabilizers using DoE approach.
This paper references
10.1016/j.jconrel.2013.08.006
Stability of nanosuspensions in drug delivery.
Y. Wang (2013)
10.1016/j.ijpharm.2009.05.006
Quality by design approach to understand the process of nanosuspension preparation.
S. Verma (2009)
10.1016/j.ijpharm.2010.07.044
Nanocrystals: industrially feasible multifunctional formulation technology for poorly soluble actives.
R. Shegokar (2010)
10.1016/j.jconrel.2016.01.056
Reformulating cyclosporine A (CsA): More than just a life cycle management strategy.
M. Guada (2016)
10.1016/j.ejpb.2018.06.022
Increased bioavailability of efonidipine hydrochloride nanosuspensions by the wet‐milling method
S. Huang (2018)
10.1016/j.ijpharm.2011.04.023
Docetaxel-loaded-lipid-based-nanosuspensions (DTX-LNS): preparation, pharmacokinetics, tissue distribution and antitumor activity.
L. Wang (2011)
10.1016/j.ijpharm.2015.09.021
Nanosuspensions of poorly water-soluble drugs prepared by bottom-up technologies.
J. Du (2015)
10.1016/j.ijpharm.2007.12.016
Studies on pharmacokinetics and tissue distribution of oridonin nanosuspensions.
L. Gao (2008)
10.1016/J.JDDST.2018.03.005
Preparation and characterization of furosemide nanosuspensions
Tugba Gulsun (2018)
10.1016/J.POWTEC.2016.09.004
Design of experiment approach in development of febuxostat nanocrystal: Application of Soluplus® as stabilizer
O. P. Sharma (2016)
10.1016/j.ijpharm.2017.03.068
Computational and experimental approaches for development of methotrexate nanosuspensions by bottom-up nanoprecipitation.
A. D. dos Santos (2017)
Nanocrystal Technology For Oral Delivery of Poorly Water-Soluble Drugs
Tuğba Gülsün (2011)
10.1016/j.ijpharm.2012.09.034
Drug nanocrystals in the commercial pharmaceutical development process.
J. Möschwitzer (2013)
10.1016/j.biotechadv.2011.03.004
Cyclosporin A--a review on fermentative production, downstream processing and pharmacological applications.
S. Survase (2011)
10.1016/J.EJPB.2004.03.022
Development of an intravenously injectable chemically stable aqueous omeprazole formulation using nanosuspension technology.
J. Möschwitzer (2004)
10.1039/C6RA28676C
Preparation and evaluation of celecoxib nanosuspensions for bioavailability enhancement
He Jiali (2017)
10.2147/IJN.S595
Nanocrystal technology, drug delivery and clinical applications
Jens-Uwe A. H. Junghanns (2008)
10.1016/J.EJPB.2005.05.009
Drug nanocrystals of poorly soluble drugs produced by high pressure homogenisation.
C. Keck (2006)
10.1016/j.ejps.2010.04.006
Preparation of stable nitrendipine nanosuspensions using the precipitation-ultrasonication method for enhancement of dissolution and oral bioavailability.
Dengning Xia (2010)
10.1016/j.ijpharm.2014.10.044
Effects of stabilizing agents on the development of myricetin nanosuspension and its characterization: an in vitro and in vivo evaluation.
C. Hong (2014)
10.1016/j.ijpharm.2017.08.082
Formulation and characterization of biocompatible and stable I.V. itraconazole nanosuspensions stabilized by a new stabilizer polyethylene glycol-poly(β-Benzyl-l-aspartate) (PEG-PBLA).
Lanlan Zong (2017)
10.1016/j.ijpharm.2011.05.075
Preparation and antitumor study of camptothecin nanocrystals.
H. Zhang (2011)
10.1016/j.ijpharm.2018.02.011
Optimization of formulation and process parameters for the production of carvedilol nanosuspension by wet media milling.
Djordje P Medarević (2018)
Pharmaceutical nanocrystals
GD Wang (2012)
10.1002/jps.23475
Performance comparison of two novel combinative particle-size-reduction technologies.
J. Salazar (2013)
10.1016/J.EJPB.2005.09.005
Spray coated pellets as carrier system for mucoadhesive drug nanocrystals.
J. Möschwitzer (2006)
10.1016/J.JDDST.2019.01.034
Preparation, optimization of intravenous ZL-004 nanosuspensions by the precipitation method, effect of particle size on in vivo pharmacokinetics and tissue distribution
Chengyue Guo (2019)
10.1016/j.jsps.2017.07.004
Ibuprofen nanocrystals developed by 22 factorial design experiment: A new approach for poorly water-soluble drugs
A. R. Fernandes (2017)
10.1016/j.ijpharm.2014.01.013
Formulation parameters of crystalline nanosuspensions on spray drying processing: a DoE approach.
S Kumar (2014)
10.1016/J.IJPHARM.2006.02.045
Oral bioavailability of cyclosporine: solid lipid nanoparticles (SLN) versus drug nanocrystals.
R. Mueller (2006)
10.1016/j.jconrel.2013.12.018
Development and evaluation of transferrin-stabilized paclitaxel nanocrystal formulation.
Y. Lu (2014)
10.1016/j.ijpharm.2017.02.065
Production of aprepitant nanocrystals by wet media milling and subsequent solidification.
F. Toziopoulou (2017)
10.1016/j.ejps.2016.05.010
Preparation of ritonavir nanosuspensions by microfluidization using polymeric stabilizers: I. A Design of Experiment approach.
A. Karakucuk (2016)
10.1016/j.ijpharm.2013.10.025
Systematic investigation of the cavi-precipitation process for the production of ibuprofen nanocrystals.
Biswadip Sinha (2013)
10.1016/j.ijpharm.2013.06.050
Study on formability of solid nanosuspensions during nanodispersion and solidification: I. Novel role of stabilizer/drug property.
P. Yue (2013)
10.1016/j.ejpb.2011.12.015
Nanocrystals: comparison of the size reduction effectiveness of a novel combinative method with conventional top-down approaches.
J. Salazar (2012)
10.1016/j.ejps.2018.07.009
Dermal flurbiprofen nanosuspensions: Optimization with design of experiment approach and in vitro evaluation
A. N. Oktay (2018)
10.1016/j.jsps.2015.03.008
Enhanced ex vivo intestinal absorption of olmesartan medoxomil nanosuspension: Preparation by combinative technology
Zenab Attari (2016)
10.1016/j.ejps.2018.08.003
Pramipexole nanocrystals for transdermal permeation: Characterization and its enhancement micro‐mechanism
Y. Li (2018)



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