Drug Polymeric Carrier of Aceclofenac Based on Amphiphilic Chitosan Micelles

Noof A Alenazi; Mohammed G Bokhari; Mohammed A S Abourehab; Mostafa R Abukhadra

doi:10.1021/acsomega.3c07065

Drug Polymeric Carrier of Aceclofenac Based on Amphiphilic Chitosan Micelles

ACS Omega. 2023 Dec 5;8(50):48145-48158. doi: 10.1021/acsomega.3c07065. eCollection 2023 Dec 19.

Authors

Noof A Alenazi¹, Mohammed G Bokhari^{2

3}, Mohammed A S Abourehab⁴, Mostafa R Abukhadra^{5

6}

Affiliations

¹ Department of Chemistry, College of Science and Humanities in Al-Kharj, Prince Sattam bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.
² Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Umm Al-Qura University, Makkah 21955, Saudi Arabia.
³ First Medical Zone, Al-Madinah Health Cluster, Ministry of Health, Riyadh 11176, Saudi Arabia.
⁴ Department of Pharmaceutics, Faculty of Pharmacy, Umm Al-Qura University, Makkah 21955, Saudi Arabia.
⁵ Materials Technologies and their Applications Lab, Geology Department, Faculty of Science, Beni-Suef University, Beni-Suef City 62511, Egypt.
⁶ Geology Department, Faculty of Science, Beni-Suef University, Beni-Suef city 62511, Egypt.

Abstract

Amphiphilic micelles based on chitosan (CS) were applied as drug carriers of aceclofenac (ACF) as a potential method to induce its bioavailability and therapeutic efficiency. N-octyl-N,O-succinyl CS (OSCS), an amphiphilic CS derivative, was successfully synthesized and loaded physically by ACF at different pH values and using different dosages of ACF, forming ACF-loaded polymeric micelles (PMs). The obtained PMs and ACF-loaded PMs were characterized by different analytical techniques, including AFM, TEM, DLS, UV-vis spectrophotometry, ¹H NMR spectroscopy, and FT-IR spectroscopy. The pH 5 sample with a 30% ACF/polymer ratio showed the highest ACF loading capacity (LC) and entrapment efficiency (EE). In vitro release behaviors of pure ACF and ACF-loaded PMs at each release point indicated that the release profile of pH-responsive PMs loaded with ACF demonstrated quicker release rates (94% after 480 min) compared to the release behavior noticed for free ACF (59.56% after 480 min). Furthermore, the release rates exhibit a notable rise when the pH is increased from 1.2 to 4.7. In the carrageenan-induced inflammation model of paw edema in rats, it has been demonstrated that the injection of ACF-loaded PMs (at a dose of 10 mg/kg) resulted in a strengthened inflammatory activity compared to the injection of free ACF at equivalent dosages as well as at time intervals. However, the use of ACF-loaded PMs for a duration of 6 h displayed a notable reduction of paw edema, with an inhibition percentage of 85.09%, in contrast to the 74.9% inhibition percentage observed for the free ACF medication.