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Soluplus® promotes efficient transport of meloxicam to the central nervous system via nasal administration.
Sipos, Bence; Bella, Zsolt; Gróf, Ilona; Veszelka, Szilvia; Deli, Mária A; Szucs, Kálmán F; Sztojkov-Ivanov, Anita; Ducza, Eszter; Gáspár, Róbert; Kecskeméti, Gábor; Janáky, Tamás; Volk, Balázs; Budai-Szucs, Mária; Ambrus, Rita; Szabó-Révész, Piroska; Csóka, Ildikó; Katona, Gábor.
Affiliation
  • Sipos B; Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös Str. 6, H-6720 Szeged, Hungary.
  • Bella Z; Department of Oto-Rhino-Laryngology and Head-Neck Surgery, University of Szeged, Tisza Lajos Blvd. 111, H-6725 Szeged, Hungary.
  • Gróf I; Institute of Biophysics, Biological Research Centre, Szeged, Temesvári Blvd. 62, H-6726 Szeged, Hungary.
  • Veszelka S; Institute of Biophysics, Biological Research Centre, Szeged, Temesvári Blvd. 62, H-6726 Szeged, Hungary.
  • Deli MA; Institute of Biophysics, Biological Research Centre, Szeged, Temesvári Blvd. 62, H-6726 Szeged, Hungary.
  • Szucs KF; Department of Pharmacology and Pharmacotherapy, Albert Szent-Györgyi Medical School, Faculty of Medicine, University of Szeged, Hungary.
  • Sztojkov-Ivanov A; Department of Pharmacodynamics and Biopharmacy, Faculty of Pharmacy, University of Szeged, Eötvös Str. 6, H-6720 Szeged, Hungary.
  • Ducza E; Department of Pharmacodynamics and Biopharmacy, Faculty of Pharmacy, University of Szeged, Eötvös Str. 6, H-6720 Szeged, Hungary.
  • Gáspár R; Department of Pharmacology and Pharmacotherapy, Albert Szent-Györgyi Medical School, Faculty of Medicine, University of Szeged, Hungary.
  • Kecskeméti G; Department of Medical Chemistry, Interdisciplinary Excellence Centre, University of Szeged, Dóm square 8, H-6720 Szeged, Hungary.
  • Janáky T; Department of Medical Chemistry, Interdisciplinary Excellence Centre, University of Szeged, Dóm square 8, H-6720 Szeged, Hungary.
  • Volk B; Directorate of Drug Substance Development, Egis Pharmaceuticals Plc., Keresztúri Str. 30 - 38, H-1106 Budapest, Hungary.
  • Budai-Szucs M; Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös Str. 6, H-6720 Szeged, Hungary.
  • Ambrus R; Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös Str. 6, H-6720 Szeged, Hungary.
  • Szabó-Révész P; Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös Str. 6, H-6720 Szeged, Hungary.
  • Csóka I; Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös Str. 6, H-6720 Szeged, Hungary.
  • Katona G; Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös Str. 6, H-6720 Szeged, Hungary. Electronic address: katona.gabor@szte.hu.
Int J Pharm ; 632: 122594, 2023 Feb 05.
Article in En | MEDLINE | ID: mdl-36626972
ABSTRACT
In our present series of experiments, we investigated the nasal applicability of the previously developed Soluplus® - meloxicam polymeric micelle formulation. Utilizing the nasal drug investigations, moderately high mucoadhesion was experienced in nasal conditions which alongside the appropriate physicochemical properties in liquid state, contributed to rapid drug absorption through human RPMI 2650 cell line. Ex vivo studies also confirmed that higher nasal mucosal permeation could be expected with the polymeric micelle nanoformulation compared to a regular MEL suspension. Also, the nanoformulation met the requirements to provide rapid drug permeation in less 1 h of our measurement. The non-toxic, non-cell barrier damaging formulation also proved to provide a successful passive transport across excides human nasal mucosa. Based on our in vivo investigations, it can be concluded that the polymeric micelle formulation provides higher meloxicam transport to the central nervous system followed by a slow and long-lasting elimination process compared to prior results where physical particle size reduction methods were applied. With these results, a promising solution and nanocarrier is proposed for the successful transport of non-steroidal anti-inflammatory drugs with acidic character to the brain.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Micelles / Nasal Mucosa Limits: Humans Language: En Journal: Int J Pharm Year: 2023 Document type: Article Affiliation country: Hungary

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Micelles / Nasal Mucosa Limits: Humans Language: En Journal: Int J Pharm Year: 2023 Document type: Article Affiliation country: Hungary
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