Quercetin (QCN) is a plant polyphenol with a variety of medicinal effects. Poor water solubility, on the other hand, restricts its therapeutic effectiveness. The purpose of this study was to develop mixed micellar systems using two biocompatible amphiphilic PEO-PPO-PEO triblock copolymers, Pluronic P123 (EO 20 -PO 70 -EO 20 ) and Pluronic F88 (EO 104 -PO 39 -EO 104 ), in order to enhance the aqueous solubility and oral bioavailability of QCN drug. The critical micelle concentrations (CMCs) of mixed P123/F88 micellar solutions were investigated using UV-visible spectroscopy with pyrene as a probe. Mixed P123/F88 micelles have low CMCs, indicating that they have a stable micelle structure even when diluted. The solubility of QCN in aqueous mixed P123/F88 micellar solutions at different temperatures was investigated to better understand drug entrapment. The QCN solubility increased with increasing temperature in the mixed P123/F88 micellar system. The QCN-incorporated mixed P123/F88 micelles were prepared using the thin-film hydration method and were well characterized in terms of size and morphology, compatibility, in vitro release and antioxidant profile. In addition, the cell proliferation activity of the mixed micelles was evaluated in the MCF-7 cell line. The QCN-incorporated mixed P123/F88 micelles had a small particle size (< 25 nm) and a negative zeta potential with a spherical shape. The in vitro release behaviour of QCN from a mixed P123/F88 micellar system was slower and more sustained at physiological conditions. The oxidation resistance of QCN-incorporating mixed P123/F88 micelles was shown to be considerably higher than that of pure QCN. An in vitro cell proliferation study revealed that QCN-incorporated mixed micells were effective in inhibiting tumour cell growth. In conclusion, the QCNincorporated mixed P123/F88 micelle may be a promising approach to increase QCN oral bioavailability, antioxidant activity, and cell viability.

This communication is dedicated to Late Yogesh Chamkure for his forever memories in Dr Rakesh K. Sharma's research laboratory.Poor drug solubility and oral bioavailability is a significant challenge with many effective drug candidates. Pluronic micelles are effective solutions for improved solubility, stability, and delivery of the hydrophobic drug to the right area, at the right time, and in the right amount. Solubilization of three drugs, namely curcumin (CUR), quercetin (QCN), and lamotrigine (LTG), were explored using Pluronics with varying molecular characteristics. All the drugs showed better solubility in Pluronic solutions. The tendency of augmentation in solubility was QCN > CUR > LTG. Results showed better solubilization of drugs in Pluronics which form micelles and have low CMTs. With an objective to enhance the oral bioavailability of drugs, the drug-loaded Pluronic P123 nanomicelles (PLC for CUR, PLQ for QCN, and PLL for LTG) have been prepared and characterized using UV-VIS, DLS, SANS, CPT, and TEM measurements. The drug-loaded P123 nanomicelles having particle sizes range from 18 to 22.5 nm and spherical in shapes. In the in-vitro release study, CUR and QCN showed slow release,while LTG exhibited a faster release profile. The PLC and PLQ assessed their anti-oxidant potential had confirmed the oxidation resistance more significantly than the free drug. Considering the pharma uses of CUR, QCN, and LTG drugs and observing the application of Pluronics in drug delivery systems, the present work facilitates insight into the possible formulations of these drugs.

No abstract

Recently the applications of Poloxamers in drug development is promising as it facilitated the drug molecule for delivering to the correct place, at the correct time and in the correct amount. Poloxamers can form nanomicelles to encapsulate hydrophobic drugs in order to increase solubility, stability and facilitate delivery at target. In this context, the solubilization of anticonvulsant lamotrigine (LMN) drug in a chain of Poloxamers containing different polyethylene oxide and polypropylene oxide noieties were examined. The results showed better solubilization of LMN in Poloxamers contain low CMTs while poor with Poloxamers having high CMTs. Systematic investigation of two mixed Poloxamer nanomicelles (P407:P403 and P407:P105) for LMN bioavailability at body temperature (37 °C) were investigated. The solubility of LMN was enhanced in mixed P407:P403 nanomicelles with the amount of P403 and reduced in mixed P407:P105 nanomicelles with the amount of P105. LMN encapsulated mixed Poloxamer nanomicelles were found spherical in shape with ~25 nm Dh sizes. The In-Vitro release profiles of mixed Poloxamer nanomicelles demonstrated the biphasic model with initial burst release and then slowly release of LMN. Better biocompatibility of LMN in the mixed P407:P403 nanomicelles was confirmed with stability data. The results of this work were proven the mixed P407:P403 nanomicelles as efficient nanocarriers for LMN.

The development of copper nanoparticles (CuNPs) with antimicrobial activities shows high potential for various clinical applications. We herein synthesized Poloxamer(P407)-assisted CuNPs with improved oxidative stability using a simple process that included environment friendly Vitamin C (ascorbic acid) as a reducing agent and nontoxic P407 polymer as a stabilizing agent. To optimize the reducing agent, the effect of the molar ratio of ascorbic acid-to-Cu 2 + salt was investigated through fluorescence measurements. The UV-Visible spectrum presented that the inclusion of P407 improved the efficiency of CuNPs synthesis. In addition, DLS demonstrated that when the concentration of P407 was increased, the particle size of CuNPs was reduced. According to the XRD patterns, all the CuNPs are fcc-structured and crystalline. The FE-SEM and EDX images indicated the cubic morphology and the absence of any oxides of copper. The synthesized CuNPs have different particle sizes, showing strong antimicrobial activities against Gram-negative and Gram-positive bacteria as well as funguses. Our findings suggest that P407-assisted CuNPs could be a new way to fight both human and plant pathogens.