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Article

Enhanced Solubility and Biological Activity of Dexibuprofen-Loaded Silica-Based Ternary Solid Dispersions

1
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad 38000, Pakistan
2
Department of Medicine, Faisalabad Medical University, Allied Hospital, Faisalabad 38000, Pakistan
3
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad 38000, Pakistan
4
Department of Physiology, Government College University Faisalabad, Faisalabad 38000, Pakistan
5
Department of Medical Laboratory Technology, Faculty of Applied Medical Sciences, King Abdulaziz University, Jeddah 21589, Saudi Arabia
6
Center of Innovation in Personalized Medicine (CIPM), 3D Bioprinting Unit, King Abdulaziz University, Jeddah 21589, Saudi Arabia
7
Department of Pharmacology, College of Medicine, University of Jeddah, Jeddah 23890, Saudi Arabia
8
Department of Medical Laboratory Sciences, Faculty of Applied Medical Sciences, King Abdulaziz University, Jeddah 22254, Saudi Arabia
9
Hematology Research Unit, King Fahd Medical Research Center, King Abdulaziz University, Jeddah 22254, Saudi Arabia
10
Department of Medical Laboratory Sciences, College of Applied Medical Sciences, Prince Sattam bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia
11
Department of Biology, College of Science, University of Jeddah, Jeddah 21589, Saudi Arabia
12
Department of Zoology, Government College University Faisalabad, Faisalabad 38000, Pakistan
13
Department of Chemistry, Government College University Faisalabad, Faisalabad 38000, Pakistan
*
Author to whom correspondence should be addressed.
Pharmaceutics 2023, 15(2), 399; https://doi.org/10.3390/pharmaceutics15020399
Received: 5 December 2022 / Revised: 11 January 2023 / Accepted: 12 January 2023 / Published: 24 January 2023
(This article belongs to the Special Issue Silica-Based Carriers for Drug Delivery)

Abstract

The current study was designed to formulate ternary solid dispersions (TSDs) of dexibuprofen (Dex) by solvent evaporation to augment the solubility and dissolution profile, in turn providing gastric protection and effective anti-inflammatory activity. Initially, nine formulations (S1 to S9) of binary solid dispersions (BSDs) were developed. Formulation S1 comprising a 1:1 weight ratio of Dex and Syloid 244FP® was chosen as the optimum BSD formulation due to its better solubility profile. Afterward, 20 TSD formulations were developed using the optimum BSD. The formulation containing Syloid 244FP® with 40% Gelucire 48/16® (S18) and Poloxamer 188® (S23) successfully enhanced the solubility by 28.23 and 38.02 times, respectively, in pH 6.8, while dissolution was increased by 1.99- and 2.01-fold during the first 5 min as compared to pure drug. The in vivo gastroprotective study in rats suggested that the average gastric lesion index was in the order of pure Dex (8.33 ± 2.02) > S1 (7 ± 1.32) > S18 (2.17 ± 1.61) > S23 (1.83 ± 1.04) > control (0). The in vivo anti-inflammatory study in rats revealed that the percentage inhibition of swelling was in the order of S23 (71.47 ± 2.16) > S18 (64.8 ± 3.79) > S1 (54.14 ± 6.78) > pure drug (18.43 ± 2.21) > control (1.18 ± 0.64) after 6 h. ELISA results further confirmed the anti-inflammatory potential of the developed formulation, where low levels of IL-6 and TNF alpha were reported for animals treated with S23. Therefore, S23 could be considered an effective formulation that not only enhanced the solubility and bioavailability but also reduced the gastric irritation of Dex.
Keywords: dexibuprofen; solid dispersions; Syloid 244FP®, Gelucire 48/16®, and Poloxamer 188® dexibuprofen; solid dispersions; Syloid 244FP®, Gelucire 48/16®, and Poloxamer 188®

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MDPI and ACS Style

Asim, M.; Nazir, M.; Chauhdary, Z.; Irfan, M.; Khalid, S.H.; Asghar, S.; Usra; Felimban, R.I.; Majrashi, M.A.; Hazzazi, M.S.; Allissa, M.; Qahl, S.H.; Hussain, G.; Rasul, A.; Chatha, S.A.S.; Khan, I.U. Enhanced Solubility and Biological Activity of Dexibuprofen-Loaded Silica-Based Ternary Solid Dispersions. Pharmaceutics 2023, 15, 399. https://doi.org/10.3390/pharmaceutics15020399

AMA Style

Asim M, Nazir M, Chauhdary Z, Irfan M, Khalid SH, Asghar S, Usra, Felimban RI, Majrashi MA, Hazzazi MS, Allissa M, Qahl SH, Hussain G, Rasul A, Chatha SAS, Khan IU. Enhanced Solubility and Biological Activity of Dexibuprofen-Loaded Silica-Based Ternary Solid Dispersions. Pharmaceutics. 2023; 15(2):399. https://doi.org/10.3390/pharmaceutics15020399

Chicago/Turabian Style

Asim, Muhammad, Marriam Nazir, Zunera Chauhdary, Muhammad Irfan, Syed Haroon Khalid, Sajid Asghar, Usra, Raed I. Felimban, Mohammed A. Majrashi, Mohannad S. Hazzazi, Mohammed Allissa, Safa H. Qahl, Ghulam Hussain, Azhar Rasul, Shahzad Ali Shahid Chatha, and Ikram Ullah Khan. 2023. "Enhanced Solubility and Biological Activity of Dexibuprofen-Loaded Silica-Based Ternary Solid Dispersions" Pharmaceutics 15, no. 2: 399. https://doi.org/10.3390/pharmaceutics15020399

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