Quantitative analysis of loxoprofen sodium loaded microspheres comprising pectin and its thiolated conjugates: In-vivo evaluation of their sustained release behavior.

Autor:	Anam A; Department of Pharmaceutics, Faculty of Pharmacy, Bahauddin Zakariya University Multan, Pakistan., Abbas G; Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University, Faisalabad, Pakistan., Shah S; Department of Pharmacy Practice, Faculty of Pharmaceutical Sciences, Government College University, Faisalabad, Pakistan., Saadullah M; Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Government College University, Faisalabad, Pakistan., Shahwar D; Department of Pharmaceutics, Faculty of Pharmacy, Bahauddin Zakariya University Multan, Pakistan., Mahmood K; Institute of Chemical Sciences, Bahauddin Zakariya University, Multan, Pakistan., Hanif M; Department of Pharmaceutics, Faculty of Pharmacy, Bahauddin Zakariya University Multan, Pakistan., Ahmad N; School of Chemical and Materials Engineering, National University of Science and Technology, Islamabad, Pakistan., Basheer E; Department of Pharmacognosy, Faculty of Pharmaceutical Sciences, Government College University, Faisalabad, Pakistan., Obaidullah AJ; Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Saudi Arabia., Alotaibi HF; Department of Pharmaceutical Sciences, College of Pharmacy, Princess Nourah Bint Abdul Rahman University, Riyadh, 11671, Saudi Arabia., Alqarni M; Department of Pharmaceutical Chemistry, College of Pharmacy, Taif University, P.O. Box 11099, Taif, 21944, Saudi Arabia., Ameer N; Department of Pharmaceutics, Faculty of Pharmacy, Bahauddin Zakariya University Multan, Pakistan.
Jazyk:	angličtina
Zdroj:	Heliyon [Heliyon] 2024 Aug 13; Vol. 10 (16), pp. e36297. Date of Electronic Publication: 2024 Aug 13 (Print Publication: 2024).
DOI:	10.1016/j.heliyon.2024.e36297
Abstrakt:	Continuous use of oral NSAIDs can damage mucosal membrane, which results in decreased bioavailability and non-compliance with the therapy. But the use of sustained release drug delivery systems might offer a solution. Objective was to synthesize mucoadhesive SR microspheres by using different combinations of pectin (PEC) and its thiolated derivative (T-PEC3100) for improved loxoprofen (LS) permeation. Thiolated pectin (T-PEC) was synthesized by the esterification method using thioglycolic acid. Thiolation was confirmed by thiol group quantification and charring point determination. Further characterization was done by Fourier Transform Infrared spectroscopy (FTIR), and Scanning electron microscopy (SEM). Ex-vivo mucoadhesion study was performed to confirm the improved characteristics. Microspheres (MS) were prepared using different ratios of PEC/T-PEC by solvent evaporation method and their particle size and surface morphology were evaluated. Mucus permeation study was carried out using the trans-well plate method. Sustained release behavior of prepared microspheres was investigated through the edema inhibition method in albino rats. T-PEC3100 was considered the optimum formulation for further evaluation and contained maximum thiol group content. FTIR spectra showed a characteristic peak of -SH and charring point was also changed considerably confirming the successful thiolation of PEC. SEM results showed spherical microspheres in the size range of 2-10 μm. Thiol-rich formulation of MS exhibited more than 80 % release after 12 h and maximum absorbable dose (MAD) was calculated as 400 μg % inhibition of edema in MS treated group was slowly attained initially but the reduction in inflammation was detected even after 24 h as compared to control group. Promising results from In-vivo edema inhibition study suggest the possible use of these thiolated MS in formulating sustained release formulation for arthritis. Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. (© 2024 Published by Elsevier Ltd.)
Databáze:	MEDLINE
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