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    Design, characterization, and evaluation of a polymeric nanofiber system for sublingual delivery of aceclofenac: A promising approach for enhanced pain management

    Year: 2023

    Journal: Journal of Drug Delivery Science and Technology, Volume 88, 2023-10-01, page 104893

    Authors: Köse Özkan, Cansel; Tort, Serdar; Aksoy, Okan Ali; Çotaoğlu, Merve Zanbak; Eşim, Özgür; Savaşer, Ayhan; Özkan, Yalçın

    Keywords: Aceclofenac; Electrospinning; In vivo evaluation; Polymer nanofiber; Sublingual delivery

    Effective pain management is crucial for improving the quality of life for patients with various medical conditions. Nonsteroidal anti-inflammatory drugs (NSAIDs) such as aceclofenac are commonly used to provide relief from pain due to their anti-inflammatory and analgesic properties. However, the traditional oral administration of aceclofenac has its limitations. These limitations include delayed onset of action, variability in drug absorption, and potential gastrointestinal side effects. To overcome these challenges, this study focuses on developing a polymeric nanofiber system for the sublingual administration of aceclofenac. Polymeric nanofibers offer unique characteristics like a high surface area to volume ratio and controlled release properties. The researchers utilized the electrospinning technique to produce these nanofibers, which allows precise control over fiber diameter, porosity, and drug loading. The main goal of this research is to gain insights into the potential of polymeric nanofibers as a new approach for the sublingual administration of aceclofenac. Nanofibers were produced with hydrophilic PVP polymer at three different polymer:drug ratios. All formulations were electrospun successfully with mean diameter of <1 μm. The tensile strength and elongation at break values were found between 1.86 to 3.58 MPa and 19.2–27.7%, respectively. In vitro dissolution studies demonstrated rapid and high drug release from the nanofibers indicating their potential for quick onset of action. Aceclofenac containing nanofibers provided more than 85% release profile within 15 min. In vivo tests conducted using an appropriate animal model showed that the sublingual nanofiber system resulted in significantly higher Cmax values compared to oral and intravenous methods of administration. Specifically, the Cmax value for sublingual administration was 0.262 ± 0.051 g/mL, while it was 0.247 ± 0.015 g/mL for oral administration and 0.154 ± 0.014 g/mL for intravenous administration. Moreover, when comparing AUC values among different methods of administration, the sublingual nanofiber system had a significantly higher AUC (AUC: 1.215 ± 0.074) compared to both oral (AUC: 0.767 ± 0.066) and intravenous (AUC: 0.331 ± 0.055) administration. Overall, this study highlights the potential of using polymeric nanofibers for the sublingual administration of aceclofenac as an alternative to traditional oral methods. The results suggest that this approach could offer improved drug release kinetics and higher drug concentrations in the body, which may enhance pain management for patients with various medical conditions. This valuable information may contribute towards creating an efficient and patient-focused alternative option for conventional oral formulations used in pain relief treatment.
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