Abstract:
PURPOSE:Present investigation was aimed to fabricate nanocrystal of exemestane, an anticancer drug with poor dissolution properties and oral bioavailability. METHODS:Influence of various process parameters on the formulation of exemestane nanosuspension using media milling technique were investigated in the trial batches. Box-Behnken design was applied with independent variables identified in the preliminary studies, viz. X1-Milling time, X2-Amount of stabilizer and X3-Amount of milling agent. In vitro dissolution and in vivo studies were carried out. Solid state characterization (PXRD, SEM, and DSC) studies demonstrated physical changes in drug due to nano-crystallization. Accelerated stability studies of optimized formulation were carried out. RESULTS:Individual process attributes exhibited significant effect on the average particle size of exemestane nanosuspension. Dissolution studies revealed enhancement in drug release rate as compared to pure exemestane powder. The in vivo pharmacokinetic parameters of exemestane nanosuspension showed significant improvement in Cmax and AUC0-t, about 283.85% and 271.63% respectively suggesting amelioration in oral bioavailability by 2.7-fold as compared to pure exemestane. Accelerated stability studies of the optimized formulation suggested stability of the nanocrystals for at least sixmonth period. CONCLUSION:Nanocrystals prepared by media milling technique were successful in improving the poor dissolution properties and oral bioavailability of exemestane.
journal_name
Curr Drug Delivjournal_title
Current drug deliveryauthors
Parmar K,Shah Jdoi
10.2174/1567201818999210112190716subject
Has Abstractpub_date
2021-01-12 00:00:00eissn
1567-2018issn
1875-5704pii
CDD-EPUB-113251pub_type
杂志文章abstract:OBJECTIVE:An injectable long acting In-Situ Forming Gel (ISFG) of human Growth Hormone (hGH) was prepared by using triblock PCL-PEG-PCL (Mw 1500-1500-1500). Ring-Opening Polymerization (ROP) of triblock using microwave was applied. METHODS:The BCA protein assay Kit was used to determine the concentration of hGH in the...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201817666200120120105
更新日期:2020-01-01 00:00:00
abstract:BACKGROUND:Atenolol has been used to treat angina and hypertension, either alone or with other antihypertensives. Despite its usefulness, it shows some side effects such as diarrhea and nausea in some patients. A method for slow release of atenolol in intestine is helpful to prevent such side effects. METHODS:A facile...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201813666160321115543
更新日期:2016-01-01 00:00:00
abstract::Percutaneous coronary intervention (PCI) has become a highly effective alternative for the treatment of coronary artery disease. The use of stents has reduced the rates of restenosis by preventing elastic recoil and negative remodeling, however neointima formation still remains an issue. Local drug delivery is an attr...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720111796642282
更新日期:2011-09-01 00:00:00
abstract::The objective of this study was to develop and evaluate mucoadhesive microsphere of diclofenac sodium with natural gums for sustained delivery. Guar gum and tragacanth were used along with sodium alginate as mucoadhesive polymers. Microspheres were formulated using orifice-ionic gelation method. Particle size, surface...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/15672018113109990054
更新日期:2013-12-01 00:00:00
abstract::In the present study, cross linked sodium carboxymethylated pea starch (SCPS) was synthesized and evaluated as tablet superdisintegrant in diclofenac sodium based tablets. SCPS was synthesized using native pea starch with monochloroacetic acid and NaOH in microwave radiation environment. Finally the dried product was ...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720111794479853
更新日期:2011-03-01 00:00:00
abstract:BACKGROUND:Bupivacaine is the most used local anesthetic in surgical procedures, producing prolonged anesthesia. The major limiting factor for the clinical use of bupivacaine comes from its systemic toxicity. Nanostructured lipid carriers (NLC) are vehicles for sustained drug delivery that are able to minimize the toxi...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201814666170726101113
更新日期:2018-01-01 00:00:00
abstract::Serrapeptase is an anti-inflammatory, proteolytic enzyme isolated from the microorganism, Serratia sp. HY-6. Very few methods are available for the quantification of serrapeptase. The activity of the enzyme is determined by an ELISA assay, colorimetric method using casein as substrate or by HPLC method. These methods ...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720108785915023
更新日期:2008-10-01 00:00:00
abstract:AIM:This study was focused on the formulation of the multi-unit extended-release peroral delivery device of lamotrigine for better management of epilepsy. BACKGROUND:The single-unit extended-release peroral preparations often suffer from all-or-none effect. A significant number of multi-unit delivery systems have been...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201817666200317124022
更新日期:2020-01-01 00:00:00
abstract::Fast-dissolving drug delivery systems have been developed as an alternative to conventional dosage form as an oral means of drug delivery in case of chronic conditions. Now a day's fast dissolving films are preferred over conventional tablets and capsules for masking the taste of bitter drugs to increase the patient c...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720111795768022
更新日期:2011-07-01 00:00:00
abstract::The blood brain barrier protects the brain from harmful substances in the blood stream and has stopped the development of many powerful and interesting drugs candidates for central nervous system due to the low poor distribution and by efflux mechanisms. Many different approaches have been developed in order to overco...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720109788680912
更新日期:2009-07-01 00:00:00
abstract::The stratum corneum (SC) is a primary rate limiting barrier to permeation of drug molecules through the skin. Small molecular weight lipophilic drugs that are effective at low doses can be effectively delivered by passive transdermal delivery. The SC does not permit passage of polar/hydrophilic and macromolecules. Pas...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720110791011765
更新日期:2010-04-01 00:00:00
abstract:BACKGROUND:Fluoroquinolones, the synthetic antibacterial agents are being successfully utilized against bacterial infections, since the time immemorial. Despite of enormous useful features, these drugs are associated with some limitations also. Large number of efforts has been made by various scientists to improve phar...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201813666161018153852
更新日期:2018-02-14 00:00:00
abstract::Since the discovery of Helicobacter pylori (H. pylori) in the early 1980s, its eradication has been one of the most important global challenges in gastroenterology. Various circumstances make the treatment with antimicrobials particularly difficult. One problem has been that antibiotics commonly used were designed for...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201811666140327145049
更新日期:2014-01-01 00:00:00
abstract::Recent studies have focused on the potential use of metal-based complexes for the treatment of cancer. However, there are some limitations of metal-based ligands for the treatment of cancer due to their toxic effects. In the present study, a novel bimetallic Cu(II) complex, [Cu2(μ-(C6H5)2CHCOO)3 (bipy)2)](ClO4), has f...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201813666160111123739
更新日期:2016-01-01 00:00:00
abstract::Metformin (MTF) improves hyperglycemia primarily by suppressing glucose production by the liver. The objective of our investigation was to evaluate nanoemulsion as a promising carrier for MTF for sustained hypoglycemic effect. The drug was incorporated into oil phase of nanoemulsion, which finally improved biopharmace...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720181102140411160817
更新日期:2014-01-01 00:00:00
abstract::The most common feature for antigen-delivery systems is their particulate nature. Together with a certain depot effect, it is the particulate nature that primarily dictates whether the antigen-delivery system will be successful in inducing a certain type and strength of immune response. In this article, we will summar...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720106778559029
更新日期:2006-10-01 00:00:00
abstract:BACKGROUND:Essential oils are poor aqueous solubility and high volatility compounds. The encapsulation of essential oils with cyclodextrins (CDs) can protect them from the adverse environmental conditions and improve their stability. Therefore, increasing the functional capabilities of essential oils when they were use...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201817666200731164902
更新日期:2020-07-31 00:00:00
abstract:BACKGROUND:Mesoporous bioactive glass (MBG) has been widely studied because of its excellent histocompatibility and degradability. However, due to the lack of good osteoinductive activity, the pure MBG scaffold is not effective in repairing large-scale bone defects. OBJECTIVE:To observe the repair effect of MBG scaffo...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201817666200916091253
更新日期:2020-09-15 00:00:00
abstract:OBJECTIVE:The present study reports the use of MicrofluidizerTM technology to form a stable nanosuspension of atovaquone (ATQ) using quality by design (QbD) approach. METHODS:The patient-centric quality target product profile and critical quality attributes (CQAs) were identified. A Box-Behnken design was employed for...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201817666191227095019
更新日期:2020-01-01 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::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::Hepatocellular carcinoma (HCC) is most common lethal malignancy worldwide. About 80% of liver cancer cases are attributed to the combined effects of Hepatitis B and C virus infections. The factors affecting development of HCC include cirrhosis and histological markers of increased liver cell proliferation, environment...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:
更新日期:2013-11-24 00:00:00
abstract::The aim of the present work was to evaluate alginate hydrogels in the form of spherical beads as carrier for antithrombotic drugs for future use in artificial grafts. The ionotropic gelation technique was employed to prepare beads from the L. hyperborea stipe of alginate with two different alginate concentrations and ...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720110793360630
更新日期:2010-10-01 00:00:00
abstract:BACKGROUND:Nasal delivery of 20 (R) -ginsenoside Rg3 (Rg3) has a short-lived anti-fatigue effect owing to rapid clearance by nasal cilia. Thus, in order to extend the residence time of Rg3 in the nasal cavity, a new drug delivery system is needed. METHODS:Chitosan microspheres loaded with Rg3 were prepared using a mul...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201814666161109121151
更新日期:2017-09-06 00:00:00
abstract::The aim of this study was to design a silica-supported solid dispersion of lacidipine (LCDP) to enhance the dissolution rate and oral absorption using supercritical CO2 (scCO2) as a solvent. The formulation was characterized using differential scanning calorimetry, powder X-ray diffraction, scanning electron microscop...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201813666151203233232
更新日期:2016-01-01 00:00:00
abstract:OBJECTIVES:In this study, central composite factorial design was used for the preparation and optimization of chitosan/Na-alginate hydrogel films containing metformin via solvent evaporation technique. METHODS:Low and high molecular weight (MW) chitosan was used as a polymer in different concentrations while genipin w...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201815666180409102459
更新日期:2018-01-01 00:00:00
abstract::Mucosal administration of vaccines is one of the most popular approaches to induce desired immunity against various types of antigen and microbial in central as well as peripheral blood and in most external mucosal surfaces. The oral route is a preferred choice over parenteral route for this purpose mainly due to an e...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201811666140709112040
更新日期:2014-01-01 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::Scientists have always been interested in the use of natural polymers for drug delivery. Chitosan, being a natural cationic polysaccharide has received a great deal of attention in the past few years. It is obtained by deacetylation of chitin and is regarded as the second most ubiquitous polymer subsequent to cellulos...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201812666150310151657
更新日期:2015-01-01 00:00:00
abstract::The development of oral insulin using the eligen technology represents a significant advance in insulin administration which is expected to improve the quality of life of diabetic patients. As clinical studies progress, a great deal of interest has focused on the process by which this technology enables insulin absorp...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201053586001
更新日期:2005-04-01 00:00:00