Flurbiprofen-encapsulated microsphere laden into heat-triggered situ gel for ocular delivery

<div style="color: rgb(119, 119, 119); font-family: Montserrat, sans-serif; font-variant-ligatures: normal; orphans: 2; widows: 2; text-decoration-thickness: initial; text-decoration-style: initial; text-decoration-color: initial; line-height: 18px !important;"><div classname="from-journal-content text-justify" style="line-height: 18px !important; letter-spacing: 0px !important;"><p style="margin-bottom: 20px; line-height: 18px !important; letter-spacing: 0px !important;"><strong>Background and Aims:</strong>&nbsp;This investigation aimed to enhance flurbiprofen’s (FB) pre-corneal residence period and ocular availability in the postoperative management of ocular inflammation. <p style="margin-bottom: 20px; line-height: 18px !important; letter-spacing: 0px !important;"><strong>Methods:&nbsp;</strong>The microsphere (MS) material was poly (lactic-co-glycolic acid) PLGA, and FB-laden microspheres were prepared using a single emulsification/solvent evaporation process, loaded onto thermosensitive in situ gels, and then characterised. <p style="margin-bottom: 20px; line-height: 18px !important; letter-spacing: 0px !important;"><strong>Results:&nbsp;</strong>The size of the microparticles was measured as 19.3±2.1 μm. Entrapment efficiency, zeta potential, and in vitro release; it was observed that the microspheres were released for six days. The optimum gelling capacity was obtained using 15% Poloxamer 407, 8% Poloxamer 188, and 1% HEC (viscosity 80-125 cp). Poloxamer 407 concentration was reduced, resulting in increased gelation temperature and duration. It was determined that the gelling temperature of the selected formulation was 35±0.1 °C, the pH was 6.9±0.02, and the viscosity at the gelling temperature was 11042±247 cP. The addition of hydroxyethyl cellulose increased the mucoadhesive strength. - in vitro release of FB from FB-PLGA MS followed the Korsmeyer-Peppas model , –, and the in situ gel preparation was found to be compatible with the Peppas-Sahlin model. In addition, MTT analysis of the ARPE-19 cell line revealed that the in situ gel formulation was biocompatible. <p style="margin-bottom: 20px; line-height: 18px !important; letter-spacing: 0px !important;"><strong>Conclusion:</strong>&nbsp;Flurbiprofen release was sustained, ocular availability was improved, and residence time was increased when flurbiprofen-loaded microspheres were incorporated into in situ gel bases. </div></div><div class="mt-2" style="color: rgb(119, 119, 119); font-family: Montserrat, sans-serif; font-variant-ligatures: normal; orphans: 2; widows: 2; text-decoration-thickness: initial; text-decoration-style: initial; text-decoration-color: initial; line-height: 18px !important; margin-top: 0.5rem !important;"><b>Anahtar Kelimeler:&nbsp;</b><a class="from-journal" href="https://iupress.istanbul.edu.tr/tr/journal/ijp/article/flurbiprofen-encapsulated-microsphere-laden-into-heat-triggered-situ-gel-for-ocular-delivery#" style="color: rgb(105, 158, 163) !important; letter-spacing: 0px !important; outline-color: currentcolor !important; outline-style: none !important;">Flurbiprofen</a>,&nbsp;<a class="from-journal" href="https://iupress.istanbul.edu.tr/tr/journal/ijp/article/flurbiprofen-encapsulated-microsphere-laden-into-heat-triggered-situ-gel-for-ocular-delivery#" style="color: rgb(105, 158, 163) !important; letter-spacing: 0px !important; outline-color: currentcolor !important; outline-style: none !important;">Poloxamer Gel</a>,&nbsp;<a class="from-journal" href="https://iupress.istanbul.edu.tr/tr/journal/ijp/article/flurbiprofen-encapsulated-microsphere-laden-into-heat-triggered-situ-gel-for-ocular-delivery#" style="color: rgb(105, 158, 163) !important; letter-spacing: 0px !important; outline-color: currentcolor !important; outline-style: none !important;">Ocular Gel</a>,&nbsp;<a class="from-journal" href="https://iupress.istanbul.edu.tr/tr/journal/ijp/article/flurbiprofen-encapsulated-microsphere-laden-into-heat-triggered-situ-gel-for-ocular-delivery#" style="color: rgb(105, 158, 163) !important; letter-spacing: 0px !important; outline-color: currentcolor !important; outline-style: none !important;">PLGA Microsphere</a>,&nbsp;<a class="from-journal" href="https://iupress.istanbul.edu.tr/tr/journal/ijp/article/flurbiprofen-encapsulated-microsphere-laden-into-heat-triggered-situ-gel-for-ocular-delivery#" style="color: rgb(105, 158, 163) !important; letter-spacing: 0px !important; outline-color: currentcolor !important; outline-style: none !important;">Release Kinetics</a></div>

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Publication Details

Journal
Istanbul Journal of Pharmacy
Published
2024-08-26
DOI
https://doi.org/10.26650/istanbuljpharm.2024.1269717
Primary Topic
Ocular Surface and Contact Lens
Type
article
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article

Flurbiprofen-encapsulated microsphere laden into heat-triggered situ gel for ocular delivery

Sedat Ünal, Heybet Kerem Polat
Istanbul Journal of Pharmacy
Ocular Surface and Contact Lens
article

Flurbiprofen-encapsulated microsphere laden into heat-triggered situ gel for ocular delivery

Sedat Ünal, Heybet Kerem Polat
article en

Abstract

<div style="color: rgb(119, 119, 119); font-family: Montserrat, sans-serif; font-variant-ligatures: normal; orphans: 2; widows: 2; text-decoration-thickness: initial; text-decoration-style: initial; text-decoration-color: initial; line-height: 18px !important;"><div classname="from-journal-content text-justify" style="line-height: 18px !important; letter-spacing: 0px !important;"><p style="margin-bottom: 20px; line-height: 18px !important; letter-spacing: 0px !important;"><strong>Background and Aims:</strong>&nbsp;This investigation aimed to enhance flurbiprofen’s (FB) pre-corneal residence period and ocular availability in the postoperative management of ocular inflammation. <p style="margin-bottom: 20px; line-height: 18px !important; letter-spacing: 0px !important;"><strong>Methods:&nbsp;</strong>The microsphere (MS) material was poly (lactic-co-glycolic acid) PLGA, and FB-laden microspheres were prepared using a single emulsification/solvent evaporation process, loaded onto thermosensitive in situ gels, and then characterised. <p style="margin-bottom: 20px; line-height: 18px !important; letter-spacing: 0px !important;"><strong>Results:&nbsp;</strong>The size of the microparticles was measured as 19.3±2.1 μm. Entrapment efficiency, zeta potential, and in vitro release; it was observed that the microspheres were released for six days. The optimum gelling capacity was obtained using 15% Poloxamer 407, 8% Poloxamer 188, and 1% HEC (viscosity 80-125 cp). Poloxamer 407 concentration was reduced, resulting in increased gelation temperature and duration. It was determined that the gelling temperature of the selected formulation was 35±0.1 °C, the pH was 6.9±0.02, and the viscosity at the gelling temperature was 11042±247 cP. The addition of hydroxyethyl cellulose increased the mucoadhesive strength. - in vitro release of FB from FB-PLGA MS followed the Korsmeyer-Peppas model , –, and the in situ gel preparation was found to be compatible with the Peppas-Sahlin model. In addition, MTT analysis of the ARPE-19 cell line revealed that the in situ gel formulation was biocompatible. <p style="margin-bottom: 20px; line-height: 18px !important; letter-spacing: 0px !important;"><strong>Conclusion:</strong>&nbsp;Flurbiprofen release was sustained, ocular availability was improved, and residence time was increased when flurbiprofen-loaded microspheres were incorporated into in situ gel bases. </div></div><div class="mt-2" style="color: rgb(119, 119, 119); font-family: Montserrat, sans-serif; font-variant-ligatures: normal; orphans: 2; widows: 2; text-decoration-thickness: initial; text-decoration-style: initial; text-decoration-color: initial; line-height: 18px !important; margin-top: 0.5rem !important;"><b>Anahtar Kelimeler:&nbsp;</b><a class="from-journal" href="https://iupress.istanbul.edu.tr/tr/journal/ijp/article/flurbiprofen-encapsulated-microsphere-laden-into-heat-triggered-situ-gel-for-ocular-delivery#" style="color: rgb(105, 158, 163) !important; letter-spacing: 0px !important; outline-color: currentcolor !important; outline-style: none !important;">Flurbiprofen</a>,&nbsp;<a class="from-journal" href="https://iupress.istanbul.edu.tr/tr/journal/ijp/article/flurbiprofen-encapsulated-microsphere-laden-into-heat-triggered-situ-gel-for-ocular-delivery#" style="color: rgb(105, 158, 163) !important; letter-spacing: 0px !important; outline-color: currentcolor !important; outline-style: none !important;">Poloxamer Gel</a>,&nbsp;<a class="from-journal" href="https://iupress.istanbul.edu.tr/tr/journal/ijp/article/flurbiprofen-encapsulated-microsphere-laden-into-heat-triggered-situ-gel-for-ocular-delivery#" style="color: rgb(105, 158, 163) !important; letter-spacing: 0px !important; outline-color: currentcolor !important; outline-style: none !important;">Ocular Gel</a>,&nbsp;<a class="from-journal" href="https://iupress.istanbul.edu.tr/tr/journal/ijp/article/flurbiprofen-encapsulated-microsphere-laden-into-heat-triggered-situ-gel-for-ocular-delivery#" style="color: rgb(105, 158, 163) !important; letter-spacing: 0px !important; outline-color: currentcolor !important; outline-style: none !important;">PLGA Microsphere</a>,&nbsp;<a class="from-journal" href="https://iupress.istanbul.edu.tr/tr/journal/ijp/article/flurbiprofen-encapsulated-microsphere-laden-into-heat-triggered-situ-gel-for-ocular-delivery#" style="color: rgb(105, 158, 163) !important; letter-spacing: 0px !important; outline-color: currentcolor !important; outline-style: none !important;">Release Kinetics</a></div>

Istanbul Journal of PharmacyVol. 54(2)
Openalex Percentile: Top 79%
Ocular Surface and Contact Lens
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