Preclinical Evaluation of Rutin-Loaded Microparticles with an Enhanced Analgesic Effect

Abstract

This study aimed to develop and characterize microparticles containing rutin to improve the analgesic activity of the flavonoid. Rutin-loaded microparticles were produced with casein and pectin using the complex coacervation physicochemical method, resulting in an average particle size of 4.903 μm ± 4.421 (mean ± standard deviation), round shape, and irregular surfaces, and rutin crystals can be observed to be adsorbed on the outer surface of microparticles. The encapsulation efficiency was 76.9% as quantified by the antioxidant activity. In vivo, rutin-loaded microparticles showed greater inhibition of carrageenan-induced mechanical hyperalgesia (64%) than nonmicroencapsulated rutin (28%). The X-ray diffraction showed that rutin was dispersed in an amorphous matrix, and its crystallographic structure and crystal size did not exhibit changes. Differential scanning calorimetric studies confirmed that rutin was dispersed in the amorphous matrix within microparticles. The fact that rutin was dispersed in an amorphous matrix in the microparticles seemed to provide enhanced absorption, resulting in an improved analgesic efficacy compared with non-microencapsulated rutin. In conclusion, rutin-loaded microparticles were successfully produced, and they improved analgesic activity compared to non-microencapsulated rutin.

Therapeutic Potential of Flavonoids in Pain and Inflammation: Mechanisms of Action, Pre-Clinical and Clinical Data, and Pharmaceutical Development

“…Indeed, flavonoids can block the expression and activation of many cellular regulatory proteins such as cytokines and transcription factors, resulting in diminished cellular inflammatory responses and pain. In conclusion, in view of the pharmacological activities of flavonoids, it could also be interesting to further develop protective delivery formulations containing flavonoids to treat inflammatory diseases and pain, since promising effects were already observed [69,266].…”

“…Microencapsulation (pectin/casein by complex coacervation) of quercetin ameliorates acetic acid-induced colitis by providing a controlled release of quercetin at the mouse colon and improves the anti-inflammatory and antioxidant effects of quercetin compared to the non-encapsulated drug [69]. Rutin-Loaded Microparticles (pectin/casein by complex coacervation as well) induce the inhibition of carrageenan-induced mechanical hyperalgesia better than nonmicroencapsulated rutin does [266].…”

GPIIb/IIIa Receptor Targeted Rutin Loaded Liposomes for Site-Specific Antithrombotic Effect

“…The XRD analysis of RUT discloses the crystalline nature with well resolved peaks . Moreover, nontargeted and targeted liposomes revealed numerous small diffuse peaks in their XRD diffraction patterns (Figure B).…”

“…The XRD analysis of RUT discloses the crystalline nature with well resolved peaks. 58 Moreover, nontargeted and targeted liposomes revealed numerous small diffuse peaks in their XRD diffraction patterns (Figure 3B). The characteristic XRD peaks of RUT were absent in liposomal formulations, which confirms the amorphous nature of RUT in liposomes that also agrees with the SAED pattern analysis.…”

Study on phytochemical, antioxidant and analgesic activity of ethanolic extract of Curcuma Amada Roxb Rhizome

“…The numerous pharmacologicalactivities of C. amadarhizome may be due to the presence of different bioactive compounds including curcumin, bis-demethoxy curcumin, demethoxy curcumin, phenol, and terpenoids etc. [4] . The essential oil extracted from the rhizome possesses different a number of pharmacological activities [5] .…”