-
1.
Mechanistic Modeling of Wet Stirred Media Milling for Production of Drug Nanosuspensions.
Bilgili, E, Guner, G
AAPS PharmSciTech. 2020;(1):2
Abstract
Drug nanocrystals have been used for a wide range of drug delivery platforms in the pharmaceutical industry, especially for bioavailability enhancement of poorly water-soluble drugs. Wet stirred media milling (WSMM) is the most widely used process for producing dense, stable suspensions of drug nanoparticles, also referred to as nanosuspensions. Despite a plethora of review papers on the production and applications of drug nanosuspensions, modeling of WSMM has not been thoroughly covered in any review paper before. The aim of this review paper is to briefly expose the pharmaceutical scientists and engineers to various modeling approaches, mostly mechanistic, including computational fluid dynamics (CFD), discrete element method (DEM), population balance modeling (PBM), coupled methods, the stress intensity-number model (SI-SN model), and the microhydrodynamic (MHD) model with a main focus on the MHD model for studying the WSMM process. A total of 71 studies, 30 on drugs and 41 on other materials, were reviewed. Analysis of the pharmaceutics literature reveals that WSMM modeling is largely based on empirical, statistically based modeling approaches, and mechanistic modeling could help pharmaceutical engineers develop a fundamental process understanding. After a review of the salient features and various pros-cons of each modeling approach, recent advances in microhydrodynamic modeling and process insights gained therefrom were highlighted. The SI-SN and MHD models were analyzed and critiqued objectively. Finally, the review points out potential research directions such as more mechanistic and accurate CFD-DEM-PBM simulations and the coupling of the MHD-PBM models with the CFD.
-
2.
Iron based nanotherapeutics for ferroptosis-induced cancer therapy.
Liu, YM, Chen, YH, Jin, YC, Tang, KZ
European review for medical and pharmacological sciences. 2020;(21):11323-11333
Abstract
Traditional anti-cancer treatments are far from satisfactory. There is an urgent to combine new therapeutics with traditional treatments to improve anti-cancer effectiveness. Ferroptosis is a new type of iron dependent non-apoptotic cell death could still offer benefits to patients who failed in apoptosis and necroptosis induction treatment. Iron plays a vital role during ferroptosis induction. While iron is a double-edged sword in cancer treatment, tumor specific distribution of iron is especially important. Nanotechnology is an efficient way to help drugs targeting distribution. We intended to review the latest progress in ferroptosis and iron based nanotherapeutics. First, the relationship between ferroptosis and iron metabolism was reviewed briefly to demonstrate the central role of iron in ferroptosis induction. Second, the latest progress of iron-based nanotechnology was presented and discussed according to the different designs. Finally, the future expectations of iron based nanotherapeutics for ferroptosis were spotlighted.
-
3.
Research advances in preparation and application of chitosan nanofluorescent probes.
Liu, P, Wang, R, Su, W, Qian, C, Li, X, Gao, L, Jiao, T
International journal of biological macromolecules. 2020;:1884-1896
Abstract
Nanofluorescent material is developing rapidly as a new type of material. Nanofluorescent probes have broad application prospects in biological analysis, drug metabolism, and semiconductor optical materials. Chitosan is non-toxic and rich in nature which has good biocompatibility, and it can be combined with fluorescent probes. Therefore, the preparation and application of Nanofluorescent probes using chitosan as a carrier is summarized in this article. Fluorescent probes can be combined with other different materials through different reaction mechanisms, and the prepared composite materials can be widely used in biomaterials, sewage treatment, medicine and other fields.
-
4.
Dendrimers as efficient nanocarriers for the protection and delivery of bioactive phytochemicals.
Yousefi, M, Narmani, A, Jafari, SM
Advances in colloid and interface science. 2020;:102125
Abstract
The genesis of dendrimers can be considered as a revolution in nano-scaled bioactive delivery systems. These structures possess a unique potential in encapsulating/entrapping bioactive ingredients due to their tree-like nature. Therefore, they could swiftly obtain a valuable statue in nutraceutical, pharmaceutical and medical sciences. Phytochemicals, as a large proportion of bioactives, have been studied and used by scholars in several fields of pharmacology, medical, food, and cosmetic for many years. But, the solubility, stability, and bioavailability issues have always been recognized as limiting factors in their application. Therefore, the main aim of this study is representing the use of dendrimers as novel nanocarriers for phytochemical bioactive compounds to deal with these problems. Hence, after a brief review of phytochemical ingredients, the text is commenced with a detailed explanation of dendrimers, including definitions, types, generations, synthesizing methods, and safety issues; then is continued with demonstration of their applications in encapsulation of phytochemical bioactive compounds and their active/passive delivery by dendrimers. Dendrimers provide a vast and appropriate surface to entrap the targeted phytochemical bioactive ingredients. Several parameters can affect the yield of nanoencapsulation by dendrimers, including their generation, type of end groups, surface charge, core structure, pH, and ambient factors. Another important issue of dendrimers is related to their toxicity. Cationic dendrimers, particularly PAMAM can be toxic to body cells through attaching to the cell membranes and disturbing their functions. However, a number of solutions have been suggested to decrease their toxicity.
-
5.
Nanocarriers as versatile delivery systems for effective management of acne.
Patel, R, Prabhu, P
International journal of pharmaceutics. 2020;:119140
Abstract
Acne vulgaris is a chronic inflammatory skin disorder affecting mostly females. It has a negative impact on the social life and psychological well-being of the individual. Its pathogenesis involves an exaggerated secretion of sebum, hyperkeratinisation of hair follicles, colonization of anaerobic microbes in the hair follicles, and inflammation. Conventional therapy for acne utilizes antibacterial and anti-inflammatory drugs. Systemic use of these drugs is associated with undesirable toxicities. Hence, topical delivery of anti-acne drugs is desired. However, topical delivery is hindered by poor aqueous solubility of drug and inadequate penetration across stratum corneum. Nanocarriers are endowed with immense potential to facilitate topical delivery of anti-acne drugs as monotherapy or in combination by a myriad of mechanisms including occlusive nature promoting skin hydration, providing sustained drug release thereby decreasing dosing frequency, follicular targeting, and protecting the labile active from degradation. Further, smart nanocarriers can deliver the anti-acne cargo in response to some stimulus present at the disease site precluding undesirable effects at non target sites. Nanocarriers have also been explored in photothermal and photodynamic therapy of acne for destruction of antibiotic resistant bacteria implicated in acne. This review focuses on the potential of a variety of nanocarriers for treatment of acne.
-
6.
Nanoformulations of Coumarins and the Hybrid Molecules of Coumarins with Potential Anticancer Effects.
Yerer, MB, Dayan, S, Han, MI, Sharma, A, Tuli, HS, Sak, K
Anti-cancer agents in medicinal chemistry. 2020;(15):1797-1816
Abstract
Coumarins are the secondary metabolites of some plants, fungi, and bacteria. Coumarins and the hybrid molecules of coumarins are the compounds which have been widely studied for their potential anticancer effects. They belong to benzopyrone chemical class, more precisely benzo-α-pyrones, where benzene ring is fused to pyrone ring. In nature, coumarins are found in higher plants like Rutaceae and Umbelliferae and some essential oils like cinnamon bark oil, cassia leaf oil and lavender oil are also rich in coumarins. The six main classes of coumarins are furanocoumarins, dihydrofuranocoumarins, pyrano coumarins, pyrone substituted coumarins, phenylcoumarins and bicoumarins. As well as their wide range of biological activities, coumarins and the hybrid molecules of coumarins are proven to have an important role in anticancer drug development due to the fact that many of its derivatives have shown an anticancer activity on various cell lines. Osthol, imperatorin, esculetin, scopoletin, umbelliprenin, angelicine, bergamottin, limettin, metoxhalen, aurapten and isopimpinellin are some of these coumarins. This review summarizes the anticancer effects of coumarins and their hybrid molecules including the novel pharmaceutical formulations adding further information on the topic for the last ten years and basically focusing on the structureactivity relationship of these compounds in cancer.
-
7.
Nanoformulations to Enhance the Bioavailability and Physiological Functions of Polyphenols.
Yang, B, Dong, Y, Wang, F, Zhang, Y
Molecules (Basel, Switzerland). 2020;(20)
Abstract
Polyphenols are micronutrients that are widely present in human daily diets. Numerous studies have demonstrated their potential as antioxidants and anti-inflammatory agents, and for cancer prevention, heart protection and the treatment of neurodegenerative diseases. However, due to their vulnerability to environmental conditions and low bioavailability, their application in the food and medical fields is greatly limited. Nanoformulations, as excellent drug delivery systems, can overcome these limitations and maximize the pharmacological effects of polyphenols. In this review, we summarize the biological activities of polyphenols, together with systems for their delivery, including phospholipid complexes, lipid-based nanoparticles, protein-based nanoparticles, niosomes, polymers, micelles, emulsions and metal nanoparticles. The application of polyphenol nanoparticles in food and medicine is also discussed. Although loading into nanoparticles solves the main limitation to application of polyphenolic compounds, there are some concerns about their toxicological safety after entry into the human body. It is therefore necessary to conduct toxicity studies and residue analysis on the carrier.
-
8.
Anti-amoebic potential of azole scaffolds and nanoparticles against pathogenic Acanthamoeba.
Walvekar, S, Anwar, A, Anwar, A, Sridewi, N, Khalid, M, Yow, YY, Khan, NA
Acta tropica. 2020;:105618
Abstract
Acanthamoeba spp. are free living amoeba (FLA) which are widely distributed in nature. They are opportunistic parasites and can cause severe infections to the eye, skin and central nervous system. The advances in drug discovery and modifications in the chemotherapeutic agents have shown little improvement in morbidity and mortality rates associated with Acanthamoeba infections. The mechanism-based process of drug discovery depends on the molecular drug targets present in the signaling pathways in the genome. Synthetic libraries provide a platform for broad spectrum of activities due to their desired structural modifications. Azoles, originally a class of synthetic anti-fungal drugs, disrupt the fungal cell membrane by inhibiting the biosynthesis of ergosterol through the inhibition of cytochrome P450 dependent 14α-lanosterol, a key step of the sterol pathway. Acanthamoeba and fungi share the presence of similar sterol intermediate, as ergosterol is also the major end-product in the sterol biosynthesis in Acanthamoeba. Sterols present in the eukaryotic cell membrane are one of the most essential lipids and exhibit important structural and signaling functions. Therefore, in this review we highlight the importance of specific targeting of ergosterol present in Acanthamoebic membrane by azole compounds for amoebicidal activity. Previously, azoles have also been repurposed to report antimicrobial, antiparasitic and antibacterial properties. Moreover, by loading the azoles into nanoparticles through advanced techniques in nanotechnology, such as physical encapsulation, adsorption, or chemical conjugation, the pharmacokinetics and therapeutic index of the drugs can be significantly improved. The current review proposes an important strategy to target Acanthamoeba using synthetic libraries of azoles and their conjugated nanoparticles for the first time.
-
9.
Targeting Tumor Immunosuppressive Microenvironment for the Prevention of Hepatic Cancer: Applications of Traditional Chinese Medicines in Targeted Delivery.
Zhang, LY, Zhang, JG, Yang, X, Cai, MH, Zhang, CW, Hu, ZM
Current topics in medicinal chemistry. 2020;(30):2789-2800
Abstract
Traditional Chinese Medicine (TCM) is one of the ancient and most accepted alternative medicinal systems in the world for the treatment of health ailments. World Health Organization recognizes TCM as one of the primary healthcare practices followed across the globe. TCM utilizes a holistic approach for the diagnosis and treatment of cancers. The tumor microenvironment (TME) surrounds cancer cells and plays pivotal roles in tumor development, growth, progression, and therapy resistance. TME is a hypoxic and acidic environment that includes immune cells, pericytes, fibroblasts, endothelial cells, various cytokines, growth factors, and extracellular matrix components. Targeting TME using targeted drug delivery and nanoparticles is an attractive strategy for the treatment of solid tumors and recently has received significant research attention under precise medicine concept. TME plays a pivotal role in the overall survival and metastasis of a tumor by stimulating cell proliferation, preventing the tumor clearance by the immune cells, enhancing the oncogenic potential of the cancer cells, and promoting tumor invasion. Hepatocellular Carcinoma (HCC) is one of the major causes of cancer-associated deaths affecting millions of individuals worldwide each year. TCM herbs contain several bioactive phytoconstituents with a broad range of biological, physiological, and immunological effects on the system. Several TCM herbs and their monomers have shown inhibitory effects in HCC by controlling the TME. This study reviews the fundamentals and applications of targeting strategies for immunosuppressing TME to treat cancers. This study focuses on TME targeting strategies using TCM herbs and the molecular mechanisms of several TCM herbs and their monomers on controlling TME.
-
10.
Trace element nanoparticles improved diabetes mellitus; a brief report.
Ashrafizadeh, H, Abtahi, SR, Oroojan, AA
Diabetes & metabolic syndrome. 2020;(4):443-445
Abstract
BACKGROUND Diabetes mellitus is a chronic metabolic disease that induces several complications in various organs such as the liver, kidney, and reproductive system. Trace elements such as copper, zinc, selenium, and magnesium play an essential role in the management or treatment of diabetes mellitus. AIM: the aim of the present study was conducted to investigate the effect of these trace elements nanoparticles and their probable mechanism of action on diabetes and its complications. METHODS The present brief report was conducted with a search of articles published in several databases including PubMed, ScienceDirect, Google Scholar, and Scopus. The articles were selected from 2011 to 2018 using the keywords "zinc," "copper," "selenium," "magnesium," and "diabetes." Following the eligibility criteria were selected 16 articles and 1 book. RESULTS The scientific results of the presented brief report show that zinc, copper, selenium, and magnesium have antidiabetic effects. Also, they improved the diabetes-induced complications through increase antioxidant enzyme level, glucose utilization, and insulin sensitivity. CONCLUSION While zinc, copper, selenium, and magnesium revealed antidiabetic effects, but their nanoparticles were more potent for the treatment of this disease.