scholarly journals A Comprehensive Review on Cyclodextrin-Based Carriers for Delivery of Chemotherapeutic Cytotoxic Anticancer Drugs

2015 ◽  
Vol 2015 ◽  
pp. 1-15 ◽  
Author(s):  
Bina Gidwani ◽  
Amber Vyas
Keyword(s):  
Anticancer Drugs ◽  
Delivery System ◽  
Antineoplastic Agents ◽  
Aqueous Solubility ◽  
Chemotherapeutic Agents ◽  
Review Article ◽  
Administration Routes ◽  
Cyclodextrin Complexation ◽  
Important Approach ◽  
Biopharmaceutical Properties

Most of the cytotoxic chemotherapeutic agents have poor aqueous solubility. These molecules are associated with poor physicochemical and biopharmaceutical properties, which makes the formulation difficult. An important approach in this regard is the use of combination of cyclodextrin and nanotechnology in delivery system. This paper provides an overview of limitations associated with anticancer drugs, their complexation with cyclodextrins, loading/encapsulating the complexed drugs into carriers, and various approaches used for the delivery. The present review article aims to assess the utility of cyclodextrin-based carriers like liposomes, niosomes, nanoparticles, micelles, millirods, and siRNA for delivery of antineoplastic agents. These systems based on cyclodextrin complexation and nanotechnology will camouflage the undesirable properties of drug and lead to synergistic or additive effect. Cyclodextrin-based nanotechnology seems to provide better therapeutic effect and sustain long life of healthy and recovered cells. Still, considerable study on delivery system and administration routes of cyclodextrin-based carriers is necessary with respect to their pharmacokinetics and toxicology to substantiate their safety and efficiency. In future, it would be possible to resolve the conventional and current issues associated with the development and commercialization of antineoplastic agents.

Self Microemulsifying Nutraceutical and Drug Delivery Systems

2014 ◽  
Vol 7 (3) ◽  
pp. 2520-2528 ◽  
Author(s):  
Vikrant P Wankhade ◽  
Nivedita S Kale ◽  
K.K Tapar
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
Aqueous Solubility ◽  
Oral Formulation ◽  
Water Soluble ◽  
Drug Dissolution ◽  
The Novel ◽  
Peristaltic Movement

Many chemical entities and nutraceuticals are poor water soluble and show high lipophilicity. It’s difficult to formulate them into oral formulation because of its low aqueous solubility which ultimately affects bioavailability. To enhance the bioavailability of such drugs compounds, self microemulsifying drug delivery system is the reliable drug delivery system. In this system the drug is incorporated in the isotropic system and formulated as unit dosage form. Self microemulsifying drug delivery system is the novel emulsified system composed of anhydrous isotropic mixture of oils, surfactant, and co solvent and sometimes co surfactant. Drug is directly dispersed into the entire gastro intestinal tract with continuous peristaltic movement and drug is available in the solution form of microemulsion, absorbed through lymphatic system and bypasses the dissolution step. Hence they increase the patient compliance. The excipients are selected on basis of construction of ternary phase diagram. Self micro-emulsifying drug delivery system is very useful for drug in which drug dissolution is rate limiting step. This review describes the novel approaches and evaluation parameters of the self microemulsifying drug delivery system towards different classic drugs, proteins-peptides, and nutraceuticals in various oral microemulsion compositions and microstructures.

Hybrid Compounds & Oxidative Stress Induced Apoptosis in Cancer Therapy

2020 ◽  
Vol 27 (13) ◽  
pp. 2118-2132 ◽  
Author(s):  
Aysegul Hanikoglu ◽  
Hakan Ozben ◽  
Ferhat Hanikoglu ◽  
Tomris Ozben
Keyword(s):  
Oxidative Stress ◽  
Drug Resistance ◽  
Side Effects ◽  
Cancer Therapy ◽  
Tumor Cells ◽  
Anticancer Drugs ◽  
Chemotherapeutic Agents ◽  
Oxidation Reactions ◽  
Hybrid Compounds ◽  
Induced Apoptosis

: Elevated Reactive Oxygen Species (ROS) generated by the conventional cancer therapies and the endogenous production of ROS have been observed in various types of cancers. In contrast to the harmful effects of oxidative stress in different pathologies other than cancer, ROS can speed anti-tumorigenic signaling and cause apoptosis of tumor cells via oxidative stress as demonstrated in several studies. The primary actions of antioxidants in cells are to provide a redox balance between reduction-oxidation reactions. Antioxidants in tumor cells can scavenge excess ROS, causing resistance to ROS induced apoptosis. Various chemotherapeutic drugs, in their clinical use, have evoked drug resistance and serious side effects. Consequently, drugs having single-targets are not able to provide an effective cancer therapy. Recently, developed hybrid anticancer drugs promise great therapeutic advantages due to their capacity to overcome the limitations encountered with conventional chemotherapeutic agents. Hybrid compounds have advantages in comparison to the single cancer drugs which have usually low solubility, adverse side effects, and drug resistance. This review addresses two important treatments strategies in cancer therapy: oxidative stress induced apoptosis and hybrid anticancer drugs.

A Conceptual Analysis of solid Self-emulsifying drug Delivery System and its Associate Patents for the Treatment of Cancer

2020 ◽  
Vol 14 ◽  
Author(s):  
Neeraj Singh ◽  
Shweta Rai ◽  
Sankha Bhattacharya
Keyword(s):  
Drug Delivery ◽  
Gastrointestinal Tract ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
Review Article ◽  
New Drugs ◽  
Systemic Absorption ◽  
Hydrophobic Drugs ◽  
Drug Bioavailability

Background: About two-third of new drugs reveal low solubility in water due to that; it becomes difficult for formulation scientists to develop oral solid dosage forms with a pharmaceutically acceptable range of therapeutic activity. In such cases, S-SMEEDS are the best carrier used universally for the delivery of hydrophobic drugs. SEDDS were also used, but due to its limitations, S-SMEDDS used widely. These are the isotropic mixtures of oils, co-solvents, and surfactants. S-SMEDDS are physically stable, easy to manufacture, easy to fill in gelatin capsules as well as improves the drug bioavailability by releasing the drug in the emulsion form to the gastrointestinal tract and make smooth absorption of the drug through the intestinal lymphatic pathway. Methods: We took on the various literature search related to our review, including the peer-reviewed research, and provided a conceptual framework to that. Standard tools are used for making the figures of the paper, and various search engines are used for the literature exploration.In this review article the author discussed the importance of S-SMEDDS, selection criteria for excipients, pseudo-ternary diagram, mechanism of action of S-SMEDDS, solidification techniques used for S-SMEDDS, Characterization of SEDDS and S-SMEDDS including Stability Evaluation of both and future prospect concluded through recent findings on S-SMEDDS on Cancer as well as a neoteric patent on S-SMEDDS Results: Many research papers discussed in this review article, from which it was found that the ternary phase diagram is the most crucial part of developing the SMEDDS. From the various research findings, it was found that the excipient selection is the essential step which decides the strong therapeutic effect of the formulation. The significant outcome related to solid-SMEDDS is less the globule size, higher would be the bioavailability. The adsorption of a solid carrier method is the most widely used method for the preparation of solid-SMEDDS. After review of many patents, it is observed that the solid-SMEDDS have a strong potential for targeting and treatment of a different type of Cancer due to their property to enhance permeation and increased bioavailability. Conclusion: S-SMEEDS are more acceptable pharmaceutically as compare to SEDDS due to various advantages over SEDDS viz stability issue is prevalent with SEDDS. A number of researchers had formulated S-SMEDDS of poorly soluble drugs and founded S-SMEDDS as prospective for the delivery of hydrophobic drugs for the treatment of Cancer. S-SMEEDS are grabbing attention, and the patentability on S-SMEDDS is unavoidable, these prove that S-SMEEDS are widely accepted carriers. These are used universally for the delivery of the hydrophilic drugs and anticancer drugs as it releases the drug to the gastrointestinal tract and enhances the systemic absorption. Abstract: Majority of active pharmaceutical ingredients (API) shows poor aqueous solubility, due to that drug delivery of the API to the systemic circulation becomes difficult as it has low bioavailability. The bioavailability of the hydrophobic drugs can be improved by the Self-emulsifying drug delivery system (SEDDS) but due to its various limitations, solid self-micro emulsifying drug delivery systems (S-SMEDDS) are used due to its advantages over SEDDS. S-SMEDDS plays a vital role in improving the low bioavailability of poorly aqueous soluble drugs. Hydrophobic drugs can be easily loaded in these systems and release the drug to the gastrointestinal tract in the form of fine emulsion results to In-situ solubilisation of the drug. In this review article the author's gives an overview of the solid SMEDSS along with the solidification techniques and an update on recent research and patents filled for Solid SMEDDS.

Icebreaker-inspired Janus nanomotors to combat barriers in the delivery of chemotherapeutic agents

Nanoscale ◽  
2021 ◽  
Author(s):  
Zhanlin Zhang ◽  
Dandan Zhang ◽  
Bo Qiu ◽  
Wenxiong Cao ◽  
Yuan Liu ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Cancer Chemotherapy ◽  
Antineoplastic Agents ◽  
Blood Circulation ◽  
Chemotherapeutic Agents ◽  
Tumor Infiltration ◽  
Intracellular Release ◽  
Pass Through

Cancer chemotherapy remains challenging to pass through various biological and pathological barriers from blood circulation, tumor infiltration and cellular uptake before intracellular release of antineoplastic agents. Herein, icebreaker-inspired Janus nanomotors...

scholarly journals Synthesis, Characterization and Antiproliferative Evaluation of Pt(II) and Pd(II) Complexes with a Thiazine-Pyridine Derivative Ligand

2021 ◽  
Vol 14 (5) ◽  
pp. 395
Author(s):  
Silvia Gutiérrez-Tarriño ◽  
Javier Espino ◽  
Francisco Luna-Giles ◽  
Ana B. Rodríguez ◽  
José A. Pariente ◽  
...  
Keyword(s):  
Cell Lines ◽  
Anticancer Drugs ◽  
Platinum Complexes ◽  
Chemotherapeutic Agents ◽  
Pyridine Derivative ◽  
Cervix Carcinoma ◽  
Multinuclear Complexes ◽  
Histiocytic Lymphoma ◽  
Ovary Adenocarcinoma

Chemical, pharmacological, and clinical research on anticancer coordination complexes has led to noteworthy anticancer drugs such as cisplatin, carboplatin and oxaliplatin. Although these compounds are effective chemotherapeutic agents in the treatment of different tumors, they are associated with high toxicity and numerous side effects. Several studies have shown that the range of platinum complexes with antitumor activity is not limited to structural analogs of cisplatin. Therefore, the development of convenient anticancer drugs that can be effectively used for the treatment of human tumors has become the main goal of most research groups in this field. In this sense, active platinum complexes without NH groups, transplatinum complexes, multinuclear complexes, cationic complexes, and several classes of palladium(II) complexes have emerged. Herein, the synthesis and characterization of two Pt(II) or Pd(II) complexes with PyTz (2-(2-pyridyl)iminotetrahydro-1,3-thiazine), a thiazine derivative ligand, with the formula [MCl2(PyTz)]·C2H6O (M = Pt(II) or Pd(II)) were reported. The potential anticancer ability of both complexes was evaluated in epithelial cervix carcinoma HeLa, human ovary adenocarcinoma SK-OV-3, human histiocytic lymphoma U-937, and human promyelocytic leukemia HL-60 cell lines. Interestingly, the Pt(II) complex showed great cytotoxic potential against all tumor cell lines tested, whereas the Pd(II) complex displayed slight antitumor actions.

A Review on Formulation and Development of Solid Self-Nano Emulsifying Drug Delivery Systems

2021 ◽  
Vol 14 (4) ◽  
pp. 5519-5228
Author(s):  
Sunitha M Reddy ◽  
Sravani Baskarla
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Drug Loading ◽  
Aqueous Solubility ◽  
Delivery Systems ◽  
Particle Size Reduction

This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.  

scholarly journals Hepato & nephro protective effects of naringenin-loaded tpgs polymeric nanosuspension against cisplatin-induced toxicity

2019 ◽  
Vol 10 (4) ◽  
pp. 2755-2764
Author(s):  
Sumathi Rajamani ◽  
Gobinath Kalyanasundaram ◽  
Tamizharasi Sengodan ◽  
Sivakumar Thangavelu ◽  
Nikhitha K Shanmukhan ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Aqueous Solubility ◽  
Protective Role ◽  
Chemotherapeutic Agents ◽  
Glycol Succinate ◽  
High Pressure Homogenization ◽  
Protective Effects ◽  
Male Wistar Rats ◽  
Nephroprotective Effect

Cisplatin (Cis-Diammineplatinum (II) dichloride/CIS) is one of the most potent chemotherapeutic agents widely used in treatment of various cancers. Naringenin (NAR), a natural flavonoid, protect against CIS-induced injury in rats without hampering CIS beneficial cytotoxic activity. Even though NAR exhibits therapeutic potency, clinical evolution of the molecule is embarrassed because of very less aqueous solubility which corresponds to low availability at the site of the tumor. In our former analysis, nanosuspension of naringenin (NARNS) was developed by the method of high-pressure homogenization. The study had been continued to evaluate the protective role of D-α-Tocopheryl polyethylene glycol succinate (TPGS) coated NARNS, against oxidative stress-induced hepato and nephrotoxicity in male Wistar rats upon CIS treatment. Induction of acute hepato and neprotoxicity was done by intraperitoneal injection (i.p) injection of CIS (7 mg/kg of body weight) and administration of NAR and NARNS. Administration of NARNS virtually suppressed CIS-induced and liver injury evidenced by a reduction of lipid peroxidation level, blood urea nitrogen, serum uric acid, creatinine and elevated enzymatic antioxidant activities of superoxide dismutase, catalase, and glutathione peroxidase in rats liver tissue. Histological studies substantiated the biochemical parameters. The study suggests that NARNS has strong hepato and nephroprotective effect compared to NAR.

scholarly journals DDIS-22. DRUG SCREEN IN PATIENT-DERIVED IDHMUT GLIOMA STEM CELLS IDENTIFIES SEVERAL FDA-APPROVED ANTINEOPLASTIC AGENTS

2019 ◽  
Vol 21 (Supplement_6) ◽  
pp. vi67-vi68
Author(s):  
Philip Dao Trong ◽  
Stefan Pusch ◽  
Andreas Unterberg ◽  
Christel Herold-Mende ◽  
Rolf Warta
Keyword(s):  
Stem Cells ◽  
Antineoplastic Agents ◽  
Chemotherapeutic Agents ◽  
Cell Culture Supernatant ◽  
Drug Screen ◽  
Preclinical Model ◽  
Glioma Stem Cells ◽  
Neurosurgical Department ◽  
Stable Production ◽  
Approved Drugs

Abstract OBJECTIVE The discovery of the Isocitrate Dehydrogenase (IDH) mutation in glioma has led to a paradigm shift on how we see glioma biology. While it is clear, that IDH mutated (IDHmut) and wildtype (IDHwt) tumors have to be viewed as separate entities, the underlying biological differences are still matter of extensive research. Difficulties in cultivating IDHmut glioma stem cells (GSC) have led to a paucity of preclinical models in IDHmut glioma making the discovery of new effective chemotherapeutic agents problematic. We therefore sought to perform a repurposing drug screen in five patient-derived IDHmut GSC lines to discover potential effective antineoplastic agents, already approved by the FDA. METHODS Patient tumor tissue was obtained in our neurosurgical department to isolate and establish IDHmut GSC lines. (D)-2-hydroxyglutarate (2HG) levels were measured in the cell culture supernatant of IDHmut GSCs using an enzymatic diaphorase/resazurin system. The drug library provided by the Developmental Therapeutics Program (DTP) of the National Cancer Institute (NCI) consisting of 146 FDA-approved drugs was used for the screen. Cell viability was assessed with the CellTiterGlo assay (Promega). RESULTS Despite several passages, the IDHmut GSCs showed stable production of 2HG and were therefore suitable for the drug screen. Cells were cultured as neurospheres and subjected to the test compounds for 72h in concentrations ranging from 0.1nM – 1µM. We identified several compounds in two IDHmut GSC lines (NCH551b, NCH1681) that had a half maximal inhibitory concentration (IC50) below 1µM and could confirm its cytotoxic potential in additional three IDHmut GSC lines (NCH612, NCH620, NCH3763). CONCLUSION In this study, we present a feasible preclinical model for a high-throughput drug screen in patient-derived IDHmut GSCs and identified several FDA-approved antineoplastic agents which warrant further investigations.

Enhanced Oral Bioavailability and Improved Biological Activities of a Quercetin/Resveratrol Combination Using a Liquid Self-Microemulsifying Drug Delivery System

Planta Medica ◽  
2020 ◽  
Author(s):  
Patcharawalai Jaisamut ◽  
Subhaphorn Wanna ◽  
Surasak Limsuwan ◽  
Sasitorn Chusri ◽  
Kamonthip Wiwattanawongsa ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Biological Activities ◽  
Area Under The Curve ◽  
Aqueous Solubility ◽  
The Self

AbstractBoth quercetin and resveratrol are promising plant-derived compounds with various well-described biological activities; however, they are categorized as having low aqueous solubility and labile natural compounds. The purpose of the present study was to propose a drug delivery system to enhance the oral bioavailability of combined quercetin and resveratrol. The suitable self-microemulsifying formulation containing quercetin together with resveratrol comprised 100 mg Capryol 90, 700 mg Cremophor EL, 200 mg Labrasol, 20 mg quercetin, and 20 mg resveratrol, which gave a particle size of 16.91 ± 0.08 nm and was stable under both intermediate and accelerated storage conditions for 12 months. The percentages of release for quercetin and resveratrol in the self-microemulsifying formulation were 75.88 ± 1.44 and 86.32 ± 2.32%, respectively, at 30 min. In rats, an in vivo pharmacokinetics study revealed that the area under the curve of the self-microemulsifying formulation containing quercetin and resveratrol increased approximately ninefold for quercetin and threefold for resveratrol compared with the unformulated compounds. Moreover, the self-microemulsifying formulation containing quercetin and resveratrol slightly enhanced the in vitro antioxidant and cytotoxic effects on AGS, Caco-2, and HT-29 cells. These findings demonstrate that the self-microemulsifying formulation containing quercetin and resveratrol could successfully enhance the oral bioavailability of the combination of quercetin and resveratrol without interfering with their biological activities. These results provide valuable information for more in-depth research into the utilization of combined quercetin and resveratrol.

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