scholarly journals Catechins within the Biopolymer Matrix—Design Concepts and Bioactivity Prospects

Antioxidants ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 1180
Author(s):  
Zvezdelina Yaneva ◽  
Donika Ivanova
Keyword(s):  
Oral Absorption ◽  
Biological Activities ◽  
Objective Assessment ◽  
Epidemiological Studies ◽  
Delivery Systems ◽  
Therapeutic Effects ◽  
Design Concepts ◽  
Advantages And Disadvantages ◽  
Clinical Investigations ◽  
Matrix Design

Epidemiological studies and clinical investigations proposed that catechins extracts alone may not provide a sufficient level of bioactivities and promising therapeutic effects to achieve health benefits due to a number of constraints related to poor oral absorption, limited bioavailability, sensitivity to oxidation, etc. Modern scientific studies have reported numerous techniques for the design of micro- and nano-bio-delivery systems as novel and promising strategies to overcome these obstacles and to enhance catechins’ therapeutic activity. The objective assessment of their benefits, however, requires a critical comparative estimation of the advantages and disadvantages of the designed catechins-biocarrier systems, their biological activities and safety administration aspects. In this respect, the present review objectively outlines, compares and assesses the recent advances related to newly developed design concepts of catechins’ encapsulation into various biopolymer carriers and their release behaviour, with a special emphasis on the specific physiological biofunctionalities of the innovative bioflavonoid/biopolymer delivery systems.

The review on the bioavailability, bio-efficacies and novel delivery systems for piperine

2021 ◽  
Author(s):  
Weiyun Zhang ◽  
Qianwang Zheng ◽  
Mingyue Song ◽  
Jie Xiao ◽  
Yong Cao ◽  
...  
Keyword(s):  
Biological Activities ◽  
Delivery Systems ◽  
Therapeutic Effects ◽  
Naturally Occurring ◽  
Pungent Odor ◽  
Novel Delivery Systems

As the major naturally occurring alkaloid in pepper with pungent odor, piperine is known for its beneficial bio-functions and therapeutic effects. In this work, the bioavailability and biological activities of...

scholarly journals Translating Research for the Radiotheranostics of Nanotargeted 188Re-liposome

2021 ◽  
Vol 22 (8) ◽  
pp. 3868
Author(s):  
Chih-Hsien Chang ◽  
Ming-Cheng Chang ◽  
Ya-Jen Chang ◽  
Liang-Cheng Chen ◽  
Te-Wei Lee ◽  
...  
Keyword(s):  
Animal Models ◽  
Nuclear Imaging ◽  
Delivery Systems ◽  
Therapeutic Effects ◽  
Clinical Investigations ◽  
Cancer Field ◽  
Nano Drug Delivery ◽  
Wide Range ◽  
Tumor Killing

Nanoliposomes are one of the leading potential nano drug delivery systems capable of targeting chemotherapeutics to tumor sites because of their passive nano-targeting capability through the enhanced permeability and retention (EPR) effect for cancer patients. Recent advances in nano-delivery systems have inspired the development of a wide range of nanotargeted materials and strategies for applications in preclinical and clinical usage in the cancer field. Nanotargeted 188Re-liposome is a unique internal passive radiotheranostic agent for nuclear imaging and radiotherapeutic applications in various types of cancer. This article reviews and summarizes our multi-institute, multidiscipline, and multi-functional studied results and achievements in the research and development of nanotargeted 188Re-liposome from preclinical cells and animal models to translational clinical investigations, including radionuclide nanoliposome formulation, targeted nuclear imaging, biodistribution, pharmacokinetics, radiation dosimetry, radiation tumor killing effects in animal models, nanotargeted radionuclide and radio/chemo-combination therapeutic effects, and acute toxicity in various tumor animal models. The systemic preclinical and clinical studied results suggest 188Re-liposome is feasible and promising for in vivo passive nanotargeted radionuclide theranostics in future cancer care applications.

Structure-Bioactivity Relationship Study of Xanthene Derivatives: A Brief Review

2020 ◽  
Vol 16 (8) ◽  
pp. 1071-1077
Author(s):  
Aref G. Ghahsare ◽  
Zahra S. Nazifi ◽  
Seyed M.R. Nazifi
Keyword(s):  
Biological Activities ◽  
Cyclic Compound ◽  
Research Field ◽  
Pharmaceutical Chemistry ◽  
Therapeutic Effects ◽  
Main Research ◽  
Research Fields ◽  
Xanthene Derivatives ◽  
Anti Cancer ◽  
Heterocyclic Derivatives

: Over the last decades, several heterocyclic derivatives compounds have been synthesized or extracted from natural resources and have been tested for their pharmaceutical activities. Xanthene is one of these heterocyclic derivatives. These compounds consist of an oxygen-containing central heterocyclic structure with two more cyclic structures fused to the central cyclic compound. It has been shown that xanthane derivatives are bioactive compounds with diverse activities such as anti-bacterial, anti-fungal, anti-cancer, and anti-inflammatory as well as therapeutic effects on diabetes and Alzheimer. The anti-cancer activity of such compounds has been one of the main research fields in pharmaceutical chemistry. Due to this diverse biological activity, xanthene core derivatives are still an attractive research field for both academia and industry. This review addresses the current finding on the biological activities of xanthene derivatives and discussed in detail some aspects of their structure-activity relationship (SAR).

Prospects for Discovering the Secondary Metabolites of Cordyceps Sensu Lato by the Integrated Strategy

2020 ◽  
Vol 17 (2) ◽  
pp. 97-120
Author(s):  
Shabana Bibi ◽  
Yuan-Bing Wang ◽  
De-Xiang Tang ◽  
Mohammad Amjad Kamal ◽  
Hong Yu
Keyword(s):  
Drug Design ◽  
Biological Activities ◽  
Design Methods ◽  
Chinese Herbs ◽  
Active Metabolites ◽  
Computer Aided Drug Design ◽  
Design Concepts ◽  
Conventional Drug ◽  
Computer Aided ◽  
Design Techniques

: Some species of Cordyceps sensu lato are famous Chinese herbs with significant biological activities, often used as edible food and traditional medicine in China. Cordyceps represents the largest entomopathogenic group of fungi, including 40 genera and 1339 species in three families and incertae sedis of Hypocreales. Objective: Most of the Cordyceps-derivatives have been approved clinically for the treatment of various diseases such as diabetes, cancers, inflammation, cardiovascular, renal and neurological disorders and are used worldwide as supplements and herbal drugs, but there is still need for highly efficient Cordyceps-derived drugs for fatal diseases with approval of the U.S. Food and Drug Administration. Methods: Computer-aided drug design concepts could improve the discovery of putative Cordyceps- derived medicine within less time and low budget. The integration of computer-aided drug design methods with experimental validation has contributed to the successful discovery of novel drugs. Results: This review focused on modern taxonomy, active metabolites, and modern drug design techniques that could accelerate conventional drug design and discovery of Cordyceps s. l. Successful application of computer-aided drug design methods in Cordyceps research has been discussed. Conclusion: It has been concluded that computer-aided drug design techniques could influence the multiple target-focused drug design, because each metabolite of Cordyceps has shown significant activities for the various diseases with very few or no side effects.

Development and Evaluation of Sustained Release Lipid Nanocarriers for Curcumin

2020 ◽  
Vol 5 (3) ◽  
pp. 224-235
Author(s):  
Harshal A. Pawar ◽  
Bhagyashree D. Bhangale
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Drug Delivery Systems ◽  
Biological Activities ◽  
Curcuma Longa ◽  
Research Work ◽  
Elimination Rate ◽  
Delivery Systems ◽  
Physicochemical Stability ◽  
Wide Range

Background: Lipid based excipients have increased acceptance nowadays in the development of novel drug delivery systems in order to improve their pharmacokinetic profiles. Drugs encapsulated in lipids have enhanced stability due to the protection they experience in the lipid core of these nano-formulations. Phytosomes are newly discovered drug delivery systems and novel botanical formulation to produce lipophilic molecular complex which imparts stability, increases absorption and bioavailability of phytoconstituent. Curcumin, obtained from turmeric (Curcuma longa), has a wide range of biological activities. The poor solubility and wettability of curcumin are responsible for poor dissolution and this, in turn, results in poor bioavailability. To overcome these limitations, the curcumin-loaded nano phytosomes were developed to improve its physicochemical stability and bioavailability. Objective: The objective of the present research work was to develop nano-phytosomes of curcumin to improve its physicochemical stability and bioavailability. Methods: Curcumin-loaded nano phytosomes were prepared by using phospholipid Phospholipon 90 H using a modified solvent evaporation method. The developed curcumin nano phytosomes were evaluated by particle size analyzer and differential scanning calorimetry (DSC). Results: Results indicated that phytosomes prepared using curcumin and lipid in the ratio of 1:2 show good entrapment efficiency. The obtained curcumin phytosomes were spherical in shape with a size less than 100 nm. The prepared nano phytosomal formulation of curcumin showed promising potential as an antioxidant. Conclusion: The phytosomal complex showed sustained release of curcumin from vesicles. The sustained release of curcumin from phytosome may improve its absorption and lowers the elimination rate with an increase in bioavailability.

An overview of Osmotic Drug Delivery System: An update review

2017 ◽  
Vol 6 (7) ◽  
pp. 5426 ◽  
Author(s):  
Hiren J. Patel ◽  
Vaishnavi P. Parikh
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Life Cycle Management ◽  
Delivery Systems ◽  
Osmotic Pump ◽  
Factors Affecting ◽  
Advantages And Disadvantages ◽  
New Chemical Entities ◽  
History Of ◽  
Novel Drug

The pharmaceutical industry has faced several marked challenges in order to bring new chemical entities (NCEs) into the market over the past few decades. Various novel drug delivery approaches have been used as a part of life cycle management from which Osmotic drug delivery systems look the most promising one. After discussing the history of osmotic pump development, this article looks at the principles, advantages and disadvantages of osmotic drug delivery systems. Then, the basic components of osmotic pump and factors affecting the design of oral osmotic drug delivery systems are discussed in detail. In the later part of the manuscript, various types of osmotic pumps available in the market and evaluation methods for osmotic drug delivery systems are discussed in detail.

scholarly journals Nanoformulations for Delivery of Pentacyclic Triterpenoids in Anticancer Therapies

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1764
Author(s):  
Anna Kaps ◽  
Paweł Gwiazdoń ◽  
Ewa Chodurek
Keyword(s):  
Water Solubility ◽  
Biological Activities ◽  
Premature Mortality ◽  
Delivery Systems ◽  
Pentacyclic Triterpenoids ◽  
Anticancer Properties ◽  
Oncological Patients ◽  
Antitumor Potential ◽  
Ring Structures

The search for safe and effective anticancer therapies is one of the major challenges of the 21st century. The ineffective treatment of cancers, classified as civilization diseases, contributes to a decreased quality of life, health loss, and premature mortality in oncological patients. Many natural phytochemicals have anticancer potential. Pentacyclic triterpenoids, characterized by six- and five-membered ring structures, are one of the largest class of natural metabolites sourced from the plant kingdom. Among the known natural triterpenoids, we can distinguish lupane-, oleanane-, and ursane-types. Pentacyclic triterpenoids are known to have many biological activities, e.g., anti-inflammatory, antibacterial, hepatoprotective, immunomodulatory, antioxidant, and anticancer properties. Unfortunately, they are also characterized by poor water solubility and, hence, low bioavailability. These pharmacological properties may be improved by both introducing some modifications to their native structures and developing novel delivery systems based on the latest nanotechnological achievements. The development of nanocarrier-delivery systems is aimed at increasing the transport capacity of bioactive compounds by enhancing their solubility, bioavailability, stability in vivo and ensuring tumor-targeting while their toxicity and risk of side effects are significantly reduced. Nanocarriers may vary in sizes, constituents, shapes, and surface properties, all of which affect the ultimate efficacy and safety of a given anticancer therapy, as presented in this review. The presented results demonstrate the high antitumor potential of systems for delivery of pentacyclic triterpenoids.

scholarly journals Melatonin in Cancer Treatment: Current Knowledge and Future Opportunities

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2506
Author(s):  
Wamidh H. Talib ◽  
Ahmad Riyad Alsayed ◽  
Alaa Abuawad ◽  
Safa Daoud ◽  
Asma Ismail Mahmod
Keyword(s):  
Clinical Trials ◽  
Current Knowledge ◽  
Biological Activities ◽  
Experimental Studies ◽  
Therapeutic Effects ◽  
Cell Proliferation Inhibition ◽  
Different Types ◽  
Solid Foundation

Melatonin is a pleotropic molecule with numerous biological activities. Epidemiological and experimental studies have documented that melatonin could inhibit different types of cancer in vitro and in vivo. Results showed the involvement of melatonin in different anticancer mechanisms including apoptosis induction, cell proliferation inhibition, reduction in tumor growth and metastases, reduction in the side effects associated with chemotherapy and radiotherapy, decreasing drug resistance in cancer therapy, and augmentation of the therapeutic effects of conventional anticancer therapies. Clinical trials revealed that melatonin is an effective adjuvant drug to all conventional therapies. This review summarized melatonin biosynthesis, availability from natural sources, metabolism, bioavailability, anticancer mechanisms of melatonin, its use in clinical trials, and pharmaceutical formulation. Studies discussed in this review will provide a solid foundation for researchers and physicians to design and develop new therapies to treat and prevent cancer using melatonin.

scholarly journals FLAVONOIDS NUTRACEUTICALS IN PREVENTION AND TREATMENT OF CANCER: A REVIEW

2018 ◽  
Vol 11 (1) ◽  
pp. 42 ◽  
Author(s):  
Robert Lotha ◽  
Arvind Sivasubramanian
Keyword(s):  
Red Wine ◽  
Biological Activities ◽  
Health Benefits ◽  
Epidemiological Studies ◽  
Anticancer Properties ◽  
Prevention And Treatment ◽  
Flavonoid Intake ◽  
Meta Analyses ◽  
Dietary Flavonoids ◽  
Broad Aspect

The objective of the study was to discuss the preventive and treatment of cancer from flavonoids nutraceuticals from our daily dietary source. There has been increasing interest in the research of flavonoids from dietary sources, due to growing evidence of the versatile health benefits of flavonoids through epidemiological studies. Numerous biological activities have been reported. Some clinical trials or meta-analyses have suggested positive associations between flavonoid intake and human health, Several findings have proven that dietary flavonoids to have anticancer properties. Flavonoids due to their nontoxicity in nature and vast, broad aspect of its benefits in biological activities have been intensively studied for their health benefits also added to its abundant availability in our daily diets, for example, green leaves, fruits, red wine, and tea vegetables.

Pharmacokinetic evaluation of an oral tablet form of low-molecular-weight heparin and deoxycholic acid conjugate as a novel oral anticoagulant

2011 ◽  
Vol 105 (06) ◽  
pp. 1060-1071 ◽  
Author(s):  
Jin Woo Park ◽  
Ok Cheol Jeon ◽  
Sang Kyoon Kim ◽  
Taslim Al-Hilal ◽  
Kyung-Min Lim ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Oral Administration ◽  
Low Molecular Weight Heparin ◽  
Deoxycholic Acid ◽  
Oral Absorption ◽  
Metabolic Stability ◽  
Oral Dosage ◽  
Low Molecular Weight ◽  
Therapeutic Effects ◽  
Oral Tablet

SummaryThis study was designed to develop a solid oral dosage form of deoxycholic acid (DOCA)-conjugated low-molecular-weight heparin (LMWH) and to evaluate its oral absorption, distribution, and metabolic stability for the prospect of providing an orally bioavailable LMWH. The LMWH derivative (LHD) was synthesised and then formulated with solubilisers and other pharmaceutical excipients to form a solid tablet. Its absorption and distribution after oral administration were evaluated in mice, rats, and monkeys. The in vitro metabolic stability of LHD was examined by liver microsome assays. More than 80% of LHD was released from the tablet within 60 minutes, guaranteeing rapid tablet disintegration after oral administration. Oral bioavailability of LHD in mice, rats and monkeys were 16.1 ± 3.0, 15.6 ± 6.1, and 15.8 ± 2.5%, respectively. After the oral administration of 131I-tyramine-LHD, most of the absorbed drug remained in the blood circulation and was eliminated mainly through the kidneys. LHD was hardly metabolised by the liver microsomes and showed a stable metabolic pattern similar to that of LMWH. In a rat thrombosis model, 10 mg/kg of orally administered LHD reduced thrombus formation by 60.8%, which was comparable to the antithrombotic effect of the subcutaneously injected LMWH (100 IU/ kg). Solid tablets of LHD exhibited high oral absorption and statistically significant therapeutic effects in preventing venous thromboembolism. Accordingly, LHD tablets are expected to satisfy the unmet medical need for an oral heparin-based anticoagulant as an alternative to injectable heparin and oral warfarin.

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