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 |
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Main Authors: | , , , |
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Language: | English |
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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] |
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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<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. |
Author_xml | – sequence: 1 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 – sequence: 3 givenname: Ahmed M.A. surname: Ali fullname: Ali, Ahmed M.A. organization: Department of Pharmaceutics, Faculty of Pharmacy, Beni Suief University, Egypt – sequence: 4 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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Copyright | 2010 Elsevier B.V. 2015 INIST-CNRS Copyright © 2010 Elsevier B.V. All rights reserved. |
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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 |
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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 |
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