scholarly journals Lipid Nanocarriers for Anti-HIV Therapeutics: A Focus on Physicochemical Properties and Biotechnological Advances

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1294
Author(s):  
Maria J. Faria ◽  
Carla M. Lopes ◽  
José das Neves ◽  
Marlene Lúcio
Keyword(s):  
Physicochemical Properties ◽  
Treatment Options ◽  
Survival Rates ◽  
Aqueous Solubility ◽  
Hiv Infections ◽  
Viral Reservoirs ◽  
Major Step ◽  
Therapeutic Outcomes ◽  
Short Period ◽  
Lipid Nanocarriers

Since HIV was first identified, and in a relatively short period of time, AIDS has become one of the most devastating infectious diseases of the 21st century. Classical antiretroviral therapies were a major step forward in disease treatment options, significantly improving the survival rates of HIV-infected individuals. Even though these therapies have greatly improved HIV clinical outcomes, antiretrovirals (ARV) feature biopharmaceutic and pharmacokinetic problems such as poor aqueous solubility, short half-life, and poor penetration into HIV reservoir sites, which contribute to the suboptimal efficacy of these regimens. To overcome some of these issues, novel nanotechnology-based strategies for ARV delivery towards HIV viral reservoirs have been proposed. The current review is focused on the benefits of using lipid-based nanocarriers for tuning the physicochemical properties of ARV to overcome biological barriers upon administration. Furthermore, a correlation between these properties and the potential therapeutic outcomes has been established. Biotechnological advancements using lipid nanocarriers for RNA interference (RNAi) delivery for the treatment of HIV infections were also discussed.

scholarly journals Lipid Nanocarriers for Anti-HIV Therapeutics: a Focus on Physicochemical Properties and Biotechnological Advances

2021 ◽  
Author(s):  
Maria J. Faria ◽  
Carla M. Lopes ◽  
José das Neves ◽  
Marlene Lúcio
Keyword(s):  
Physicochemical Properties ◽  
Treatment Options ◽  
Survival Rates ◽  
Aqueous Solubility ◽  
Hiv Infections ◽  
Viral Reservoirs ◽  
Major Step ◽  
Therapeutic Outcomes ◽  
Short Period ◽  
Lipid Nanocarriers

Since HIV was first identified, and in a relatively short period of time, AIDS has become one of the most devastating infectious diseases of the 21st century. Classical antiretroviral therapies were a major step forward in disease treatment options, significantly improving the survival rates of HIV-infected individuals. Even though these therapies have greatly improved HIV clinical outcomes, antiretrovirals (ARV) feature biopharmaceutic and pharmacokinetic problems such as poor aqueous solubility, short half-life and poor penetration into HIV reservoir sites, which contribute to the sub-optimal efficacy of these regimens. To overcome some of these issues, novel nanotechnology-based strategies for ARV delivery towards HIV viral reservoirs have been proposed. The current review focus on the benefits of using lipid-based nanocarriers for tuning the physicochemical properties of ARVs to overcome biological barriers upon administration. Furthermore, a correlation of these properties and the potential therapeutic outcomes has been established. Biotechnological advancements using lipid nanocarriers for RNA interference delivery for the treatment of HIV infections were also discussed.

scholarly journals Cannabinoid glycosides: In vitro production of a new class of cannabinoids with improved physicochemical properties

2017 ◽  
Author(s):  
Janee’ M. Hardman ◽  
Robert T. Brooke ◽  
Brandon J. Zipp
Keyword(s):  
Physicochemical Properties ◽  
Targeted Delivery ◽  
Treatment Options ◽  
Stevia Rebaudiana ◽  
Aqueous Solubility ◽  
In Vitro Production ◽  
New Class ◽  
Delivery Options ◽  
Arachidonoyl Glycerol

AbstractThe cannabinoid signaling system has recently garnered attention as a therapeutic target for numerous indications, and cannabinoids are now being pursued as new treatment options in diverse medical fields such as neurology, gastroenterology, pain management, and oncology. Cannabinoids are extremely hydrophobic and relatively unstable compounds, and as a result, formulation and delivery options are severely limited. Enzymatic glycosylation is a strategy to alter the physicochemical properties of small molecules, often improving their stability and aqueous solubility, as well as enabling site-specific drug targeting strategies. To determine if cannabinoids are a candidate for glycosylation, a library of glucosyltransferase (UGT) enzymes was screened for glycosylation activity towards various cannabinoids. The UGT76G1 enzyme from Stevia rebaudiana has been identified as having glucosyltransferase activity towards a broad range of cannabinoids. Compounds that were successfully glycosylated by UGT76G1 include the phytocannabinoids cannabidiol (CBD), Δ9-tetrahydrocannabinol (Δ9-THC), cannabidivarin (CBDV), and cannabinol (CBN), and the human endocannabinoids anandamide (AEA), 2-arachidonoyl-glycerol (2AG), 1-arachidonoyl-glycerol (1AG), and synaptamide (DHEA). Interestingly, UGT76G1 is able to transfer primary, secondary, and tertiary glycosylations at each acceptor of most of the cannabinoids tested. Additionally, Os03g0702000p, a glycosyltransferase from Oryza sativa, was able to transfer secondary glucose residues onto cannabinoid monoglycosides previously established by UGT76G1. This new class of cannabinoid-glycosides has been termed cannabosides. The compounds have greatly improved solubility in aqueous solutions. This increased aqueous solubility may enable new oral pharmaceutical delivery options for cannabinoids, as well as targeted delivery and release of cannabinoids within the intestines through glycoside prodrug metabolism.

Új lehetőségek a refrakter és relabált Hodgkin-lymphomás betegek kezelésében

2015 ◽  
Vol 156 (45) ◽  
pp. 1824-1833 ◽  
Author(s):  
Árpád Illés ◽  
Ádám Jóna ◽  
Zsófia Simon ◽  
Miklós Udvardy ◽  
Zsófia Miltényi
Keyword(s):  
Stem Cell ◽  
Hodgkin Lymphoma ◽  
Treatment Options ◽  
Survival Rates ◽  
Relapse Free Survival ◽  
Term Survival ◽  
Free Survival ◽  
Novel Treatment ◽  
Refractory Hodgkin Lymphoma

Introduction: Hodgkin lymphoma is a curable lymphoma with an 80–90% long-term survival, however, 30% of the patients develop relapse. Only half of relapsed patients can be cured with autologous stem cell transplantation. Aim: The aim of the authors was to analyze survival rates and incidence of relapses among Hodgkin lymphoma patients who were treated between January 1, 1980 and December 31, 2014. Novel therapeutic options are also summarized. Method: Retrospective analysis of data was performed. Results: A total of 715 patients were treated (382 men and 333 women; median age at the time of diagnosis was 38 years). During the studied period the frequency of relapsed patients was reduced from 24.87% to 8.04%. The numbers of autologous stem cell transplantations was increased among refracter/relapsed patients, and 75% of the patients underwent transplantation since 2000. The 5-year overall survival improved significantly (between 1980 and 1989 64.4%, between 1990 and 1999 82.4%, between 2000 and 2009 88.4%, and between 2010 and 2014 87.1%). Relapse-free survival did not change significantly. Conclusions: During the study period treatment outcomes improved. For relapsed/refractory Hodgkin lymphoma patients novel treatment options may offer better chance for cure. Orv. Hetil., 2015, 156(45), 1824–1833.

Surface Modified Nanoparticulate Carriers for the Targeted Treatment of Breast Cancer

2015 ◽  
Vol 8 (1) ◽  
pp. 2698-2714
Author(s):  
Neeraj Mishra ◽  
Tejinder Singh ◽  
Nidhi ◽  
Supandeep Singh Hallan ◽  
Veerpal Kaur
Keyword(s):  
Breast Cancer ◽  
Tumor Targeting ◽  
Lipid Nanoparticles ◽  
Targeted Treatment ◽  
Therapeutic Effects ◽  
Target Drug Delivery ◽  
Target Drug ◽  
Therapeutic Outcomes ◽  
Lipid Nanocarriers ◽  
Surface Modified

Breast cancer left overs one of the greatest common metastasis disease in females. Advanced diagnostic devices and better understanding of tumour biology can extend the better therapeutic outcomes. Nanotechnology is a tool that helps in cancer diagnosis and treatment therapy. Many nanocarriers such as solid lipid nanoparticles, magnetic nanoparticles, nanocrystals, nanogels, nano-lipid nanocarriers, biodegradable nanoparticles, liposomes, and dendrimers are introduced to improve the therapeutic efficacy of antineoplastic agents. Surface modified target drug delivery system has the potential to increase the therapeutic effects and also reduce the cytotoxicity of breast cancer. Different approaches have been explored for treatment of breast cancer. This review describes the recent advances in the development of nanocarriers used for the targeted treatment of breast cancer. It also focuses on etiology, risk factor and conventional therapy of breast cancer. KEYWORDS: Breast Cancer; Nano-carriers; Tumor Targeting; Ligands; Receptor.

Nano Drug Delivery in Treatment of Oral Cancer, A Review of the Literature

2019 ◽  
Vol 20 (10) ◽  
pp. 1008-1017 ◽  
Author(s):  
Vandita Kakkar ◽  
Manoj Kumar Verma ◽  
Komal Saini ◽  
Indu Pal Kaur
Keyword(s):  
Drug Delivery ◽  
Oral Cancer ◽  
Treatment Options ◽  
Oral Submucous Fibrosis ◽  
Survival Rates ◽  
Cancer Therapeutics ◽  
Developed Countries ◽  
Current Treatment ◽  
Poor Overall Survival ◽  
Hereditary Disorders

Oral Cancer (OC) is a serious and growing problem which constitutes a huge burden on people in more and less economically developed countries alike. The scenario is clearly depicted from the increase in the expected number of new cases in the US diagnosed with OC from 49,670 people in 2016, to 49,750 cases in 2017. The situation is even more alarming in India, with 75,000 to 80,000 new cases being reported every year, thus making it the OC capital of the world. Leukoplakia, erythroplakia, oral lichen planus, oral submucous fibrosis, discoid lupus erythmatosus, hereditary disorders such as dyskeratosis congenital and epidermolisys bullosa are highlighted by WHO expert working group as the predisposing factors increasing the risk of OC. Consumption of tobacco and alcohol, genetic factors, and human papilloma virus are assigned as the factors contributing to the aetiology of OC. On the other hand, pathogenesis of OC involves not only apoptosis but also pain, inflammation and oxidative stress. Inspite of current treatment options (surgery, radiotherapy, and chemotherapy), OC is often associated with recurrence and formation of secondary primary tumours resulting in poor overall survival rates (∼50%). The intervention of nano technology-based drug delivery systems as therapeutics for cancers is often viewed as a cutting edge for technologists. Though ample literature on the usefulness of nano-coutured cancer therapeutics, rarely any product is in pipeline. Yet, despite all the hype about nanotechnology, there are few ongoing trials. This review discusses the current and future trends of nano-based drug delivery for the treatment of OC.

Current Progresses of Functional Nanomaterials for Imaging Diagnosis and Treatment of Melanoma

2019 ◽  
Vol 19 (27) ◽  
pp. 2494-2506 ◽  
Author(s):  
Congcong Zhu ◽  
Yunjie Zhu ◽  
Huijun Pan ◽  
Zhongjian Chen ◽  
Quangang Zhu
Keyword(s):  
Treatment Options ◽  
Skin Tumor ◽  
Diagnosis And Treatment ◽  
Chemotherapeutic Drugs ◽  
Imaging Diagnosis ◽  
Functional Nanomaterials ◽  
Disease Prognosis ◽  
Unsuccessful Treatment ◽  
Short Period ◽  
Malignant Skin

Melanoma is a malignant skin tumor that results in poor disease prognosis due to unsuccessful treatment options. During the early stages of tumor progression, surgery is the primary approach that assures a good outcome. However, in the presence of metastasis, melanoma hasbecome almost immedicable, since the tumors can not be removed and the disease recurs easily in a short period of time. However, in recent years, the combination of nanomedicine and chemotherapeutic drugs has offered promising solutions to the treatment of late-stage melanoma. Extensive studies have demonstrated that nanomaterials and their advanced applications can improve the efficacy of traditional chemotherapeutic drugs in order to overcome the disadvantages, such as drug resistance, low drug delivery rate and reduced targeting to the tumor tissue. In the present review, we summarized the latest progress in imaging diagnosis and treatment of melanoma using functional nanomaterials, including polymers, liposomes, metal nanoparticles, magnetic nanoparticles and carbon-based nanoparticles. These nanoparticles are reported widely in melanoma chemotherapy, gene therapy, immunotherapy, photodynamic therapy, and hyperthermia.

scholarly journals Propolis Extract and Chitosan Improve Health of Nosema ceranae Infected Giant Honey Bees, Apis dorsata Fabricius, 1793

Pathogens ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 785
Author(s):  
Sanchai Naree ◽  
Rujira Ponkit ◽  
Evada Chotiaroonrat ◽  
Christopher L. Mayack ◽  
Guntima Suwannapong
Keyword(s):  
Honey Bees ◽  
Treatment Options ◽  
Survival Rates ◽  
Nosema Ceranae ◽  
Apis Dorsata ◽  
Propolis Extract ◽  
Bee Health ◽  
Honey Bee Health ◽  
Underlying Mechanisms ◽  
Honey Solution

Nosema ceranae is a large contributing factor to the most recent decline in honey bee health worldwide. Developing new alternative treatments against N. ceranae is particularly pressing because there are few treatment options available and therefore the risk of increased antibiotic resistance is quite high. Recently, natural products have demonstrated to be a promising avenue for finding new effective treatments against N. ceranae. We evaluated the effects of propolis extract of stingless bee, Tetrigona apicalis and chito-oligosaccharide (COS) on giant honey bees, Apis dorsata, experimentally infected with N. ceranae to determine if these treatments could improve the health of the infected individuals. Newly emerged Nosema-free bees were individually inoculated with 106N. ceranae spores per bee. We fed infected and control bees the following treatments consisting of 0%, 50%, propolis extracts, 0 ppm and 0.5 ppm COS in honey solution (w/v). Propolis extracts and COS caused a significant increase in trehalose levels in hemolymph, protein contents, survival rates and acini diameters of the hypopharyngeal glands in infected bees. Our results suggest that propolis and COS could improve the health of infected bees. Further research is needed to determine the underlying mechanisms responsible for the improved health of the infected bees.

scholarly journals Hitting the Bull’s-Eye: Mesothelin’s Role as a Biomarker and Therapeutic Target for Malignant Pleural Mesothelioma

Cancers ◽  
2021 ◽  
Vol 13 (16) ◽  
pp. 3932
Author(s):  
Dannel Yeo ◽  
Laura Castelletti ◽  
Nico van Zandwijk ◽  
John E. J. Rasko
Keyword(s):  
Malignant Pleural Mesothelioma ◽  
Treatment Options ◽  
Survival Rates ◽  
Treatment Strategies ◽  
Pleural Mesothelioma ◽  
Normal Tissues ◽  
Drug Conjugates ◽  
Aggressive Cancer ◽  
Immunotherapy Target ◽  
Bull's Eye

Malignant pleural mesothelioma (MPM) is an aggressive cancer with limited treatment options and poor prognosis. MPM originates from the mesothelial lining of the pleura. Mesothelin (MSLN) is a glycoprotein expressed at low levels in normal tissues and at high levels in MPM. Many other solid cancers overexpress MSLN, and this is associated with worse survival rates. However, this association has not been found in MPM, and the exact biological role of MSLN in MPM requires further exploration. Here, we discuss the current research on the diagnostic and prognostic value of MSLN in MPM patients. Furthermore, MSLN has become an attractive immunotherapy target in MPM, where better treatment strategies are urgently needed. Several MSLN-targeted monoclonal antibodies, antibody–drug conjugates, immunotoxins, cancer vaccines, and cellular therapies have been tested in the clinical setting. The biological rationale underpinning MSLN-targeted immunotherapies and their potential to improve MPM patient outcomes are reviewed.

scholarly journals A Novel In Vitro Approach for Simultaneous Evaluation of CYP3A4 Inhibition and Kinetic Aqueous Solubility

2014 ◽  
Vol 20 (2) ◽  
pp. 254-264 ◽  
Author(s):  
José Pérez ◽  
Caridad Díaz ◽  
Francisco Asensio ◽  
Alexandra Palafox ◽  
Olga Genilloud ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Physicochemical Properties ◽  
Safety Concern ◽  
Aqueous Solubility ◽  
Cyp3a4 Inhibition ◽  
Use Of Resources ◽  
Simultaneous Evaluation ◽  
New Chemical Entities ◽  
Further Development

In the early stages of the drug discovery process, evaluation of the drug metabolism and physicochemical properties of new chemical entities is crucial to prioritize those candidates displaying a better profile for further development. In terms of metabolism, drug–drug interactions mediated through CYP450 inhibition are a significant safety concern, and therefore the effect of new candidate drugs on CYP450 activity should be screened early. In the initial stages of drug discovery, when physicochemical properties such as aqueous solubility have not been optimized yet, there might be a large number of candidate compounds showing artificially low CYP450 inhibition, and consequently potential drug–drug interaction toxicity might be overlooked. In this work, we present a novel in vitro approach for simultaneous evaluation of CYP3A4 inhibition potential and kinetic aqueous solubility (NIVA-CYPI-KS). This new methodology is based on fluorogenic CYP450 activities and turbidimetric measurements for compound solubility, and it provides a significant improvement in the use of resources and a better understanding of CYP450 inhibition data.

scholarly journals Epidemiology of spinal cord and column tumors

2020 ◽  
Vol 7 (Supplement_1) ◽  
pp. i5-i9
Author(s):  
Joshua T Wewel ◽  
John E O’Toole
Keyword(s):  
Spinal Cord ◽  
Treatment Options ◽  
Survival Rates ◽  
Spinal Metastases ◽  
Cord Compression ◽  
Severe Form ◽  
Spinal Instability ◽  
Treatment Cascade ◽  
Tumor Pathology ◽  
Pathologic Fractures

Abstract The spine is a frequent location for metastatic disease. As local control of primary tumor pathology continues to improve, survival rates improve and, by extension, the opportunity for metastasis increases. Breast, lung, and prostate cancer are the leading contributors to spinal metastases. Spinal metastases can manifest as bone pain, pathologic fractures, spinal instability, nerve root compression, and, in its most severe form, spinal cord compression. The global extent of disease, the spinal burden, neurologic status, and life expectancy help to categorize patients as to their candidacy for treatment options. Efficient identification and workup of those with spinal metastases will expedite the treatment cascade and improve quality of life.

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