scholarly journals Natural Product-based Hybrids as Potential Candidates for the Treatment of Cancer: Focus on Curcumin and Resveratrol

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4665
Author(s):  
Nicola Micale ◽  
Maria Sofia Molonia ◽  
Andrea Citarella ◽  
Francesco Cimino ◽  
Antonina Saija ◽  
...  

One of the main current strategies for cancer treatment is represented by combination chemotherapy. More recently, this strategy shifted to the “hybrid strategy”, namely the designing of a new molecular entity containing two or more biologically active molecules and having superior features compared with the individual components. Moreover, the term “hybrid” has further extended to innovative drug delivery systems based on biocompatible nanomaterials and able to deliver one or more drugs to specific tissues or cells. At the same time, there is an increased interest in plant-derived polyphenols used as antitumoral drugs. The present review reports the most recent and intriguing research advances in the development of hybrids based on the polyphenols curcumin and resveratrol, which are known to act as multifunctional agents. We focused on two issues that are particularly interesting for the innovative chemical strategy involved in their development. On one hand, the pharmacophoric groups of these compounds have been used for the synthesis of new hybrid molecules. On the other hand, these polyphenols have been introduced into hybrid nanomaterials based on gold nanoparticles, which have many potential applications for both drug delivery and theranostics in chemotherapy.

2021 ◽  
Vol 21 ◽  
Author(s):  
Madhukar Garg ◽  
Anju Goyal ◽  
Sapna Kumari

: Cubosomes are highly stable nanostructured liquid crystalline dosage delivery form derived from amphiphilic lipids and polymer-based stabilizers converting it in a form of effective biocompatible carrier for the drug delivery. The delivery form comprised of bicontinuous lipid bilayers arranged in three dimensional honeycombs like structure provided with two internal aqueous channels for incorporation of number of biologically active ingredients. In contrast liposomes they provide large surface area for incorporation of different types of ingredients. Due to the distinct advantages of biocompatibility and thermodynamic stability, cubosomes have remained the first preference as method of choice in the sustained release, controlled release and targeted release dosage forms as new drug delivery system for the better release of the drugs. As lot of advancement in the new form of dosage form has bring the novel avenues in drug delivery mechanisms so it was matter of worth to compile the latest updates on the various aspects of mentioned therapeutic delivery system including its structure, routes of applications along with the potential applications to encapsulate variety drugs to serve health related benefits.


Author(s):  
Desmond I. J. Morrow ◽  
Martin J. Garland ◽  
Paul A. McCarron ◽  
A. David Woolfson ◽  
Ryan F. Donnelly

2018 ◽  
Author(s):  
Karel Kleisner ◽  
Šimon Pokorný ◽  
Selahattin Adil Saribay

In present research, we took advantage of geometric morphometrics to propose a data-driven method for estimating the individual degree of facial typicality/distinctiveness for cross-cultural (and other cross-group) comparisons. Looking like a stranger in one’s home culture may be somewhat stressful. The same facial appearance, however, might become advantageous within an outgroup population. To address this fit between facial appearance and cultural setting, we propose a simple measure of distinctiveness/typicality based on position of an individual along the axis connecting the facial averages of two populations under comparison. The more distant a face is from its ingroup population mean towards the outgroup mean the more distinct it is (vis-à-vis the ingroup) and the more it resembles the outgroup standards. We compared this new measure with an alternative measure based on distance from outgroup mean. The new measure showed stronger association with rated facial distinctiveness than distance from outgroup mean. Subsequently, we manipulated facial stimuli to reflect different levels of ingroup-outgroup distinctiveness and tested them in one of the target cultures. Perceivers were able to successfully distinguish outgroup from ingroup faces in a two-alternative forced-choice task. There was also some evidence that this task was harder when the two faces were closer along the axis connecting the facial averages from the two cultures. Future directions and potential applications of our proposed approach are discussed.


Author(s):  
Bibhu Prasad Panda ◽  
N.S Dey ◽  
M.E.B. Rao

Over the past few decades, there has been an increased interest for innovative drug delivery systems to improve safety, efficacy and patient compliance, thereby increasing the product patent life cycle. The discovery and development of new chemical entities is not only an expensive but also time consuming affair. Hence the pharmaceutical industries are focusing on the design and development of innovative drug delivery systems for existing drugs. One such delivery system is the fast disintegrating oral film, which has gained popularity among pediatric and geriatric patients. This fast disintegrating film with many potential benefits of a fast disintegrating tablet but devoid of friability and risk of choking is more acceptable to pediatric and geriatric patients. Formulation of fast disintegrating film can be achieved by various techniques, but common methods of preparation include spraying and casting. These film forming techniques use hydrophilic film former in combination with suitable excipients, which allow the film to disintegrate or dissolve quickly in the mouth within a few seconds without the administration of water. In view of the advantages of the fast disintegrating films over the fast disintegrating tablets and other dosage forms, it has the potential for commercial exploitation. The oral film dosage form not only has certain advantages of other fast disintegrating systems but also satisfies the unmet needs of the market. The present review emphasizes on the potential benefits, design and development of robust, stable, and innovative orally fast- disintegrating films and their future scenarios on a global market as a pharmaceutical dosage form.  


2019 ◽  
Vol 26 (14) ◽  
pp. 2502-2513 ◽  
Author(s):  
Md. Iqbal Hassan Khan ◽  
Xingye An ◽  
Lei Dai ◽  
Hailong Li ◽  
Avik Khan ◽  
...  

The development of innovative drug delivery systems, versatile to different drug characteristics with better effectiveness and safety, has always been in high demand. Chitosan, an aminopolysaccharide, derived from natural chitin biomass, has received much attention as one of the emerging pharmaceutical excipients and drug delivery entities. Chitosan and its derivatives can be used for direct compression tablets, as disintegrant for controlled release or for improving dissolution. Chitosan has been reported for use in drug delivery system to produce drugs with enhanced muco-adhesiveness, permeation, absorption and bioavailability. Due to filmogenic and ionic properties of chitosan and its derivative(s), drug release mechanism using microsphere technology in hydrogel formulation is particularly relevant to pharmaceutical product development. This review highlights the suitability and future of chitosan in drug delivery with special attention to drug loading and release from chitosan based hydrogels. Extensive studies on the favorable non-toxicity, biocompatibility, biodegradability, solubility and molecular weight variation have made this polymer an attractive candidate for developing novel drug delivery systems including various advanced therapeutic applications such as gene delivery, DNA based drugs, organ specific drug carrier, cancer drug carrier, etc.


2020 ◽  
Vol 26 (27) ◽  
pp. 3234-3250
Author(s):  
Sushil K. Kashaw ◽  
Prashant Sahu ◽  
Vaibhav Rajoriya ◽  
Pradeep Jana ◽  
Varsha Kashaw ◽  
...  

Potential short interfering RNAs (siRNA) modulating gene expression have emerged as a novel therapeutic arsenal against a wide range of maladies and disorders containing cancer, viral infections, bacterial ailments and metabolic snags at the molecular level. Nanogel, in the current medicinal era, displayed a comprehensive range of significant drug delivery prospects. Biodegradation, swelling and de-swelling tendency, pHsensitive drug release and thermo-sensitivity are some of the renowned associated benefits of nanogel drug delivery system. Global researches have also showed that nanogel system significantly targets and delivers the biomolecules including DNAs, siRNA, protein, peptides and other biologically active molecules. Biomolecules delivery via nanogel system explored a wide range of pharmaceutical, biomedical engineering and agro-medicinal application. The siRNAs and DNAs delivery plays a vivacious role by addressing the hitches allied with chronic and contemporary therapeutic like generic possession and low constancy. They also incite release kinetics approach from slow-release while mingling to rapid release at the targets will be beneficial as interference RNAs delivery carriers. Therefore, in this research, we focused on the latest improvements in the delivery of siRNA loaded nanogels by enhancing the absorption, stability, sensitivity and combating the hindrances in cellular trafficking and release process.


2020 ◽  
Vol 17 ◽  
Author(s):  
Marina Gallarate ◽  
Daniela Chirio ◽  
Giulia Chindamo ◽  
Elena Peira ◽  
Simona Sapino

: Osteomyelitis is a bone marrow infection which generally involves cortical plates and which may occur after bone trauma, orthopedic/maxillofacial surgery or after vascular insufficiency episodes. It mostly affects people from the Third World Countries, elderly and patients affected by systemic diseases e.g. autoimmune disorders, AIDS, osteoporosis and microvascular disease. The highest percentage of osteomyelitis cases (almost 75%) is caused by Staphylococcus spp., and in particular by Staphylococcus aureus (more than 50%). The ideal classification and the diagnosis of osteomyelitis are two important tools which help the physicians to choose the best therapeutic strategies. Currently, common therapies provide an extensive debridement in association with intravenous administration of antibiotics (penicillin or clindamycin, vancomycin and fluoroquinolones among all for resistant microorganisms), to avoid the formation of sequestra. However, conventional therapeutic approach involves several drawbacks like low concentration of antibiotic in the infected site, which can lead to resistance and adverse effects due to the intravenous administration. For these reasons, in the last years several studies have been focused on the development of drug delivery systems such as cement, beads, scaffold and ceramics made of hydroxyapatite (HA), calcium phosphate (CaP) and β-tricalcium phosphate (β-TCP) which demonstrated to be biocompatible, poorly toxic and capable to allow osteointegration and a prolonged drug release. The aim of this review is to provide a focus on current therapies and latest developed drug delivery systems with particular attention on those based on CaP and its derivatives, hoping that this work could allow further direction in the field of osteomyelitis.


2017 ◽  
Vol 14 (6) ◽  
pp. 883-903 ◽  
Author(s):  
Boppudi Hari Babu ◽  
Gandavaram Syam Prasad ◽  
Chamarthi Naga Raju ◽  
Mandava Venkata Basaveswara Rao

Background: Michaelis–Arbuzov reaction has played a key role for the synthesis of dialkyl or diaryl phosphonates by reacting various alkyl or aryl halides with trialkyl or triaryl phosphite. This reaction is very versatile in the formation of P-C bond from the reaction of aliphatic halides with phosphinites or phosphites to yield phosphonates, phosphinates, phosphine oxides. The Arbuzov reaction developed some methodologies, possible mechanistic pathways, selectivity, potential applications and biologically active various phosphonates. Objective: The synthesis of phosphonates via Michaelis–Arbuzov reaction with many new and fascinating methodologies were developed and disclosed in the literature, and these are explored in this review. Conclusion: This review has discussed past developments and vast potential applications of Arbuzov reaction in the synthesis of organophosphonates. As presented in this review, various synthetic methodologies were developed to prepare a large variety of phosphonates. Improvements in the reaction conditions of Lewis-acid mediated Arbuzov rearrangement as well as the development of MW-assisted Arbuzov rearrangement were discussed. Finally, to achieve high selectivities and yields, fine-tuning of reaction conditions including solvent type, temperature, and optimal reaction times to be considered.


2020 ◽  
Vol 16 (3) ◽  
pp. 272-306
Author(s):  
Ioannis Fotopoulos ◽  
Dimitra Hadjipavlou-Litina

Background: Coumarins exhibit a plethora of biological activities, e.g. antiinflammatory and anti-tumor. Molecular hybridization technique has been implemented in the design of novel coumarin hybrids with several bioactive groups in order to obtain molecules with better pharmacological activity and improved pharmacokinetic profile. Objective: Therefore, we tried to gather as many as possible biologically active coumarin hybrids referred in the literature till now, to delineate the structural characteristics in relation to the activities and to have a survey that might help the medicinal chemists to design new coumarin hybrids with drug-likeness and varied bioactivities. Results: The biological activities of the hybrids in most of the cases were found to be different from the biological activities presented by the parent coumarins. The results showed that the hybrid molecules are more potent compared to the standard drugs used in the evaluation experiments. Conclusion: Conjugation of coumarin with varied pharmacophore groups/druglike molecules responsible for different biological activities led to many novel hybrid molecules, with a multitarget behavior and improved pharmacokinetic properties.


Author(s):  
Emily C. Whipple ◽  
Camille A. Favero ◽  
Neal F. Kassell

Abstract Introduction Intra-arterial (lA) delivery of therapeutic agents across the blood-brain barrier (BBB) is an evolving strategy which enables the distribution of high concentration therapeutics through a targeted vascular territory, while potentially limiting systemic toxicity. Studies have demonstrated lA methods to be safe and efficacious for a variety of therapeutics. However, further characterization of the clinical efficacy of lA therapy for the treatment of brain tumors and refinement of its potential applications are necessary. Methods We have reviewed the preclinical and clinical evidence supporting superselective intraarterial cerebral infusion (SSJACI) with BBB disruption for the treatment of brain tumors. In addition, we review ongoing clinical trials expanding the applicability and investigating the efficacy of lA therapy for the treatment of brain tumors. Results Trends in recent studies have embraced the use of SSIACI and less neurotoxic chemotherapies. The majority of trials continue to use mannitol as the preferred method of hyperosmolar BBB disruption. Recent preclinical and preliminary human investigations into the lA delivery of Bevacizumab have demonstrated its safety and efficacy as an anti-tumor agent both alone and in combination with chemotherapy. Conclusion lA drug delivery may significantly affect the way treatment are delivered to patients with brain tumors, and in particular GBM. With refinement and standardization of the techniques of lA drug delivery, improved drug selection and formulations, and the development of methods to minimize treatment-related neurological injury, lA therapy may offer significant benefits for the treatment of brain tumors.


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