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Publications (127)
Background: The present study aimed to determine the pharmacokinetic parameters and bioequivalence of the test medicinal product, apixaban 5 mg tablet, and its reference product, Eliquis®, in healthy male and female subjects under a fasted state. Methods: Before in vivo evaluation, the quality control parameters of the products were evaluated and c...
Posaconazole (PCZ) is a triazole antifungal agent with a broad-spectrum activity. Our research aims to present a novel approach by combining a 2-level fractional factorial design and machine learning to optimize both chromatography and extraction experiments, allowing for the development of a rapid method with a low limit of quantification (LOQ) in...
Biofilm-mediated osteomyelitis presents significant therapeutic challenges. Given the limitations of existing osteomyelitis treatment approaches, there is a distinct need to develop a localized drug delivery system that is biocompatible, biodegradable, and capable of controlled antibiotic release. Multivesicular liposomes (MVLs), characterized by t...
Cerasomes are a modified form of liposomes containing both inorganic and organic parts and due to their strong polyorganosiloxane surface have remarkably high morphological stability and provide easier functionalization compared with conventional liposomes. To investigate the potential of these nanocarriers for oral delivery, bile salt integrated c...
Background: Lately, there has been increasing interest in the benefits of metal-organic frameworks, and among them, zeolitic imidazolate frameworks (ZIF - 8) stand out as one of the most commonly employed systems owing to their unique characteristics. Objectives: Given that properties like particle size play a key role in biomedical applications of...
Bile salts were first used in the preparation of nanoparticles due to their stabilizing effects. As time went by, they attracted much attention and were increasingly employed in fabricating nanoparticles. It is well accepted that the physicochemical properties of nanoparticles are influential factors in their permeation, distribution, elimination a...
Aim: This study aimed to develop nanoaggregates of berberine–phospholipid complex incorporated into thiolated chitosan (TCS) hydrogel for the treatment of aphthous stomatitis. Methods: The berberine–phospholipid complex was formulated through the solvent evaporation technique and assembled into nanoaggregates. TCS was synthesized through the attach...
Background: Cerasomes, due to their external siloxane network, demonstrate markedly higher physicochemical stability and, therefore, easier handling and storage than liposomes. Objectives: The main objective of this study was to compare the pharmacokinetics (PK) of cerasome and liposome following intravenous administration. The PK of PEGylated and...
Over the last few years, among controlled-release delivery systems, multivesicular liposomes (MVLs) have attracted attention due to their unique benefits as a loco-regional drug delivery system. Considering the clinical limitations of the current treatment strategies for osteomyelitis, MVLs can be a suitable carrier for the local delivery of effect...
Background
Amphotericin B (AmB) is the first-line drug to treat invasive fungal infections. However, its delivery to the body and clinical use faces many challenges because of its poor solubility, poor pharmacokinetics, and severe nephrotoxicity.
Objectives
Due to the necessity for designing safer and more effective nanocarriers for AmB and the im...
This study aimed to prepare piperine (PIP) loaded liposomes in hyaluronic acid (HA) hydrogel to provide a hybrid superstructure for postoperative adhesion prevention. Liposomes were prepared using thin-film hydration method. The optimised formulation was characterised by size, SEM, TEM, FTIR, encapsulation efficiency (EE)% (w/w), and release patter...
Background:
Despite the advantages of direct intratumoral (IT) injection, the relatively rapid withdrawal of most anti-cancer drugs from the tumor due to their small molecular size limits the effectiveness of this method of administration. To address these limitations, recently, increasing attention has been directed to using slow-release biodegra...
Background:
A large number of new substances have insufficient biopharmaceutical properties for oral administration caused by their slow dissolution rate and poor solubility.
Objective:
The purpose of our experiment was to improve the physicochemical properties of a hydrophobic drug, quercetin, by the nanomilling approach.
Methods:
Quercetin n...
Objective
Breast cancer accounts for significant mortality worldwide. Here, we develop a localized, sustained-release delivery system for breast cancer therapy.
Methods
Sirolimus (SIR) core-shell nanofibers (NFs) are fabricated by coaxial electrospinning with poly(ε-caprolactone) (PCL) for the core and chitosan and PCL for the shell. The NFs were...
Current study intended to prepare and evaluate phospholipid-based, mixed micelles (MMs) to improve the ocular delivery of posaconazole (POS), a broad-spectrum antifungal drug. For this, MMs based on egg phosphatidylcholine (EPC), as the main component, in combination with various bile salts (sodium cholate (NaC), sodium deoxycholate (NaDC), sodium...
Background:
Efavirenz nanosuspensions (EZ-NSs) were developed by the wet milling method as the most promising top-down nanosizing technique. Different process and formulation parameters were studied and optimized to produce appropriate EZ-NS in suitable conditions to enhance drug dissolution.
Methods:
In the preliminary studies, various polymeri...
Simvastatin (SIM), an anti-hyperlipidemic agent, has poor solubility and dissolution rate, resulting in low bioavailability after oral administration. The present study aimed to enhance the dissolution rate of SIM by ternary solid dispersion formulation and therefore to improve its anti-hyperlipidemic effect.
Solid dispersions (SDs) with various ra...
Tumorectomy followed by radiotherapy, hormone, and chemotherapy, are the current mainstays for breast cancer treatment. However, these strategies have systemic toxicities and limited treatment outcomes. Hence, there is a crucial need for a novel controlled release delivery system for implantation following tumor resection to effectively prevent rec...
Objective:
Considering the limitations of conventional risperidone (RSP) therapies, the present research characterizes the usefulness of multivesicular liposomes (MVLs) as an efficient controlled-release carrier for this widely used antipsychotic drug, to be employed for the treatment of schizophrenia.
Methods:
A 23 full factorial design based o...
Objectives:
To investigate the pharmacokinetics, biodistribution and peritoneal retention of Ag2S quantum dots (Qds) after intraperitoneal (IP) injection into mice and to compare the results with those reported for the intravenous (IV) injection of these particles.
Methods:
Ag2S Qds was prepared by a simple one-step co-precipitation method and w...
Cancer is among the most challenging diseases in the world and the number of people who are diagnosed with various cancers is growing every year. Chemotherapy with cytotoxic drugs is one of the main strategies for cancer treatment, however cell cycle-specific drugs, as a wide group of cytotoxic drugs, suffer from having a short plasma half-life. Be...
Introduction: Osteomyelitis is a destructive inflammatory condition of the bone that is usually caused by a wide range of microorganisms especially Staphylococcus aureus. Considering the downsides of systemic antibiotic therapies as well as conventional local drug delivery systems such as using polymethylmethacrylate, this study aimed to develop, c...
Metal-organic frameworks (MOFs) are a fascinating class of crystalline porous materials composed of metal ions and organic ligands. Due to their attractive properties, MOFs can potentially offer biomedical field applications, such as drug delivery and imaging. This study aimed to systematically identify the affecting factors on the MOF characterist...
Many new chemical entities have limited water solubility and therefore show low and/or variable oral bioavailability. Among the various strategies to overcome this challenge, nanoformulations have emerged as an attractive strategy to improve the oral permeability and absorption of many hydrophobic drugs. In this paper, we give an overview of the mo...
In this study, an enzyme-triggered system based on β-cyclodextrin (β-CD) has been developed to achieve controlled release of hydrophobic drugs in the presence of maltogenic amylase (MAase). The inclusion complex formation of curcumin (CUR), as a model anticancer compound, with β-CD was characterized by fluorescence and Fourier transform infrared (F...
Metal–Organic Frameworks (MOFs) are a new class of crystalline porous structures which can be used as a novel structure in diverse fields of medical science. Several studies have shown that chromium supplementation can be effective in amelioration of biochemical parameters of diabetes and its renal complications. Therefore, a chromium‐containing MO...
Background
Niosomes, bilayer vesicles formed by the self-assembly of nonionic surfactants, are receiving increasing attention as potential oral drug delivery systems but the impact of niosomal formulation parameters on their oral capability has not been studied systematically. The aim of this study was to investigate the impact of surfactant compos...
Over the last few decades, intraperitoneal (IP) local drug delivery, providing high drug concentrations with prolonged retention in the peritoneal cavity, has opened a new horizon for the management of life-threatening peritoneal disorders, such as peritoneal carcinomatosis (PC). However, clinical translation of this strategy is hampered by several...
Background
The growing morbidity and mortality rate of chronic kidney disease (CKD) has forced researchers to find more efficient strategies for controlling this disease. Studies have proven the important role of alteration in iron, zinc and selenium metabolism in CKD pathological process. Nanotechnology, through synthetizing nano metal-organic fra...
A targeted and controlled drug delivery system based on β-cyclodextrin (β-CD) for encapsulation and controlled release of hydrophobic drugs in the presence of maltogenic amylase (MAase), as a cyclodextrin-hydrolyzing enzyme, and trastuzumab antibody has been developed. In this study, the inclusion complex of curcumin (CUR), as a model anticancer co...
Background
One common feature of chronic diseases, such as cancer, diabetes and chronic kidney disease (CKD), is the disruption of iron metabolism and increase in labile iron pool, which can result in excessive production of harmful oxidative stress. The proper management of iron metabolism in this situation can be a valuable tool to ameliorate pat...
The therapeutic efficacy of orally administered drugs is often restricted by their inherent limited oral bioavailability. Low water solubility, limited permeability through the intestinal barrier, instability in harsh environment of the gastrointestinal (GI) tract and being substrate of the efflux pumps and the cytochrome P450 (CYP) can impair oral...
The present study aimed at exploring the potential of the P-glycoprotein (P-gp) transporters as a barrier to the repaglinide (REG) epithelial permeability. In-vitro intestinal absorption models, the everted gut sac, and Caco-2 cell line, were used to study the possible role of P-gp in intestinal transport of REG. In the everted gut sacs, apparent p...
Objectives:
As the main pathway for the clearance of radiopharmaceutical from the body, kidney is a dose-limiting organ in medical application of radionuclides. Because of its unique physiology, radioactivity is seen to concentrate on kidney nonuniformly. This nonuniformity can be considered in nephron microstructures. A microdosimetry model of ki...
Allogeneic hematopoietic stem cell transplantation (AHSCT) is a major method of treatment for different hematologic and congenital disease. Graft versus host disease (GvHD) is a life-threatening adverse effect of AHSCT. Cyclosporine is the most important and common agent for GvHD prophylaxis. Because of variable and unpredictable pharmacokinetics o...
This study was aimed to develop a novel nanocarrier for coenzyme Q10 (CoQ10) by a green process that prevented the use of surfactants and organic solvents. Triglyceride/phospholipid‐based nanocarriers were developed through high‐pressure homogenization (an industrial feasible process), and a 25‐1 fractional factorial design was adopted to assess th...
Restenosis is one of the major complications affecting outcomes of percutaneous coronary interventions. The aims of this study were to formulate curcumin (CUR) nanoparticles by using only lipidic ingredients in the absence of any organic solvent and to determine key formulation parameters using 2-level factorial design. CUR nanoparticles were prepa...
Tadalafil (a phosphodiesterase-5 inhibitor) is a choice for treatment of pulmonary arterial hypertension (PAH) that is known as an increase in mean pulmonary arterial pressure ≥25 mmHg at rest and ≥30 mmHg during exercise with reduced cardiac output. The aim of this study was to prepare inhalable tadalafil nanocomposites as a dry powder formulation...
Purpose
We systematically investigated the effects of injection dose, particle size and surface charge on the pharmacokinetics, tissue distribution and excretion of Ag2S quantum dots (Qds) in rats and mice.
Methods
Three different doses of Ag2S Qds with similar size and composition were administrated to rats and mice. The effect of size and surfac...
Nanocarriers radiolabeled with [99mTc] can be used for diagnostic imaging and radionuclide therapy, as well as tracking their pharmacokinetic and biodistribution characteristics. Due to the advantages of niosomes as an ideal drug delivery system, in this study, the radiolabeling procedure of niosomes by [99mTc]-HMPAO complexes was investigated and...
Poor penetration of vancomycin into Central Nervous System (CNS) can lead to treatment failure. The aim of this study was to evaluate and compare CSF concentration and serum pharmacokinetics of high dose vancomycin by continuous infusion vs. intermittent infusion in post neurosurgical meningitis patients. Twenty patients were divided into two group...
The present study was conducted to investigate the performance of different size reduction techniques including probe sonication, extrusion, and high pressure homogenization for nanosizing of niosomes. Also, the effects of cholesterol content and surfactant type on the size and poly dispersity index (PDI) of the formulations were evaluated. Various...
The aim of current study was to investigate the effect of Brij decoration of liposomes on in-vitro and in-vivo characteristics of the nanocarriers. Two hydrophilic Brij surfactants (Brij 35 and Brij 78) with almost similar molecular weight but differing in acyl chain were incorporated into liposomal bilayers at two percentages (5% and 10%). Convent...
The purpose of the current study was to develop a novel liposomal formulation to improve the oral bioavailability of carvedilol, a Biopharmaceutics Classification System class II with poor aqueous solubility and extensive presystemic metabolism. Conventional and various surfactant-enriched carvedilol-loaded liposomes were prepared by thin film hydr...
Aim:
For simultaneous bioimaging and drug delivery via direct intratumoral injection, doxorubicin and Ag2S quantum dots co-loaded multifunctional niosomes were prepared and fully characterized.
Materials & methods:
Various theranostic niosomes were prepared and investigated regarding cytotoxicity, in vivo imaging, drug accumulation in breast can...
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 investigated invivo and in-vitro...
Nonsteroidal anti-inflammatory drugs (NSAIDs) act mainly via inhibition of prostaglandins synthesis by inhibition of cyclooxygenase (COX) isoenzymes (COX-1 and COX-2). Selective COX-2 inhibitors which are also known as coxibs provide the main therapeutic effects of NSAIDs. Zarghi et al. reported 6-benzoyl-2-(4-(methylsulfonyl) phenyl) quinoline-4-c...
Sirolimus (rapamycin) is a mammalian target of rapamycin (mTOR) inhibitor with immunosuppressive, antiproliferative, antiangiogenic, antifungal, anti-restenosis and anti-inflammatory properties. However, its clinical application is often hampered by poor aqueous solubility, first-pass metabolism, transport by p-glycoprotein efflux pump, limited ora...
Nanocrystals of tadalafil, a poorly water-soluble drug, were successfully prepared by sonoprecipitation technique for improving the solubility and dissolution rate. Tween 80 was selected as an efficient surfactant to inhibit aggregation in stabilization of drug nanocrystals. Response surface methodology based on central composite design (CCD) was u...
Specific delivery of therapeutic agents to solid tumors and their bioavailability at the target site are the most clinically important and challenging goals in cancer therapy. Liposomes are promising nanocarriers and have been well investigated for cancer therapy. In spite of preferred accumulation in tumors via the enhanced permeability and retent...
Aim:
In this study, the effects of liposome characteristics on oral absorption of doxorubicin, as a hydrophilic low-permeability drug, were investigated.
Materials & methods:
Different doxorubicin-loaded liposomes were prepared, characterized and orally administered to 18 groups of rats. Plasma concentrations of doxorubicin and its aglycone meta...
Glaucoma is a common progressive eye disorder and the treatment strategies will benefit from nanoparticulate delivery systems with high drug loading and sustained delivery of intraocular pressure lowering agents. Niosomes have been reported as a novel approach to improve drug low corneal penetration and bioavailability characteristics. Along with t...
Coxibs such as celecoxib, rofecoxib, and valdecoxib are introduced as selective COX-2 inhibitors to the market. It has been reported that inhibition of COX-2 beside traditional effects of NSAIDs, reduces the risk of colorectal, breast and lung cancers and also slow the progress of Alzheimer’s disease. Zarghi et al. reported 8-benzoyl-2-(4-(methylsu...
Ag2S quantum dots (Qds) are a new type of near-infrared Qds and hold great potential for in vivo imaging. There is great demand for versatile, practical, and environmentally-friendly processes for formation of hydrophilic Ag2S Qds. The present study prepared hydrophilic Ag2S near-infrared Qds using a simple, easy, one-step method. The Qds were char...
Aim:
To develop an ameliorated sirolimus (SIR) liposome for intramural delivery, the effects of various carrier physicochemical parameters on the antirestenosis efficacy were evaluated.
Materials & methods:
Different liposomes were prepared, characterized and administered to balloon injured rats (12 animal groups). Their efficacies were investig...
Assuring the efficient local delivery via biocompatible nanosystems can be considered as a promising therapy for restenosis. The aim of the present study was preparation, in vitro characterization, and in vivo efficacy evaluation of sirolimus containing chitosan decorated liposomes for restenosis treatment. Liposomes were coated with chitosan, lead...
Liposomes are self-assembled bilayer vesicles which have attracted a great deal of interest as potential carriers for a wide range of therapeutic agents. They have significantly decreased toxicity of drugs while improving or at least maintaining their efficacy. However, their further development has been hampered by their considerable instabilities...
The epidermal growth factor receptor (EGFR) is a promising target for anti-cancer therapy. The aim of this study was to design thermosensitive liposomes (TSL) functionalized with anti-EGFR ligands for targeted delivery and localized triggered release of chemotherapy. For targeting we used EGFR specific peptide (GE11) as well as Fab́ fragments of ce...
Despite the advantages of liposomal drug delivery, the bioavailability of the chemotherapeutic drugs to tumor cells is limited by their slow release from nanocarriers and low drug permeability across cell membranes. Drug encapsulation into stealth thermosensitive liposomes can improve drug delivery to tumors by combining efficient accumulation at t...
Oral administration of medication is the first option when patient compliance is considered. However, many barriers face oral absorption of drugs that limit bioavailability in about 90% of therapeutic agents. Utilization of nanoparticulate drug delivery systems is a major strategy for increasing oral absorption. They can improve oral bioavailabilit...
The purpose of this study was to prepare and characterize a hybrid system of moxifloxacin loaded niosomes incorporated into chitosan gel as a potential carrier for topical antimicrobial delivery. The prepared system was characterized regarding entrapment efficiency, particle size, zeta potential, in vitro drug release kinetics, morphology, FTIR ana...
Objectives:
Graft versus host disease (GVHD) is a life threatening reaction in the stem cell transplantation process. Nowadays Cyclosporine is the most commonly utilized agent for GVHD prophylaxis and it has a major role in successful transplantation. Cyclosporine has been applied for many years in this field but it could be stated that currently n...
A validated HPLC method was developed to determine the doxorubicin concentration in a small volume of rat plasma (60 mu L) with convenient fluorescence detection. Sample preparation includes a simple one-step liquid-liquid extraction using a minimum amount of organic solvent, with extraction recovery more than 95%. The analysis was accomplished usi...
Carvedilol (CRV) is an antihypertensive drug with both alpha and beta receptor blocking activity used to preclude angina and cardiac arrhythmias. To overcome the low, variable oral bioavailability of CRV, niosomal formulations were prepared and characterized: plain niosomes (without bile salts), bile salt-enriched niosomes (bilosomes containing var...
FTIR spectra of empty niosomes (A), carvedilol-loaded niosomes (B).
Abbreviations: FTIR, Fourier transform infrared; WN, Wavenumber.
Cervical cancer has been shown to be highly associated with human papillomavirus (HPV) infection. The viral oncogenes E6 and E7 are constantly expressed by the tumor cells and are therefore potent targets for therapeutic genetic vaccination. In the present study, it was investigated the potential effect of HPV-16 E6, E7 and L1 co-administration to...
A recirculating isolated perfused rat liver model was used to investigate the hepatobiliary disposition of etoposide and the effects of cyclosporine A (CyA) on the pattern of drug disposition in the bile and uptake in the liver.
The portal vein, bile duct, and superior vena cava were cannulated in four groups of rats. The perfusions were conducted...
Background and Aim: Today, cervical cancer has been shown to be highly associated with human papillomavirus (HPV) infection.
The viral oncogenes E6 and E7 are constantly expressed by the tumor cells and are therefore potent targets for therapeutic genetic
vaccination. The few studies are indicated on increasing cellular mediated immunity potency by...
A bioequivalence study of two verapamil formulations (generic verapamil tablets and Isoptin(®) tablets) was performed by comparing pharmacokinetic parameters of the parent drug and its major metabolite, norverapamil following a single dose administration of 80 mg verapamil hydrochloride in 22 healthy volunteers according to a randomized, two-period...
Chemotherapy research highly prioritizes overcoming the multidrug resistance (MDR) in human tumors. Liposomal formulation of fluoxetine, as a fourth generation chemosensitizer, was constructed and characterized for percent entrapment, release profile, morphology, particle size, zeta potential and stability. Liposomes were prepared using different a...
The purpose of this study was to investigate the effect of d-alpha tocopheryl polyethylene glycol 1000 succinate (TPGS) alone or in combination with other emulsifiers in the fabrication of etoposide-loaded PLGA-PEG nanoparticles for in vivo applications. Nanoparticles were prepared by nanoprecipitation or single-emulsion solvent evaporation method...
Restenosis after angioplasty remains a serious complication in clinical cardiology. This study aims to investigate the stealth colloidal systems for local intra-arterial drug delivery. Micelles from polyethylene glycol conjugated with phosphatidylethanolamine and PEGylated liposomes loaded with sirolimus were prepared and characterized with regard...
Etoposide, a widely used anticancer drug, exhibits low and variable oral bioavailability mainly because of being substrate for the efflux transporter, P-glycoprotein (P-gp). Therefore, the present study was aimed to investigate the effect of D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) and PEG 400 as P-gp inhibitors on the intestinal ab...
The purpose of the present study was to investigate the effect of polyethylene glycol (PEG) molecular weights (6000, 12000 and 20000) as solid dispersion (SD) carriers on the dissolution behavior of simvastatin. SDs with various drug : carrier ratios were prepared by solvent method and evaluated for dissolution rate. Differential scanning calorimet...
Purpose:
To investigate accelerated blood clearance (ABC) induction upon repeated injections of PLGA-PEG nanoparticles as a commonly used polymeric drug carrier.
Methods:
Etoposide-loaded PLGA-PEG NPs were developed and administered as the test dose to rats pre-injected with various NP treatments at certain time intervals. Pharmacokinetic parame...
Purpose:
This study was aimed at developing co-encapsulated stealth nanoliposomes containing PSC 833, an efficient MDR modulator, and doxorubicin (DOX) in order to increase the effectiveness and decrease adverse effects of the anticancer drug.
Methods:
In attempt to increase the encapsulation efficiency of drugs, different methods for liposome p...
This study was directed towards the preparation and optimization of PEGylated (PEG, poly(ethylene glycol)) estradiol benzoate (ESB)-loaded liposomes to be used for the treatment of restenosis by local vascular delivery. Various liposomal formulations were prepared by thin film hydration method followed by sonication. Response surface methodology wa...
The present study was aimed at developing a validated HPLC method to quantify the sufficiently low concentrations of etoposide and its cis-isomer in plasma and tissue samples with emphasize on (1) employing a conventional UV detector, (2) using a low biological sample size and a minimized organic solvent volume, and (3) providing precise informatio...
For preclinical study an HPLC method was developed and validated for the determination of a novel and selective cyclooxygenase-2 (COX-2) inhibitor in mouse plasma. The sample preparation procedure involved simple protein precipitation following extraction of analyte and internal standard (IS) from plasma. The separation was achieved on a Lichrosphe...
The main objective of this study was to formulate an effective controlled-release liposomal drug delivery system for sirolimus (SIR), a potent antiproliferative and anti-inflammatory drug, to be used for the treatment of restenosis following local vascular delivery. Liposomes were prepared using remote film loading method and characterized with reg...
The uptake and transport of 9-nitrocamptothecin (9-NC), a potent anticancer agent, across Caco-2 cell monolayers was studied as a free and PLGA nanoparticle loaded drug.
Different sizes (110 to 950 nm) of 9-nitrocamptothecin nanoparticles using poly (lactic-glycolic acid) were prepared by via the nanoprecipitation method. The transport of nanoparti...
In the treatment of peritoneal carcinomatosis, systemic chemotherapy is not quite effective due to the poor penetration of cytotoxic agents into the peritoneal cavity, whereas intraperitoneal administration of chemotherapeutic agents is generally accompanied by quick absorption of the free drug from the peritoneum. Local delivery of drugs with cont...
The purpose in this study was to investigate poly(ethylene glycol)-modified poly (d,l-lactide-co-glycolide) nanoparticles (PLGA-PEG-NPs) loading 9-nitrocamptothecin (9-NC) as a potent anticancer drug. 9-NC is an analog of the natural plant alkaloid camptothecin that has shown high antitumor activity and is currently in the end stage of clinical tri...
Thiacetazone (TAZ), one of the oldest known antituberculosis drugs, causes severe skin reactions in patients co-infected with tuberculosis and human immunodeficiency virus (HIV). KBF611 is a new fluorinated thiacetazone analogue that has shown strong antituberculosis effects. In order to provide valuable information for subsequent preclinical devel...
In the present study the release rate and kinetics of carbamazepine as a model drug from various single and bi-polymeric matrices were studied. Matrices containing different percentages of hydroxylpropyl methylcellulose (HPMC), ethylcellulose (EC), Eudragit RS (EuRS) or various ratios of polymer blends based on HPMC were prepared. In vitro release...
Peritoneal carcinomatosis is a serious concern when treating digestive or ovarian tumors. Treatment with systemic chemotherapy suffers from poor penetration of cytotoxic agents into the peritoneal cavity and is not quite effective. Local delivery of drugs, especially as controlled-release delivery systems like liposomes, could provide sustained and...
KBF-611 is a new thiosemicarbazone derivative which has demonstrated significant antituberculosis effect. A sensitive and specific HPLC method was established and validated for the determination of KBF-611 and its deacetylated metabolite (KM) in mouse and rabbit plasma. Chromatographic separation was achieved on a Eurospher-100 C8 column using acet...
Due to a narrow therapeutic range, measurment of theophylline serum levels is highly recommended in patients with a long-term theophylline therapy. In this regard, since blood sampling is an invasive method, exploring alternative methods using other biological fluids in particular saliva samples are targeted. This study was designed to determine an...
Background and purpose of the study: Propranolol HCl, a widely used drug in the treatment of cardiac arrhythmias and hypertension, is a weak basic drug with pH-dependent solubility that may show release problems from sustained release dosage forms at higher pH of small intestine. This might decrease drug bioavailability and cause variable oral abso...
The objective of this study was to evaluate the cytotoxicity and pharmacokinetics of total and lactone forms of 9-nitrocamptothecin (9-NC), an effective antineoplastic drug, after intravenous injection of drug incorporated into poly (DL-lactic-glycolic acid) nanoparticles (NPs). Drug-loaded NPs (9-NC.NP) were prepared by the nanoprecipitation metho...
Technetium-99m complex of hexamethyl-propylene-amineoxime (HMPAO) is used as an efficient agent to label liposomes. For this, 99mTc-HMPAO is incubated with preformed liposomes that contain glutathione (GSH). Effect of GSH and lipid concentration on labeling efficiency, as well as the effect of lipid composition on in vitro stability of labeled lipo...