Promising synthesized bis (arylmethylidene) acetone -polymeric PCL emulsified nanoparticles with enhanced antimicrobial/antioxidant efficacy: in-vitro and in-vivo evaluation

Introduction: Recently, bis(arylmethylidene)acetone drugs known as C5-curcumin, were acknowledged for their potent biological effects as a neoteric synthetic alternative to curcumin effectively used to treat many diseases. Methods: In this study, new polymeric emulsified nanoparticles (PENS) carrying biodegradable polycaprolactone (PCL) polymer moieties within their framework were developed as promising carriers for a modern synthesized bis(arylmethylidene)acetone “(1E,4E)-1,5-di(thiophen-2-yl) penta-1,4dien-3-one” (TPO) with improved bioavailability. Such systems were evaluated by studying their; encapsulation efficiency, release behavior, physicochemical evaluations, TEM and SEM measurements and cytotoxicity, besides the in-vitro and in-vivo biological studies screening. Results: The results revealed high encapsulation efficiency ranging between 99.31± 2.15 and 99.55 ± 2.03 %, and a sustained release behavior for up to 24 h with nanosized particle size. TPO emulsified nanoparticles (TPO-ENPs) showed effective antimicrobial activity against Candida albicans and Aspergillus brasiliensis as well as antioxidant efficacy with a higher scavenging activity of 177.6μg TE/ mg against free radicals of 2,2-diphenyl-1-picrylhydrazyl hydrate (DPPH) relatively to the control drug. F1’ and F2’ TPO-ENPs were safe on Vero-cells and proved a significant reduction of hepatocellular alterations and serum ALT levels in control groups. Conclusion: In conclusion, these novel synthesized TPO-ENPs showed pronounced efficacy as antimicrobial/ antioxidant/ anti-inflammatory/ analgesic/ hepatoprotective therapeutic vehicles

Appraisal terpenoids rich Boswellia carterri ethyl acetate extract in binary cyclodextrin oligomer nano complex for improving respiratory distress

Abstract Boswellia carterii (BC) resins plants have a long historical background as a treatment for inflammation, as indicated by information originating from multiple countries. Twenty-seven diterpenoids have been identified in ethyl acetate and total methanol BC, comprising seventeen boscartins of the cembrane-type diterpenoids and ten boscartols of the prenylaromadendrane-type diterpenoids. Moreover, twenty-one known triterpenoids have also been found, encompassing nine tirucallane-type, six ursane-type, four oleanane-type, and two lupane-type. The cembrane-type diterpenoids hold a significant position in pharmaceutical chemistry and related industries due to their captivating biological characteristics and promising pharmacological potentials. Extraction of BC, creation and assessment of nano sponges loaded with either B. carterii plant extract or DEX, are the subjects of our current investigation. With the use of ultrasound-assisted synthesis, nano sponges were produced. The entrapment efficiency (EE%) of medications in nano sponges was examined using spectrophotometry. Nano sponges were characterized using a number of methods. Within nano sponges, the EE% of medicines varied between 98.52 ± 0.07 and 99.64 ± 1.40%. The nano sponges' particle sizes varied from 105.9 ± 15.9 to 166.8 ± 26.3 nm. Drugs released from nano sponges using the Korsmeyer-Peppas concept. In respiratory distressed rats, the effects of BC plant extract, DEX salt and their nano formulations (D1, D5, P1 and P1), were tested. Treatment significantly reduced ICAM-1, LTB4, and ILβ 4 levels and improved histopathologic profiles, when compared to the positive control group. Boswellia extract and its nano sponge formulation P1 showed promising therapeutic effects. The effect of P1 may be due to synergism between both the extract and the formulation. This effect was achieved by blocking both ICAM-1 and LTB4 pathways, therefore counteracting the effects of talc powder