Abstract:
BACKGROUND:Chrysin is a strong inhibitor of breast cancer resistance protein (BCRP) but it is practically insoluble in water. Effective solubilization of chrysin is critical for its pharmaceutical application as an absorption enhancer via inhibition of BCRP-mediated drug efflux. OBJECTIVE:This study aimed to develop an effective oral formulation of chrysin to improve its in vivo effect as an absorption enhancer. METHOD:Solid dispersions (SDs) of chrysin were prepared with hydrophilic carriers having surface acting properties and a pH modulator. In vitro and in vivo characterizations were performed to select the optimal SDs of chrysin. RESULTS:SDs with Brij®L4 and aminoclay was most effective in increasing the solubility of chrysin by 13-53 fold at varying drug-carrier ratios. Furthermore, SDs significantly improved the dissolution rate and extent of drug release. SDs (chrysin: Brij®L4: aminoclay=1:3:5) achieved approximately 60% and 83% drug release within 1 h and 8 h, respectively, in aqueous medium, while the dissolution of the untreated chrysin was less than 13%. XRD patterns indicated the amorphous state of chrysin in SDs. The SD formulation was effective in improving the bioavailability of topotecan, a BCRP substrate in rats. Following oral administration of topotecan with the SDs of chrysin, the Cmax and AUC of topotecan was enhanced by approximately 2.6- and 2-fold, respectively, while the untreated chrysin had no effect. CONCLUSION:The SD formulation of chrysin with Brij®L4 and aminoclay appeared to be promising in improving the dissolution of chrysin and enhancing its in vivo effect as an absorption enhancer.
journal_name
Curr Drug Delivjournal_title
Current drug deliveryauthors
Lee SH,Lee YS,Song JG,Han HKdoi
10.2174/1567201815666180924151458subject
Has Abstractpub_date
2019-01-01 00:00:00pages
86-92issue
1eissn
1567-2018issn
1875-5704pii
CDD-EPUB-93186journal_volume
16pub_type
杂志文章abstract:OBJECTIVE:A new tumor targeted polymer-coated gold/graphene hybrid has been developed for achieving simultaneously thermoablation and chemoterapy of folate receptor-positive cancer cells. METHODS:The gold/graphene hybrid was prepared by depositing gold nanospheres onto graphene oxide and coating it with an inulin-fola...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201813666160520113804
更新日期:2017-01-01 00:00:00
abstract::The objective of this investigation was aimed to explore the cancer targeting potential of folate conjugated dendrimer (polypropylene imine, PPI) under strategic influence of folate receptor up-regulators (all trans Retinoic acid, ATRA and Dexamethasone, DEXA). The folate conjugated dendrimer nanoconjugate (FPPI) was ...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201811310040012
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abstract::There are still so-called unmet needs in the treatment of epithelial and cutaneous lesions. Mucositis, ocular lesions, chronic skin wounds represent typical examples. These pathologies do not yet afford a satisfactory treatment. In particular chronic wounds represent a major health care burden, likely to increase as t...
journal_title:Current drug delivery
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abstract:BACKGROUND:Subarachnoid hemorrhage (SAH) is considered as a violent disease with high rate of morbidity and mortality. Early brain injury (EBI) and delayed vasospasm are the two aspects of this disease that are becoming research hotspots. OBJECTIVE:We aim to update the role of oxidative stress in the development of EB...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201813666161025115531
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abstract::Nowadays, cancer is one of the deadliest diseases affecting an annually enormous number of people. Around 9.6 million people had died from different cancer types in 2018. Chemotherapy is considered to be a mainline treatment, and systemic administration of a single anticancer agent is also considered as vital clinical...
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pub_type: 杂志文章
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abstract:BACKGROUND:Tuberculosis is an infection and caused by gentle growing bacteria. The Internet provides opportunities for people with tuberculosis (TB) to connect with one another to address these challenges. OBJECTIVE:The aim of this paper is to introduce readers to the platforms on which Tuberculosis participants inter...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201814666171120125916
更新日期:2018-01-01 00:00:00
abstract::The discovery of liposome or lipid vesicle emerged from self forming enclosed lipid bi-layer upon hydration; liposome drug delivery systems have played a significant role in formulation of potent drug to improve therapeutics. Recently the liposome formulations are targeted to reduce toxicity and increase accumulation ...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720107782151269
更新日期:2007-10-01 00:00:00
abstract:BACKGROUND:Colloidal systems are most prominent delivery systems mainly used as vehicles for the transportation, targeting the various types of biomolecules, proteins, peptides, synthetic medicinal agents. OBJECTIVE:To provide concise information on patents that are directly or indirectly related to the nanoemulsions....
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201812666150901111930
更新日期:2016-01-01 00:00:00
abstract::The research presented in this paper discusses the potential of iontophoresis facilitated transdermal delivery of glycine. Iontophoresis has been widely investigated as a noninvasive transdermal drug delivery system. Iontophoresis is the use of a low electric current to carry ionized as well as unionized drug molecule...
journal_title:Current drug delivery
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abstract::Conventional eye drops show relatively low bioavailability due to poor precorneal contact time. In situ hydrogels are of great importance in providing sustained ocular drug delivery. By exhibiting elastic properties they resist ocular drainage of the drug leading to longer contact times. In the present study an in sit...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720110791560928
更新日期:2010-07-01 00:00:00
abstract::The placenta has traditionally been considered as a highly permeable organ for a large variety of substances with diverse molecular structures that are readily able to cross it from the maternal blood to reach the foetus. This has recommended limiting the use of drugs during pregnancy as far as possible. However, our ...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201043334731
更新日期:2004-07-01 00:00:00
abstract:BACKGROUND:The scope of nanotechnology has been extended to almost every sphere of our daily life. As a result of this, nanocarriers like Carbon Nanotubes (CNTs) are gaining considerable attention for their use in various therapeutic and diagnostic applications. OBJECTIVE:The objective of the current article is to rev...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201817999200508092821
更新日期:2020-01-01 00:00:00
abstract::Previous studies suggested that caspofungin dose escalation against Candida species is more beneficial than currently used lower daily doses. Thus, we determined in vitro and in vivo activity of caspofungin against six wild-type C. albicans clinical isolates, the ATCC 10231 strain and an echinocandin resistant strain....
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201812666150623091336
更新日期:2016-01-01 00:00:00
abstract::Biphenyl Dimethyl Dicarboxylate (BDD) is insoluble in aqueous solution and the bioavailability after oral administration is low. Self-nanoemulsifying drug delivery system (SNEDDS) containing BDD has been successfully prepared using carefully selected ingredients which are less affected by pH and ionic strength changes...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720108784911695
更新日期:2008-07-01 00:00:00
abstract::The objective of present investigation was the characterization of chitosan films after in vivo implantation. Chitosan films were prepared at three dose loadings of paclitaxel by classical casting method. They were implanted subcutaneously in Swiss mice in the neck region and were removed at 7, 15, 21 and 30 days post...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720106777731028
更新日期:2006-07-01 00:00:00
abstract:OBJECTIVES:A ceftiofur hydrochloride long-acting oily suspension with no irritation was prepared by testing and optimizing the types and amounts of organic solvents, suspending agents, and surfactants.
Methods: Its properties, stability, injection site irritation, in vitro release, and pharmacokinetics in pigs were...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201817666200903165119
更新日期:2020-09-03 00:00:00
abstract::Since its discovery in 1796 by Edward Jenner, vaccines have been an integral aspect of therapeutics, combating a number of infectious diseases with remarkable success. In recent years, due to rapid advances in proteomics, genomics, biotechnology and immunology and the plethora of knowledge amassed in related fields, i...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720106776359249
更新日期:2006-04-01 00:00:00
abstract::Hydrogels can constitute reliable delivery systems of drugs, including those based on nucleic acids (NABDs) such as small interfering ribonucleic acid (siRNA). Their nature, structure, and response to physiological or external stimuli strongly influence the delivery mechanisms of entrapped active molecules, and, in tu...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201813666160721142202
更新日期:2017-01-01 00:00:00
abstract::The mucosal administration of vaccines is an area currently receiving a high level of interest due to potential advantages offered by this technique. These advantages include the ability to administer vaccines without need for needles, thus improving patient compliance with vaccination schedules, and the capacity to i...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201043334588
更新日期:2004-10-01 00:00:00
abstract::Cutaneous gene therapy and DNA vaccination are potential applications of plasmid delivery methods where a gene for an antigen or a therapeutic protein is inserted in the plasmid and applied to the skin. However, the delivery of the DNA plasmid is a major challenge due to the unusual physicochemical properties of the D...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720106775197493
更新日期:2006-01-01 00:00:00
abstract:BACKGROUND:Nanoparticles (NPs) suffer from rapid clearance from body and require frequent dosing if long treatment is required. METHOD:In order to solve this problem for solid lipid nanoparticles (SLN) and prolong their action, SLNs were incorporated into thermo-responsive Poloxamer sol-gels and their fate was investi...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201815666180201093424
更新日期:2018-01-01 00:00:00
abstract::ImmunoPET is a non-invasive imaging technology based on tracking and quantification of radiolabeled monoclonal antibodies, antibody fragments and peptides in vivo. The knowledge of distribution and expression levels of a given receptor is a key for successful receptor targeted cancer therapy. ImmunoPET performed with ...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720111793663589
更新日期:2011-01-01 00:00:00
abstract::The aim of this present research work was to prepare and evaluate alginate microspheres of aceclofenac by ionic gelation method for targeting the drug release in intestinal region and decrease distinct tissue protection in the stomach. This method offers to prepare microspheres which are important in controlling the r...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720112802650725
更新日期:2012-09-01 00:00:00
abstract:BACKGROUND:The management of TB is difficult due to the resistance developed by Mycobacterium tuberculosis against anti-tubercular drugs causes the new challenges for treating and managing the disease. OBJECTIVE:The objective of the study was to combat multiple drug resistance (MDR) exhibited by mycobacterium species ...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201813666160502124811
更新日期:2016-01-01 00:00:00
abstract::A palpable need for the optimization of therapeutic agents, due to challenges tackled by them such as poor pharmacokinetics and chemoresistance, has steered the journey towards novel interdisciplinary scientific field for emergence of nanostructure materials as a carrier for targeted delivery of therapeutic agents. Am...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201812666141229104304
更新日期:2015-01-01 00:00:00
abstract::Among the common myths in the cosmetics industry is the perception that acne only happens to teenagers, and specifically to females. However, acne is neither limited to a specific age, nor to a certain gender, it creates a stressful problem for many people. Many chemical treatments for acne were proven to be successfu...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201815666180913144145
更新日期:2019-01-01 00:00:00
abstract::Severe acute respiratory syndrome coronavirus 2 has spread rapidly since its discovery in December 2019 in the Chinese province of Hubei, reaching this day, all the continents. This scourge is, unfortunately, in lineage with various dangerous outbreaks such as Ebola, Cholera, Spanish flu, American seasonal flu. Until ...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201817666200917124241
更新日期:2020-09-17 00:00:00
abstract::The objective of the present study was to fabricate and evaluate a multiparticulate oral gastroretentive dosage form of baclofen characterized by a central large cavity (hollow core) promoting unmitigated floatation with practical applications to alleviate the signs and symptoms of spasticity and muscular rigidity. So...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201811666140414113838
更新日期:2014-01-01 00:00:00
abstract::The aim of the present work is the development and evaluation of solid lipid nanoparticles (SLNs) as carrier system for topical delivery of benzocaine (BZC) improving its local anesthesia aiming to produce a fast acting and long lasting topical formulation. BZC loaded SLNs were prepared using a full factorial design t...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201812666150703115126
更新日期:2015-01-01 00:00:00
abstract:BACKGROUND:Levofloxacin is a potent antibiotic with severe side effects due to its high doses. Bacterial resistance may be due to frequent use of antibiotics. Biogenic gold nanoparticles conjugated levofloxacin (Au-HSA-LvN-NPs) were developed by Human Serum Albumin (HSA) and nitrate reductasemediated pathways. METHODS...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201814666170316113432
更新日期:2017-01-01 00:00:00