Physical Characteristic and In vitro Transdermal Delivery of PCL-b-PEG Micelles Containing Quercetin and Rutin

Abstract

In this study, we prepared polymer micelles containing quercetin and rutin, known as antioxidants, using poly(ε-caprolactone)-b-poly(ethylene glycol), and evaluated in vitro skin permeation of the active materials. Quercetin and rutin loaded micelles were characterized by DSC (differential scanning calorimetry), HPLC (high performance liquid chromatography) and DLS (dynamic light scattering) measurements. The particle size of the polymer micelles increased in a concentration dependent manner (0.5~2.0% PCL-b-PEG). The Zeta potential of quercetin and rutin loaded micelles remained constant. To evaluate the skin penetration of PCL-b-PEG micelles, Franz diffusion cell experiment was performed. The aqueous solutions of quercetin and rutin were used as the control groups. Quercetin and rutin loaded PCL-b-PEG micelles showed more efficient skin permeation than the control groups. Safety assessment (patch test) of quercetin and rutin loaded PCL-b-PEG micelles on skin was performed to test application possibility of the polymer micelles to cosmetics. Any adverse symptoms were not observed.

Fabrication of electrospun antioxidant nanofibers by rutin‐pluronic solid dispersions for enhanced solubility

“…The T m peak of rutin was observed in RU&PF PM and was slightly shifted owing to a simply mixed system. However, the peaks of rutin disappeared in the thermograms of RU@PF SDs because rutin was loaded onto Pluronic and was converted to an amorphous state as a core‐corona micellar system . As shown in Figure (b), not all thermograms of PUL‐based nanofibers displayed melting peaks.…”

Polymeric micelles for cutaneous drug delivery

“…In these studies, micellar carriers have been developed for the treatment of psoriasis (tacrolimus and cyclosporine) [64,65]; and photo-aging (all-trans retinoic acid) [66]; breast cancer (endoxifen) [67]; and skin cancer (oridonin) [68], fungal infections (clotrimazole, econazole nitrate and fluconazole) [21], and acne (benzoyl peroxide) [69], and the skin permeation of drugs from micelles was also examined. The micellar carriers of quercetin and rutin as antioxidant compounds [70], and polymeric micelle loaded sumatriptan for the treatment of pain in migraine [71] have also been optimised, and the efficacy of these formulations have been evaluated with in vitro/in vivo studies. In another study, an anti-inflammatory drug was loaded into a core of polymeric micelles, which resulted in delayed drug release and slow drug permeation due to the core and shell structure.…”

“…The flavonoids rutin and quercetin have been described as cell-protecting agents because of their antioxidant, antinociceptive, and anti-inflammatory actions [82]. Micellar carriers of quercetin and rutin which are antioxidant compounds were prepared and the permeation of these drugs across skin using Franz diffusion cells was examined in vitro [70]. The aqueous solutions of both quercetin and rutin were used as the control groups.…”

Characterization and Release Behavior of Polymersomes of PEG-Poly(fumaric-sebacic acids)-PEG Triblock Copolymer in Aqueous Solution

“…23,31,33 They are, thus, considered as preferred vehicles for delivery of drugs [20][21][22]25,27,34 and other therapeutic agents. [35][36][37] We have previously reported the synthesis of a novel biodegradable triblock copolymer made of PEG and poly (fumaric acid-co-sebacoyl chloride) (PEG-co-P(FA/SC)-co-PEG) and its inertness against insulin, as a model therapeutic protein. 38,39 We hereby report on the formation and further characterization of these polymersomes, namely their shape and size by means of transmission electron microscopy (TEM), and dynamic light scattering as well as their stability at 25 o C (room temperature) and 37 o C (physiological temperature) by UV-vis spectroscopy.…”