Hydrocortisone nanosuspensions for ophthalmic delivery: A comparative study between microfluidic nanoprecipitation and wet milling

Recently, drug nanosuspensions have shown a potential for ophthalmic delivery. In this study, a hydrocortisone (HC) nanosuspension (NS) was developed using microfluidic nanoprecipitation as a recent, simple and cost-effective bottom-up technique of drug nanonization. For comparison, a second HC NS w...

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Published in:Journal of controlled release Vol. 149; no. 2; pp. 175 - 181
Main Authors: Ali, Hany S.M., York, Peter, Ali, Ahmed M.A., Blagden, Nicholas
Format: Journal Article
Language:English
Published: Kidlington Elsevier B.V 20-01-2011
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Abstract Recently, drug nanosuspensions have shown a potential for ophthalmic delivery. In this study, a hydrocortisone (HC) nanosuspension (NS) was developed using microfluidic nanoprecipitation as a recent, simple and cost-effective bottom-up technique of drug nanonization. For comparison, a second HC NS was prepared by top-down wet milling procedures. The produced nanosuspensions were characterized for particle size, shape and zeta potential. HC nanosuspensions of approximately 300 nm particle size were produced by adjusting experimental conditions of the two processing techniques. Results of X-ray diffraction and differential scanning calorimetry revealed that HC maintained the crystalline structure upon milling, while predominant amorphous particles were generated after precipitation. Ocular bioavailability of HC nanosuspensions was assessed in albino rabbits using HC solution as a control. A sustained drug action was maintained up to 9 h for the nanosuspensions compared to 5 h for the drug solution. The precipitated and milled NS achieved comparable AUC 0–9h values of 28.06 ± 4.08 and 30.95 ± 2.2, respectively, that were significantly ( P < 0.05) higher than that of HC solution (15.86 ± 2.7). After 2 months storage at room temperature, the milled HC NS showed good stability with no discernable changes in particle size, whereas the particle size of the precipitated HC NS increased to 440 nm. Changes in intraocular pressure (IOP) of Albino rabbits after administration of Hc solution and nanosuspensions produced by milling and precipitation. [Display omitted]
AbstractList Recently, drug nanosuspensions have shown a potential for ophthalmic delivery. In this study, a hydrocortisone (HC) nanosuspension (NS) was developed using microfluidic nanoprecipitation as a recent, simple and cost-effective bottom-up technique of drug nanonization. For comparison, a second HC NS was prepared by top-down wet milling procedures. The produced nanosuspensions were characterized for particle size, shape and zeta potential. HC nanosuspensions of approximately 300 nm particle size were produced by adjusting experimental conditions of the two processing techniques. Results of X-ray diffraction and differential scanning calorimetry revealed that HC maintained the crystalline structure upon milling, while predominant amorphous particles were generated after precipitation. Ocular bioavailability of HC nanosuspensions was assessed in albino rabbits using HC solution as a control. A sustained drug action was maintained up to 9 h for the nanosuspensions compared to 5 h for the drug solution. The precipitated and milled NS achieved comparable AUC sub(0-9h) values of 28.06 +/- 4.08 and 30.95 +/- 2.2, respectively, that were significantly (P < 0.05) higher than that of HC solution (15.86 +/- 2.7). After 2 months storage at room temperature, the milled HC NS showed good stability with no discernable changes in particle size, whereas the particle size of the precipitated HC NS increased to 440 nm.
Recently, drug nanosuspensions have shown a potential for ophthalmic delivery. In this study, a hydrocortisone (HC) nanosuspension (NS) was developed using microfluidic nanoprecipitation as a recent, simple and cost-effective bottom-up technique of drug nanonization. For comparison, a second HC NS was prepared by top-down wet milling procedures. The produced nanosuspensions were characterized for particle size, shape and zeta potential. HC nanosuspensions of approximately 300nm particle size were produced by adjusting experimental conditions of the two processing techniques. Results of X-ray diffraction and differential scanning calorimetry revealed that HC maintained the crystalline structure upon milling, while predominant amorphous particles were generated after precipitation. Ocular bioavailability of HC nanosuspensions was assessed in albino rabbits using HC solution as a control. A sustained drug action was maintained up to 9h for the nanosuspensions compared to 5h for the drug solution. The precipitated and milled NS achieved comparable AUC(0-9h) values of 28.06±4.08 and 30.95±2.2, respectively, that were significantly (P&lt;0.05) higher than that of HC solution (15.86±2.7). After 2 months storage at room temperature, the milled HC NS showed good stability with no discernable changes in particle size, whereas the particle size of the precipitated HC NS increased to 440nm.
Recently, drug nanosuspensions have shown a potential for ophthalmic delivery. In this study, a hydrocortisone (HC) nanosuspension (NS) was developed using microfluidic nanoprecipitation as a recent, simple and cost-effective bottom-up technique of drug nanonization. For comparison, a second HC NS was prepared by top-down wet milling procedures. The produced nanosuspensions were characterized for particle size, shape and zeta potential. HC nanosuspensions of approximately 300 nm particle size were produced by adjusting experimental conditions of the two processing techniques. Results of X-ray diffraction and differential scanning calorimetry revealed that HC maintained the crystalline structure upon milling, while predominant amorphous particles were generated after precipitation. Ocular bioavailability of HC nanosuspensions was assessed in albino rabbits using HC solution as a control. A sustained drug action was maintained up to 9 h for the nanosuspensions compared to 5 h for the drug solution. The precipitated and milled NS achieved comparable AUC 0–9h values of 28.06 ± 4.08 and 30.95 ± 2.2, respectively, that were significantly ( P < 0.05) higher than that of HC solution (15.86 ± 2.7). After 2 months storage at room temperature, the milled HC NS showed good stability with no discernable changes in particle size, whereas the particle size of the precipitated HC NS increased to 440 nm. Changes in intraocular pressure (IOP) of Albino rabbits after administration of Hc solution and nanosuspensions produced by milling and precipitation. [Display omitted]
Recently, drug nanosuspensions have shown a potential for ophthalmic delivery. In this study, a hydrocortisone (HC) nanosuspension (NS) was developed using microfluidic nanoprecipitation as a recent, simple and cost-effective bottom-up technique of drug nanonization. For comparison, a second HC NS was prepared by top-down wet milling procedures. The produced nanosuspensions were characterized for particle size, shape and zeta potential. HC nanosuspensions of approximately 300nm particle size were produced by adjusting experimental conditions of the two processing techniques. Results of X-ray diffraction and differential scanning calorimetry revealed that HC maintained the crystalline structure upon milling, while predominant amorphous particles were generated after precipitation. Ocular bioavailability of HC nanosuspensions was assessed in albino rabbits using HC solution as a control. A sustained drug action was maintained up to 9h for the nanosuspensions compared to 5h for the drug solution. The precipitated and milled NS achieved comparable AUC₀–₉ₕ values of 28.06±4.08 and 30.95±2.2, respectively, that were significantly (P<0.05) higher than that of HC solution (15.86±2.7). After 2months storage at room temperature, the milled HC NS showed good stability with no discernable changes in particle size, whereas the particle size of the precipitated HC NS increased to 440nm.
Recently, drug nanosuspensions have shown a potential for ophthalmic delivery. In this study, a hydrocortisone (HC) nanosuspension (NS) was developed using microfluidic nanoprecipitation as a recent, simple and cost-effective bottom-up technique of drug nanonization. For comparison, a second HC NS was prepared by top-down wet milling procedures. The produced nanosuspensions were characterized for particle size, shape and zeta potential. HC nanosuspensions of approximately 300nm particle size were produced by adjusting experimental conditions of the two processing techniques. Results of X-ray diffraction and differential scanning calorimetry revealed that HC maintained the crystalline structure upon milling, while predominant amorphous particles were generated after precipitation. Ocular bioavailability of HC nanosuspensions was assessed in albino rabbits using HC solution as a control. A sustained drug action was maintained up to 9h for the nanosuspensions compared to 5h for the drug solution. The precipitated and milled NS achieved comparable AUC(0-9h) values of 28.06±4.08 and 30.95±2.2, respectively, that were significantly (P<0.05) higher than that of HC solution (15.86±2.7). After 2 months storage at room temperature, the milled HC NS showed good stability with no discernable changes in particle size, whereas the particle size of the precipitated HC NS increased to 440nm.
Author Blagden, Nicholas
York, Peter
Ali, Ahmed M.A.
Ali, Hany S.M.
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  givenname: Hany S.M.
  surname: Ali
  fullname: Ali, Hany S.M.
  email: hsmali@bradford.ac.uk, hafandy2000@yahoo.com
  organization: Institute of Pharmaceutical Innovation, University of Bradford, Bradford, BD7 1DP, UK
– sequence: 2
  givenname: Peter
  surname: York
  fullname: York, Peter
  organization: Institute of Pharmaceutical Innovation, University of Bradford, Bradford, BD7 1DP, UK
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  givenname: Ahmed M.A.
  surname: Ali
  fullname: Ali, Ahmed M.A.
  organization: Department of Pharmaceutics, Faculty of Pharmacy, Beni Suief University, Egypt
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  givenname: Nicholas
  surname: Blagden
  fullname: Blagden, Nicholas
  email: n.blagden@bradford.ac.uk
  organization: Institute of Pharmaceutical Innovation, University of Bradford, Bradford, BD7 1DP, UK
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https://www.ncbi.nlm.nih.gov/pubmed/20946923$$D View this record in MEDLINE/PubMed
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Fri Feb 23 02:28:56 EST 2024
IsPeerReviewed true
IsScholarly true
Issue 2
Keywords Nanosuspension
Hydrocortisone
Ophthalmic delivery
Controlled release
Microfluidics
Milling
Corticosteroid
Pharmaceutical technology
Steroid hormone
Controlled release form
Control release polymer
Antiinflammatory agent
Grinding(comminution)
Ophthalmic preparation
Adrenal hormone
Dosage form
Comparative study
Nanotechnology
Language English
License CC BY 4.0
Copyright © 2010 Elsevier B.V. All rights reserved.
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MergedId FETCHMERGED-LOGICAL-c450t-dc6b70ae1aa9564b7272abd326ba1e44744aee1060328c95dd6f36748d355b8e3
Notes http://dx.doi.org/10.1016/j.jconrel.2010.10.007
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ObjectType-Feature-2
content type line 23
ObjectType-Article-2
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PMID 20946923
PQID 843412475
PQPubID 23479
PageCount 7
ParticipantIDs proquest_miscellaneous_899163135
proquest_miscellaneous_843412475
crossref_primary_10_1016_j_jconrel_2010_10_007
pubmed_primary_20946923
pascalfrancis_primary_23769318
fao_agris_US201500181616
elsevier_sciencedirect_doi_10_1016_j_jconrel_2010_10_007
PublicationCentury 2000
PublicationDate 2011-01-20
PublicationDateYYYYMMDD 2011-01-20
PublicationDate_xml – month: 01
  year: 2011
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PublicationDecade 2010
PublicationPlace Kidlington
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PublicationTitle Journal of controlled release
PublicationTitleAlternate J Control Release
PublicationYear 2011
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Elsevier
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– name: Elsevier
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Snippet Recently, drug nanosuspensions have shown a potential for ophthalmic delivery. In this study, a hydrocortisone (HC) nanosuspension (NS) was developed using...
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SubjectTerms Animals
bioavailability
Biological and medical sciences
Biological Availability
Chemical Precipitation
Controlled release
cortisol
cost effectiveness
crystal structure
differential scanning calorimetry
Drug Carriers - chemistry
Drug Compounding - methods
drugs
Eye - metabolism
General pharmacology
Hydrocortisone
Hydrocortisone - administration & dosage
Hydrocortisone - pharmacokinetics
Male
Medical sciences
Microfluidics
Milling
Nanostructures - chemistry
Nanosuspension
Nanotechnology - methods
Ophthalmic delivery
Ophthalmic Solutions
Particle Size
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Rabbits
Solutions
Suspensions
temperature
wet milling
Wettability
X-ray diffraction
zeta potential
Title Hydrocortisone nanosuspensions for ophthalmic delivery: A comparative study between microfluidic nanoprecipitation and wet milling
URI https://dx.doi.org/10.1016/j.jconrel.2010.10.007
https://www.ncbi.nlm.nih.gov/pubmed/20946923
https://search.proquest.com/docview/843412475
https://search.proquest.com/docview/899163135
Volume 149
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