Cinnamaldehyde hydrazone derivatives as potential cathepsin B inhibitors: parallel in-vitro investigation in liver and cerebrospinal fluid.

The emergence of cathepsins as a potential target for anticancer drugs has led to extensive research in the development of their inhibitors. In the present study, we designed, synthesized, and characterized several cinnamaldehyde schiff bases employing diverse hydrazines, as potential cathepsin B inhibitors. The parallel studies on cathepsin B isolated from liver and cerebrospinal fluid unveiled the significance of the synthesized compounds as cathepsin B inhibitors at nanomolar concentrations. The compound, 7 exhibited the highest inhibition of 83.48 % and 82.96 % with an IC50 value of 0.06 nM and 0.09 nM for liver and cerebrospinal fluid respectively. The inhibitory potential of synthesized compounds has been extremely effective in comparison to previous reports. With the help of molecular docking studies using iGEMDOCK software, we found that the active site -CH2SH group is involved in the case of α-N-benzoyl-D, l-arginine-b-naphthylamide (BANA), curcumin 2, 3, 6, and 7. For toxicity prediction, ADMET studies were conducted and the synthesized compounds emerged to be non-toxic. The results obtained from the in vitro studies were supported with in silico studies. The synthesized cinnamaldehyde schiff bases can be considered promising drug candidates in conditions with elevated cathepsin B levels.

Recent advances in cellulose, pectin, carrageenan and alginate-based oral drug delivery systems.

Polymers-based drug delivery systems constitute one of the highly explored thrust areas in the field of the medicinal and pharmaceutical industries. In the past years, the properties of polymers have been modified in context to their solubility, release kinetics, targeted action site, absorption, and therapeutic efficacy. Despite the availability of diverse synthetic polymers for the bioavailability enhancement of drugs, the use of natural polymers is still highly recommended due to their easy availability, accessibility, and non-toxicity. The aim of the review is to provide the available literature of the last five years on oral drug delivery systems based on four natural polymers i.e., cellulose, pectin, carrageenan, and alginate in a concise and tabulated manner. In this review, most of the information is in tabulated form to provide easy accessibility to the reader. The data related to active pharmaceutical ingredients and supported components in different formulations of the mentioned polymers have been made available.