Abstract:
OBJECTIVE:The aim of the current research to formulate a nano delivery system for effective delivery of primaquine for liver targeting to achieve the potential antimalarial activity. An objective of current development is to formulate a lactobionic acid conjugated polyphosphazene based nanodelivery of primaquine for liver targeting to distinguish antimalarial activity. METHOD:The particle size, entrapment efficiency, in-vitro drug release pattern, hepatotoxicity, MTT assay, erythrocyte toxicity assay, histopathology study, HepG2 cell uptake study, antimalarial study, and organ-distribution was also carried out to estimate the activity and potential features of nanoparticle system. RESULTS:The results obtained from the above analysis justify the efficiency and effectiveness of the system. The NMR studies confirm the conjugation pattern and the TEM represent the spherical morphological features of nanoparticles. The controlled release pattern from the in-vitro release study was observed and found to be 73.25% of drug release in 20 hrs and also found in nano-size range (61.6± 1.56 nm) by particle size analysis. SGOT level, SGPT, ALP, Parasitemia level of optimized drug-loaded PEGylated lactobionic acid conjugated polyphosphazene derivatized nanoparticles (FF) was found to lie in safe range showing that the formulation is non-toxic to the liver. Higher cell uptake on HepG2 cell lines of Primaquine drug-loaded PEGylated lactobionic acid conjugated polyphosphazene polymeric nanoparticles showed higher cell uptake on HepG2 cell lines as compared to the drug-loaded in PEGylated polyphosphazene polymeric nanoparticles and plain drug. Percentage cell viability of drug-loaded PEGylated lactobionic acid conjugated polyphosphazene derivatized nanoparticles was decreased with enhancing the concentration of prepared nanoparticle system accessed by MTT assay. CONCLUSION:From the studies, it can be concluded that the optimized formulation of drug-loaded PEGylated lactobionic acid conjugated polyphosphazene derivatized nanoparticles showed high liver targeting, least toxicity to the liver, controlled release of the drug as well as higher antimalarial activity against hepatocytes in low dose and more effectively and can be treated as a potential candidate for antimalarial therapy.
journal_name
Curr Mol Pharmacoljournal_title
Current molecular pharmacologyauthors
Mehan P,Garg A,Ajay K,Mishra Ndoi
10.2174/1874467213999201125220729subject
Has Abstractpub_date
2020-11-25 00:00:00eissn
1874-4672issn
1874-4702pii
CMP-EPUB-111856pub_type
杂志文章abstract::Estrogens are hormones that modulate a diverse array of effects during development and adulthood. The effects of estrogen are mediated by two estrogen receptor (ER) isotypes, ERalpha and ERbeta, which classically function as transcription factors to modulate specific target gene expression and in addition regulate a g...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467210902030215
更新日期:2009-11-01 00:00:00
abstract:BACKGROUND:Valproic acid (VPA) is an HDAC inhibitor (HDACI) with anticancer activity, but it is hepatotoxic. N-(2-hydroxyphenyl)-2-propylpentanamide (o-OH-VPA) is a VPA aryl derivative designed in silico as a selective inhibitor of HDAC8 with biological properties against HeLa, rhabdomyosarcoma and breast cancer cell c...
journal_title:Current molecular pharmacology
pub_type: 杂志文章
doi:10.2174/1874467213666200730113828
更新日期:2020-07-29 00:00:00
abstract::Population growth in the last century has raised important social and economic questions. Thus, current methods of fertility control have been under debate for a long period. Birth rates are essentially dependent on several environmental and social factors but women, who are great users of contraceptives, play a major...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467208666150126155912
更新日期:2014-01-01 00:00:00
abstract::The solute carrier family 1 (SLC1) consists of two neutral amino acid transporters and five high-affinity excitatory amino acid transporters (EAAT1-5). EAATs are expressed in glial cells (EAAT1/GLAST and EAAT2/GLT-1), neurons (EAAT3/EAAC1 and EAAT4), and the retina (EAAT5), where they precisely regulate extracellular ...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/18744672113069990033
更新日期:2013-07-01 00:00:00
abstract::Autism spectrum disorder (ASD) is a neurodevelopmental disease, and the number of patients has increased rapidly in recent years. The causes of ASD involve both genetic and environmental factors, but the details of causation have not yet been fully elucidated. Many reports have investigated genetic factors related to ...
journal_title:Current molecular pharmacology
pub_type: 杂志文章
doi:10.2174/1874467213666200319125109
更新日期:2021-01-01 00:00:00
abstract:INTRODUCTION:Addiction is a compulsive drug-seeking and drug-taking behavior. Reduction of high-risk behaviors can reduce the burden of addiction in society and can improve the overall prognosis of drug addiction. The aim of this study is to show that reduction of oxidative stress with socialization will reduce occurre...
journal_title:Current molecular pharmacology
pub_type: 杂志文章
doi:10.2174/1874467210666170919161045
更新日期:2018-01-01 00:00:00
abstract::Bentham Science has decided to withdraw this article due to the purposeful breach of COPE guidelines and the copyright agreement by the authors as they had submitted this paper simultaneously to another journal. Bentham Science apologizes to the readers of the journal for any inconvenience this may have caused. The Be...
journal_title:Current molecular pharmacology
pub_type: 杂志文章
doi:10.2174/1874467213666201007125021
更新日期:2020-10-07 00:00:00
abstract::In humans, glucocorticoid excess may cause neuropsychiatric symptoms, including psychosis and cognitive impairment, and glucocorticoid signaling hyperactivation may sensitize to substance of abuse. The aim of this work was to evaluate whether exposure to glucocorticoid excess triggers molecular changes in dopaminergic...
journal_title:Current molecular pharmacology
pub_type: 杂志文章
doi:10.2174/187446720603140415215941
更新日期:2013-11-01 00:00:00
abstract::As gene therapy has matured from clinical trials to the first commercial products, understanding of the mechanisms of gene delivery has increased tremendously. This has also been reflected in viral vector development, creating a number of new approaches to tackle issues in transduction efficiency, biodistribution and ...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467210801010013
更新日期:2008-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVE:Sphingolipid metabolites, including ceramide, sphingosine, and their phosphorylates (ceramide-1-phosphonate [C1P] and sphingosine-1-phosphate [S1P]), regulate diverse cellular processes including apoptosis, the cell cycle, and cellular differentiation. Recent studies have shown that these sphin...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467211666180516101111
更新日期:2018-01-01 00:00:00
abstract::Ca(2+) influx via L-type Ca(2+) channel (L-VDCC; CaV1.2) is required for cardiac and smooth muscle contraction. These channels are located in the plasma membrane and along the T-tubules (in cardiomyocytes), along with various scaffold and trafficking proteins. CaV1.2 is modulated by different hormones and transmitters...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467208666150507094733
更新日期:2015-01-01 00:00:00
abstract:BACKGROUND:Alterations in microRNAs (miRNAs) are related to the occurrence of nasopharyngeal carcinoma (NPC) and play an important role in the molecular mechanism of NPC. Our previous studies show low expression of 14-3-3σ (SFN) is related to the metastasis and differentiation of NPC, but the underlying molecular mecha...
journal_title:Current molecular pharmacology
pub_type: 杂志文章
doi:10.2174/1874467212666181218113930
更新日期:2019-01-01 00:00:00
abstract::Inhibition of voltage-gated L-type calcium channels by organic calcium channel blockers is a well-established pharmacodynamic concept for the treatment of hypertension and cardiac ischemia. Since decades these antihypertensives (such as the dihydropyridines amlodipine, felodipine or nifedipine) belong to the most wide...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467208666150507105845
更新日期:2015-01-01 00:00:00
abstract::The successful treatment of hematological malignancies remains challenging. Prognosis is often dismal given the frequency of disease relapse or treatment refractory disease. Cytotoxic and cytostatic chemotherapy remain mainstream therapeutics for most hematological malignancies. However, improved understanding of tumo...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467208666150716121253
更新日期:2016-01-01 00:00:00
abstract::Nelfinavir (Viracept) was originally designed as a specific HIV protease inhibitor and, since its introduction in 1997, has served as an effective, reliable, and well-tolerated HIV drug. Although nelfinavir is being increasingly displaced by second generation HIV protease inhibitors that allow better combination treat...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467211003020091
更新日期:2010-06-01 00:00:00
abstract::Valproic acid (VPA, 2-propylpentanoic acid) has been widely used as an antiepileptic drug and for the therapy of bipolar disorders for several years. Its mechanism of action was initially found to be primarily related to neurotransmission and modulation of intracellular pathways. More recently, it emerged as an anti-n...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467210902010095
更新日期:2009-01-01 00:00:00
abstract::For more than 30 years, lipid droplets (LDs) were considered as an inert bag of lipid for storage of energy-rich fat molecules. Following a paradigm shift almost a decade ago, LDs are presently considered an active subcellular organelle especially designed for assembling, storing and subsequently supplying lipids for ...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467208666150817111727
更新日期:2017-01-01 00:00:00
abstract:BACKGROUND:The use of drugs of addiction, as mephedrone, is associated with functional neuronal disorders due to remodeling of the nervous tissue. Key enzymes in remodeling are extracellular matrix (ECM) proteases like matrix metalloproteases (MMPs). Recently, MMPs have been of great interest as some studies point to a...
journal_title:Current molecular pharmacology
pub_type: 杂志文章
doi:10.2174/1874467212666190114154307
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVE:Recently, nitric oxide (NO) and hydrogen sulfide (H2S) donating moieties were extensively studied for their role in the vasculature as they are responsible for many cellular and pathophysiological functioning. The objective of the present study is to evaluate novel NO and H2S donating chalcone ...
journal_title:Current molecular pharmacology
pub_type: 杂志文章
doi:10.2174/1874467212666191025092346
更新日期:2020-01-01 00:00:00
abstract::The androgen receptor plays a pivotal role in the sebaceous glands. Its primary function is to stimulate cell proliferation and differentiation in the sebaceous and its associate with acne. Previous studies have demonstrated expression of AR and steroidogenic enzymes in normal sebaceous glands and in all sebaceous dis...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467208666150710120217
更新日期:2016-01-01 00:00:00
abstract:BACKGROUND:Mutations in the brain-derived neurotrophic factor (BDNF) gene and its receptor, tyrosine receptor kinase B (TrkB), have been reported to cause severe obesity in rodents. Our previous study demonstrated that the oral administration of 5% Eucommia leaf extract (ELE) or ELE aroma treatment (ELE aroma) produced...
journal_title:Current molecular pharmacology
pub_type: 杂志文章
doi:10.2174/1874467213666200505094631
更新日期:2021-01-01 00:00:00
abstract::Bone morphogenetic proteins (BMPs) were discovered in 1965 as potent inducers of ectopic bone formation when implanted subcutaneously. BMP2, BMP4, BMP6, and BMP7 are osteoinductive, and BMP2 and BMP7 are currently approved for clinical applications such as bone fracture healing and spine surgery. Although BMPs' role i...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467211205020153
更新日期:2012-06-01 00:00:00
abstract::Cannabinoid (CB) agonists exhibit numerous potentially useful pharmacological properties, but unwanted side effects limit their use in clinical practice. Thus, novel strategies are needed to identify potential CB pharmaceuticals with fewer side effects. Activated CB receptors initiate multiple parallel intracellular s...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467210801030273
更新日期:2008-11-01 00:00:00
abstract::Stem cells are unique cell types with the ability of self-renewal and differentiation, which mainly include embryonic stem cells, induced pluripotent stem cells, and adult stem cells. Recently, several research groups have reported that stem cells can differentiate into germ cells under appropriate conditions in vitro...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467208666150928154053
更新日期:2016-01-01 00:00:00
abstract:BACKGROUND:There has been a constant pursuit for development of newer therapies which can contribute to the relatively nascent field of cardioprotection in the setting of myocardial ischemiareperfusion injury. One novel cardioprotective agent among others, that has shown promising results in the limited number of resea...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467210666170223101422
更新日期:2018-01-01 00:00:00
abstract::DNA is modified by many mutagens, including reactive oxygen species (ROS). When ROS react with DNA, various kinds of modified base and/or sugar moieties are produced. One of the most important oxidative DNA lesions is 7,8-dihydro-8-oxoguanine (8-oxo-G). Contrary to normal deoxyguanosine, 8-oxo-G favors a syn conformat...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467210801020162
更新日期:2008-06-01 00:00:00
abstract::The mevalonic acid synthesis pathway, cholesterol, and lipoproteins play fundamental roles in lung physiology and the innate immune response. Recent literature investigating roles for cholesterol synthesis and trafficking in host defense against respiratory infection was critically reviewed. The innate immune response...
journal_title:Current molecular pharmacology
pub_type: 杂志文章
doi:10.2174/1874467209666160112123603
更新日期:2017-01-01 00:00:00
abstract::Cystic fibrosis (CF) is a hereditary disease caused by mutations in the gene encoding the chloride channel "cystic fibrosis transmembrane conductance regulator" (CFTR). The lack of functional CFTR in CF airways leads to impaired ion and fluid homeostasis of the fluid layer which lines the airway surfaces (ASL). The AS...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/18744672112059990025
更新日期:2013-03-01 00:00:00
abstract::FK506-binding proteins have been implicated in numerous human diseases suggesting novel therapeutic opportunities. In particular, the large FKBP51 has emerged as an important regulator of the stress-coping system and as an established risk factor for stress-related disorders. The principal druggabilty of FKBPs is evid...
journal_title:Current molecular pharmacology
pub_type: 杂志文章,评审
doi:10.2174/1874467208666150519113313
更新日期:2015-01-01 00:00:00
abstract:BACKGROUND:Allosteric modulators of G-protein coupled receptors regulate receptor activity by binding to sites other than the active site and have emerged as a new and highly desirable class of drugs. PAOPA (3(R)-[(2(S)- pyrrolidinylcarbonyl)amino]-2-oxo-1-pyrrolidineacetamide), a peptidomimetic analog of Prolyl-Leucyl...
journal_title:Current molecular pharmacology
pub_type: 杂志文章
doi:10.2174/1874467213666200910091007
更新日期:2020-09-09 00:00:00