7-chloro-4-(phenylselanyl) quinoline incorporation into polymeric nanocapsules improves its pharmacological action: Physicochemical, toxicological, and behavioral studies
Jaini Janke Paltian , Vinicius Costa Prado , Caren Aline Ramson da Fonseca , Roberto Barbosa de Morais , Larissa Marafiga Cordeiro , Aline Franzen da Silva , Diego Alves , Felix Alexandre Antunes Soares , Cristiane Luchese , Letícia Cruz , Ethel Antunes Wilhelm
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引用次数: 0
Abstract
The encapsulation of active substances offers significant advantages for various pharmaceutical applications. In this study, we explored the potential of nanotechnology to enhance the efficacy of the organic selenium compound 7-chloro-4-(phenylselanyl) quinoline (4-PSQ) by encapsulating it within ethylcellulose polymeric nanocapsules. Initially, we developed and characterized the nanocapsule containing 4-PSQ. To evaluate their safety and pharmacological benefits, we conducted a series of studies, including hemolysis assays (in vitro), neurotoxicity assessments using Caenorhabditis elegans, and analyses of hepatic and renal toxicity in Swiss mice. The pharmacological activity of 4-PSQ nanocapsules (4-PSQ NCs) was further investigated in nociception and acute inflammation models in male and female Swiss mice. The physicochemical characteristics of 4-PSQ NC comply with nanometric standards and allow for controlled release in vitro. In toxicity evaluations, 4-PSQ NCs exhibited reduced hemolytic and neurotoxic effects compared to the free compound (4-PSQ Free). Furthermore, oxidative damage markers and plasma biomarkers showed no significant differences between the encapsulated and free forms of 4-PSQ. Treatment with 4-PSQ Free or 4-PSQ NC demonstrated antinociceptive and antiedematogenic effects in the glutamate and hot plate tests; however, 4-PSQ NCs showed significantly greater efficacy. Furthermore, 4-PSQ NC showed a prolonged effect, reducing mechanical hypersensitivity in the inflammatory pain model induced by Complete Freund’s Adjuvant. These findings highlight the potential of 4-PSQ NCs as a novel and promising strategy for developing safer and more effective analgesic and anti-inflammatory therapies.
期刊介绍:
The International Journal of Pharmaceutics is the third most cited journal in the "Pharmacy & Pharmacology" category out of 366 journals, being the true home for pharmaceutical scientists concerned with the physical, chemical and biological properties of devices and delivery systems for drugs, vaccines and biologicals, including their design, manufacture and evaluation. This includes evaluation of the properties of drugs, excipients such as surfactants and polymers and novel materials. The journal has special sections on pharmaceutical nanotechnology and personalized medicines, and publishes research papers, reviews, commentaries and letters to the editor as well as special issues.