Enhanced therapeutic efficacy of a novel self-micellizing nanoformulation-loading fisetin against acetaminophen-induced liver injury

Aim: To evaluate the feasibility of using dipotassium glycyrrhizinate (DG) as a nanocarrier-loading fisetin (FIT) with strengthened treatment efficacies against liver injury induced by acetaminophen overdose. Methods: DG–FIT was prepared, and its efficacy against liver injury induced by acetaminophen overdose was evaluated. Results: DG–FIT was successfully fabricated with excellent physicochemical properties. DG–FIT could be easily dissolved in water to form a clear micelle solution with high FIT encapsulation efficiency. FIT in DG–FIT exhibited a dramatically improved aqueous solubility. DG–FIT improved intestinal permeation. Regarding in vivo efficacies, DG–FIT exhibited significant effect against acetaminophen overdose by suppressing oxidative stress and proinflammatory cytokines involved. Conclusion: DG–FIT formulation possibly represents a promising method for strengthening the efficacy of FIT against acetaminophen-induced liver injury.

Quantitative 1H Nuclear Magnetic Resonance Method for Assessing the Purity of Dipotassium Glycyrrhizinate

A simple, rapid, accurate, and selective quantitative method based on 1H nuclear magnetic resonance (qNMR) was successfully established and developed for assessing the purity of dipotassium glycyrrhizinate (KG). In this study, using potassium hydrogen phthalate and fumaric acid as internal standard (IS), several important experimental parameters, such as relaxation delay and pulse angle, were explored. Reliability, specificity, linearity, limit of quantification, precision, stability, and accuracy were also validated. Calibration results obtained from qNMR were consistent with those obtained from HPLC coupled with ultraviolet detection. The proposed method, independent of the reference standard substance, is a useful, reliable, and practical protocol for the determination of KG and glycyrrhizin analogs.

Transfersomes: the ultra-deformable carrier system for non-invasive delivery of drug

: Vesicular systems have many advantages like prolong the existence of the drug in the systemic circulation, minimizes the undesirable side-effects, reaches the active moieties to its target sites using the carriers. But the main drawback related to transdermal delivery is to cross stratum corneum which can be overcome by the utilization of novel carrier systems e.g. transfersomes which are ultra-deformable carrier system composed of phospholipid (phosphatidylcholine) and edge activators (surfactants). Edge activators are responsible for the flexibility of the bilayer membranes of transfersomes. Different edge activators utilized for transfersomes include tween, span, bile salts (sodium cholate and sodium deoxycholate) and dipotassium glycyrrhizinate. These activators decrease the interfacial tension therefore increases the deformability of carrier system. Transfersomes can encapsulate both hydrophilic and hydrophobic drugs into a vesicular structure which consists of one or more concentric bilayers. Due to the elastic nature of transfersomes, they can easily cross the natural physiological barriers i.e., skin and deliver the drug to its active site. The main benefit of using transfersomes as a carrier is the delivery of macromolecules through the skin by non-invasive route therefore increasing the patient’s compliance. The transfersomal formulations can be used in the treatment of ocular diseases, alopecia, vulvovaginal candidiasis, osteoporosis, apotic dermatitis, tumor, leishmaniasis. It is also used in the delivery of growth hormones, anaesthesia, insulin, proteins, and herbal drugs. This review also focuses on the patents and clinical studies for various transfersomal products.

Enhanced corneal permeation of coumarin-6 using nanoliposomes containing dipotassium glycyrrhizinate: in vitro mechanism and in vivo permeation evaluation

The fluidity of the liposomal membrane differently affected cellular uptake/internalization and in vivo corneal penetration of the nanoliposomes.