RESUMEN

Skin cancer poses a significant global health concern necessitating innovative treatment approaches. This review explores the potential of vesicle nanoformulation incorporating EA (edge activators) to overcome barriers in skin cancer management. The skin's inherent protective mechanisms, specifically the outermost layer called the stratum corneum and the network of blood arteries, impede the permeation of drugs. Phospholipid-enriched EA based nanoformulation offer a promising solution by enhancing drug penetration through skin barriers. EAs like Span 80, Span 20, Tween 20, and sodium cholate etc., enhance vesicles deformability, influencing drug permeation. This review discusses topical application of drugs treat skin cancer, highlighting challenges connected with the conventional liposome and the significance of using EA-based nanoformulation in overcoming these challenges. Furthermore, it provides insights into various EA characteristics, critical insights, clinical trials, and patents. The review also offers a concise overview of composition, preparation techniques, and the application of EA-based nanoformulation such as transfersomes, transliposomes, transethosomes, and transniosomes for delivering drugs to treat skin cancer. Overall, this review intends to accelerate the development of formulations that incorporate EA, which would further improve topical drug delivery and enhance therapeutic outcomes in skin cancer treatment.

RESUMEN

Background Because of cost effectiveness, most of the laboratories in India estimate low-density lipoprotein cholesterol (LDL-C) levels with the Friedewald's formula. There were many shortcomings of the Friedewald's formula. Recently, Martin and colleagues have derived a new formula for calculating LDL-C. The present study was undertaken to calculate LDL-C using various formulae (Friedewald's formula, Anandaraja's formula, and Martin's formula) and to compare directly measured LDL-C (D-LDL-C) with calculated LDL-C at various ranges of triglyceride (TG) concentration. Materials and Methods The present study compared LDL-C measured by Martin's formula, Friedewald's formula, and Anandaraja's formula with D-LDL-C in 280 outpatient fasting samples between the age groups of 18 and 50 years. Depending on the TG values, study samples were divided into four groups. Group 1: less than 200 mg/dL; Group 2: 200 to 300 mg/dL; Group 3: 300 to 400 mg/dL; and Group 4: more than 400 mg/dL. Results Martin's formula shows highest correlation with r -value of 0.9979 compared with Friedewald's (0.9857) and Anandaraja's (0.9683) r -values. The mean difference was least for Martin's formula (0.31 ± 3.53) compared with other formulae. Among all the groups, percentage of error was least for Martin's formula (0.23%). Martin's LDL-C shows highest concordance (90.90%) compared with Friedewald's (79.60%) and Anandaraja's formulae (82.90%). Conclusion Among all the groups, Martin's formula shows highest correlation, least percentage of error, highest concordance, and least mean differences. At all TG levels, Martin's formula is the best formula compared with the Friedewald's formula and Anandaraja's formula.

RESUMEN

At present, people and patients worldwide are relying on the medicinal plant as a therapeutic agent over pharmaceuticals because the medicinal plant is considered safer, especially for chronic disorders. Several medicinal plants and their components are being researched and explored for their possible therapeutic contribution to CNS disorders. Thymoquinone (TQ) is one such molecule. Thymoquinone, one of the constituents of Plant Nigella Sativa, is effective against several neurodegenerative diseases like, Alzheimer's, Depression, Encephalomyelitis, Epilepsy, Ischemia, Parkinson's, and Traumatic. This review article presents the neuropharmacological potential of TQ's, their challenges, and delivery prospects, explicitly focusing on neurological disorders along with their chemistry, pharmacokinetics, and toxicity. Since TQ has some pharmacokinetic challenges, scientists have focused on novel formulations and delivery systems to enhance bioavailability and ultimately increase its therapeutic value. In the present work, the role of nanotechnology in neurodegenerative disease and how it improves the bioavailability and delivery of a drug to the site of action has been discussed. There are a few limitations to developing novel drug formulations, including solubility, pH, and compatibility of nanomaterials. Since here we are targeting CNS disorders, the bloodbrain barrier (BBB) becomes an additional challenge. Hence, the review summarized the novel aspects of delivery and biocompatible nanoparticles-based approaches for targeted drug delivery into CNS, enhancing TQ bioavailability and its neurotherapeutic effects.

Asunto(s)

RESUMEN

In the current research, a thymoquinone-enriched naringenin (NGN)-loaded nanostructured lipid carrier (NLC) was developed and delivered via the nasal route for depression. Thymoquinone (TQ) oil was used as the liquid lipid and provided synergistic effects. A TQ- and NGN-enriched NLC was developed via the ultrasonication technique and optimized using a central composite rotatable design (CCRD). The optimized NLC exhibited the following properties: droplet size, 84.17 to 86.71 nm; PDI, 0.258 to 0.271; zeta potential, -8.15 to -8.21 mV; and % EE, 87.58 to 88.21%. The in vitro drug release profile showed the supremacy of the TQ-NGN-NLC in comparison to the NGN suspension, with a cumulative drug release of 82.42 ± 1.88% from the NLC and 38.20 ± 0.82% from the drug suspension. Ex vivo permeation study displayed a 2.21-fold increase in nasal permeation of NGN from the NLC compared to the NGN suspension. DPPH study showed the better antioxidant potential of the TQ-NGN-NLC in comparison to NGN alone due to the synergistic effect of NGN and TQ oil. CLSM images revealed deeper permeation of the NGN-NLC (39.9 µm) through the nasal mucosa in comparison to the NGN suspension (20 µm). Pharmacodynamic studies, such as the forced swim test and the locomotor activity test, were assessed in the depressed rat model, which revealed the remarkable antidepressant effect of the TQ-NGN-NLC in comparison to the NGN suspension and the marketed formulation. The results signify the potential of the TQ-enriched NGN-NLC in enhancing brain delivery and the therapeutic effect of NGN for depression treatment.

RESUMEN

This manuscript aims to provide the latest update on polymeric nanoparticle drug delivery system for breast cancer treatment after 2015 and how research-oriented it is based on the available research data. Therefore, the authors have chosen breast cancer which is the most frequent and common reason for mortality in women worldwide. The first-line treatment for breast cancer treatment is chemotherapy, apart from surgery, radiation and hormonal therapy. Chemotherapy is associated with lesser therapeutics and undesirable side effects and hence. In addition, drug resistance affects the therapeutic dose to the target site. Although various nano-based formulations have been developed for effective treatment, the polymeric nanoparticles effectively avoid the lacunae of conventional chemotherapy. There has been an effort made to understand the chemotherapy drugs and their conventional formulation-related problems for better targeting and effective drug delivery for breast cancer treatment. Thus, the polymeric nanoparticles as a strategy overcome the associated problems with resulting dose reduction, enhanced bioavailability, reduced side effects, etc. This present review has compiled the research reports published from 2015 to 2021 from different databases, such as PubMed, Google Scholar, ScienceDirect, which are related to breast cancer treatment in which the drug delivery of numerous chemotherapeutic agents alone or in combination, including phytoconstituents formulated into various polymer-based nanoparticles.

RESUMEN

In the present study, SEL was loaded in a lipid nanocarrier (LNC) formulation with a P-gp pump inhibitor i.e., Quercetin (QUR) for improving the bioavailability of the SEL in the brain via the oral route. SEL-QUR LNC was formulated using modified emulsiosonication method and optimized using central composite rotatable design (CCRD) design. The results showed that optimized SEL-QUR LNC formulation was spherical with globule size, polydispersity index, entrapment efficiency and zeta potential within the range of 92.46-95.34 nm, 0.239-0.248, 88.94-91.26%, and -6.21 to -7.75 mV respectively. A 4-fold and 6-fold increase was observed in the permeation of SEL from SEL-QUR LNC across the gut sac in comparison with SEL-QUR and SEL suspensions respectively. CLSM images showed 2-fold deeper permeation of SEL across intestinal membrane demonstrating excellent in vivo prospect of the formulation. The behavioural studies including forced swimming, muscle coordination, locomotor activity, akinesia, and catalepsy were performed in the haloperidol-induced PD rats that demonstrated increased efficacy of the formulation in contrast to the SEL-QUR and SEL suspensions. These studies concluded that developed LNC formulation loaded SEL with P-gp inhibitor had the potential in improving bioavailability of SEL in the brain via oral route.

Asunto(s)

RESUMEN

α-Diketones are an important class of building blocks employed in many organic synthetic reactions. However, their coordination chemistry has rarely been explored. In light of this, our earlier report on [(acac)2RuII(µ-2,2'-pyridil)RuII(acac)2] (acac = acetylacetonate) showcased the sensitivity of a diketone fragment towards oxidative C-C cleavage. Following the lead, the synthesis of similar but stable diketo fragments containing diruthenium compounds was attempted. Three diruthenium compounds with the bridge 1,2-bis(2-hydroxyphenyl)ethane-1,2-dione (L) were prepared: diastereomeric [(acac)2RuIII(µ-L2-)RuIII(acac)2], 1a(rac)/1b(meso), [(bpy)2RuII(µ-L2-)RuII(bpy)2](ClO4)2, [2](ClO4)2 and [(pap)2RuII(µ-L2-)RuII(pap)2](ClO4)2, [3](ClO4)2 with ancillary ligands of different donating/accepting characteristics. The metal is stabilised in different oxidation states in these complexes: Ru(iii) is preferred in 1a/1b when σ-donating acac is used as the co-ligand whereas electron rich Ru(ii) is preferred in [2](ClO4)2 and [3](ClO4)2 when co-ligands of moderate to strong π-accepting properties are employed. The oxidative chemistry of these systems is of particular interest with respect to the participation of varying bridging-ligands which contain phenoxide groups. On the other hand, the reduction processes primarily resulting from the metal or the ancillary ligands are noteworthy as the normally reducible 1,2-diketo- group remains unreduced. These results have been rationalised and outlined from thorough experimental and theoretical investigations. The results presented here shed light on the stability of metal coordinated α-diketones as a function of their substituents.

RESUMEN

The structure of the eye is very complex in nature which makes it a challenging task for pharmaceutical researchers to deliver the drug at the desired sites via different routes of administration. The development of the nano-based system helped in delivering the drug in the desired concentration. Improvement in penetration property, bioavailability, and residence time has all been achieved by encapsulating drugs into liposomes, dendrimers, solid lipid nanoparticle, nanostructured lipid carrier, nanoemulsion, and nanosuspension. This review puts emphasis on the need for nanomedicine for ocular drug delivery and recent developments in the field of nanomedicine along with recent patents published in the past few years.

Asunto(s)

RESUMEN

Unactivated olefins usually react poorly in conventional alkenylation reactions. Their introduction via C-H activation is limited to aromatic acids. Herein, we disclose a C-H functionalization protocol of aromatic amines with unactivated olefins, which shows exclusive allylic selectivity for the distal ring of the biphenyl system by exploiting a readily available cobalt(II) catalyst. The allylation proceeds smoothly involving a broad set of unbiased olefins and biaryls, giving access to the functionalization of the biphenyl scaffold.

RESUMEN

In the recent years, there has been an emerging research interest in the domain of C-C bond-cleavage reactions. The present contribution deals with the redox-mediated dioxygen activation and C-C bond cleavage in a diruthenium complex [(acac)2 RuII (µ-L1)RuII (acac)2 ], 1 (acac=acetylacetonate) incorporating 2,2'-pyridil (L1) as the bridging ligand. The above process leads to a C-C-cleaved monomeric product [(acac)2 RuIII (pic- )], 2 (pic- =piconilate). Intriguingly, similar diastereomeric complexes [(acac)2 RuII (µ-L2)RuII (acac)2 ], meso (ΔΛ): 3 a and rac (ΔΔ/ΛΛ): 3 b, involving an analogous diimine bridge (L2=N1,N2-diphenyl-1,2-di(pyridin-2-yl)ethane-1,2-diimine), were stable towards such oxidative transformations. Electrochemical and spectroelectrochemical studies, in combination, establish the potential non-innocent feature of the 2,2'-Pyridil (L1) and its derivative (L2) both in oxidation and reduction processes. Additionally, theoretical calculations have been employed to verify the redox states and their behavior. Furthermore, transition state (TS) calculations at the M06L/6-31G*/LANL2DZ level of theory together with detailed kinetic studies outline a putative mechanism for the selective transformation of 1→2 involving the formation of an intermediate bearing peroxide linkage to complex 1.

RESUMEN

Ligands containing the azo group are often used in various metal complexes owing to their facile one-electron reduction, which in effect extends the means of degrading environmentally harmful azo dyes. In order to probe the idea of the generally accepted ease of reduction of azo-containing compounds, we present here three different diruthenium complexes [(acac)2RuIII(µ-L2-)RuIII(acac)2] (diastereomeric 1/2), [(bpy)2RuII(µ-L2-)RuII(bpy)2](ClO4)2 ([3](ClO4)2), and [(pap)2RuII(µ-L2-)RuII(pap)2](ClO4)2 ([4](ClO4)2 ) with a bridging ligand (L2- = 1,8-bis(( E)-phenyldiazenyl)naphthalene-2,7-dioxido) that contains azo groups in addition to phenoxide-type donors. The RuIII-RuIII complexes (1/2) display interesting one-dimensional-chain effects, as revealed by temperature-dependent magnetic studies. The stability of the RuIII oxidation state in 1/2 under ambient conditions correlates well with the σ-donating acetylacetonato (acac) coligands. However, with π-accepting 2,2/-bipyridine (bpy) or phenylazopyridine (pap) the RuII state is preferably stabilized in 32+ or 42+, respectively, but there are interesting differences in their oxidative chemistry. The moderately π accepting bpy allows for the RuII to RuIII oxidation at reasonably low anodic potentials. However, for the strongly π accepting pap, no RuII to RuIII oxidation is observed within the solvent window. Instead, a phenoxide to phenoxyl radical type of oxidation based on the bridging ligand is observed. Surprisingly, the reductive chemistry of all three complexes is dominated by either the ruthenium centers or the coligands (bpy or pap), with no reductions observed on the azo function associated with the central bridging ligand (L2-). All of the above conclusions were drawn from combined structural, electrochemical, magnetic, spectroelectrochemical, and DFT investigations. Our results thus conclusively establish that the ease of reduction of an azo group in a particular compound is critically dependent on its substituents and that the noninnocence of the bridging ligands (L2-) in the dinuclear complexes can be decisively tuned by the appropriate choice of ancillary ligands.

RESUMEN

Addressing remote C-H functionalization is a prominent challenge in the field of homogeneous catalysis. The past two decades have accounted for major developments in this domain, proclaiming efficient selectivity at the meta and para positions. Recognizing such transformations remains significant, owing to their importance in the biological and chemical industries. This focus review aims to summarize the relatively new concept of σ-C-H activation enabled by a ruthenium metal center.