Rapamycin-Loaded, Capryol 90 and Oleic Acid Mediated Nanoemulsions: Formulation Development, Characterization and Toxicity Assessment.

This study was planned to explore the capability of nanoemulsions (NEs) consisting of Capryol 90 and oleic acid for the delivery of rapamycin (RAP). Permeability and cytotoxicity of RAP-loaded NEs were also inspected. Pseudo-ternary phase diagrams were created with oleic acid and Capryol 90 (as oil phase) and four surfactants and co-surfactants at various weight ratios (R).

Application of Guanidine Hcl to Improve Enantioseparation of a Model Basic Drug, Cetirizine, By Capillary Electrophoresis Using Sulfated Β-Cyclodextrin.

A common approach in resolving enantiomers of chiral basic drugs by capillary electrophoresis (CE) is to use cyclodextrins (especially their anionic derivatives) as chiral selector in the acidic buffer (pH ≤ 3) in normal or reversed (carrier) mode. Then, some organic modifiers are added to the buffer solution if the resolution is not satisfactory. In case of cetirizine (CTN), applying the same approach, a reversed mode capillary zone electrophoresis (CZE) method with an acidic buffer and sulfated-β-cyclodextrine (S-bCD) as chiral selector, was failed and no complete enantioseparation was achieved.

Evaluation of Ion-pair Formation of Adefovir to Improve Permeation across Artificial and Biological Membranes.

Purpose: Adefovir is an antiviral drug that exhibits high hydrophilic properties and negligible bioavailability (less than 12%). It is only applied in the form of the ester prodrug adefovir dipivoxil (ADV). The oral bioavailability of ADV is limited (32% to 45%) by its low permeability (Class 3) and biological conversion of the prodrug to adefovir.

Physicochemical, Stress Degradation Evaluation and Pharmacokinetic Study of AZGH101; a New Synthesized COX2 Inhibitor after I.V. and Oral Administration in Male and Female Rats.

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 .

Pharmacokinetics and Biodistribution of Pegylated Methotrexate after IV Administration to Mice.

The efficacy of methotrexate (MTX) as an antimetabolite chemotherapeutic agent highly depends on its blood circulation half-life. In our previous study, different conjugates of MTX (MTX-PEG) were synthesized, their physicochemical properties were investigated and MTX-PEG5000 was finally selected as optimum drug-conjugate for further investigations. In the current work, first the stability of MTX-PEG5000 was studied at 37 °C and the results indicated its high stability in plasma (T = 144 h) and a relatively rapid degradation in tissue homogenate (T = 24 h).

Physicochemical, Stress Degradation Evaluation and Pharmacokinetic Study of AZGH102, a New Synthesized COX2 Inhibitors after I.V. and Oral Administration in Male and Female Rats.

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.

An investigation into the ability of alendronate ion pairs to increase oral absorption.

The purpose of this study is to increase oral absorption of the highly charged drug alendronate using an ion pair strategy. Ion pairing is a formulation approach in drug delivery that is performed to improve the lipophilicity of ionized drugs. Cationic counter ions, such as arginine, phenazopyridine, hyoscine and pyridostigmine, were selected to enhance the lipophilicity and permeability of alendronate.

A Simple and Specific Stability- Indicating RP-HPLC Method for Routine Assay of Adefovir Dipivoxil in Bulk and Tablet Dosage Form.

A simple and reliable stability-indicating RP-HPLC method was developed and validated for analysis of adefovir dipivoxil (ADV).The chromatographic separation was performed on a C column using a mixture of acetonitrile-citrate buffer (10 mM at pH 5.2) 36:64 (%v/v) as mobile phase, at a flow rate of 1.

Block Copolymer Stereoregularity and Its Impact on Polymeric Micellar Nanodrug Delivery.

Stereoregularity of polymers is known to influence their physicochemical and functional properties in the bulk form. Recent studies have also provided evidence for the effect of polymer stereoregularity on the physicochemical and functional properties of their self-assembled nanostructures. Research in this area has witnessed a relatively rapid pace in the past few years; however, to the best of our knowledge, a proper review of the literature has not been made to date.

Development and Validation of an HPLC Method for Determination of Amifostine and/or Its Metabolite (WR-1065) In Human Plasma Using OPA Derivatization and UV Detection.

A rapid, sensitive and reproducible HPLC method was developed and validated for the analysis of amifostine (AMF) and/or its metabolite, WR-1065 in human plasma. The method involves the alkylation of free sulfydryl group with iodoacetic acid followed by derivatization of the drug and its metabolite with o-phthaldialdehyde (OPA) and UVdetection at 340 nm. The derivatized AMF and WR-1065 were eluted in less than 11 min, and in the case of the metabolite with no interferences from the endogenous plasma peaks.

DETERMINATION OF FLUCONAZOLE IN HUMAN PLASMA BY REVERSE PHASE HIGH PERFORMANCE LIQUID CHROMATOGRAPHY.

A rapid, simple and reproducible high performance liquid chromatographic method was developed and validated for determination of fluconazole in human plasma. The separation was performed on MZ C8 column (125 x 4 mm, 5 µm) using acetonitrile - potassium dihydrogen phosphate buffer (15 : 85, v/v), pH 3.0, as the mobile phase at a flow rate of 1.

Formulation Development and Toxicity Assessment of Triacetin Mediated Nanoemulsions as Novel Delivery Systems for Rapamycin.

The aim of this investigation was to design and develop nanoemulsions (NEs) as novel delivery systems for rapamycin. Phase behavior of quaternary systems composed of Traicetin (as oil), various surfactants and co-surfactants and water at different surfactant/co-surfactant weight ratios was investigated by the construction of phase diagrams. Formulations were taken from the o/w NE region of the phase diagrams, depending upon the extent of NE domain.

A rapid HPLC method for determination of zolpidem and its degradation product in tablets using a monolithic column.

A simple, accurate reverse phase high-performance liquid chromatographic method, utilizing a monolithic silica column, for determination of zolpidem hemitartrate and its degradation product in tablet dosage form was developed. Analysis was achieved on the monolithic, C18 (100 mm, 3.9 mm) column, in isocratic mode with acetonitrile-NaH2PO4 (pH 7.

Occurrence of deoxynivalenol in foods for human consumption from tehran, iran.

The occurrence of deoxynivalenol (DON) in retail foods in Tehran (Iran) was determined using high-performance liquid chromatography technique and immunoaffinity column as the clean-up step. A method was validated for analysis of DON in rice, bread, puffed corn snack and wheat flour. The average recoveries and precision (RSD) for DON in different foods ranged 84.

Study on the effect of solution conditions on heat induced-aggregation of human alpha interferon.

A major problem in the formulation of therapeutic proteins is the irreversible protein aggregation. Recombinant human interferon alpha2b (rhIFNα2b) has poor stability and undergoes physical degradation. The aim of this study was to investigate the effect of solution conditions on the heat-induced aggregation of rhIFNα2b.

A reversed phase high performance liquid chromatographic method for determination of rapamycin.

Easily degradating and various isomeric forms of rapamycin (Sirolimus) face the determination of this compound to many challenges. In this study, we developed and validated the isocratic reversed phase high performance liquid chromatographic (RP-HPLC) method for rapamycin. Separation was performed on a C8 column (MZ, 15 × 4.

Improvement of capillary electrophoretic enantioseparation of fluoxetine by a cationic additive.

One of the problems encountered in CE separations of basic compounds is the adsorption of analytes onto the negatively charged capillary wall which could lead to poor repeatability of migration time and peak area. Additionally, separation of enantiomers of chiral of basic drugs is commonly carried out in low pH buffer which contributes to strong ionic interaction of the cationic drug ions with negatively charged chiral selectors. The two phenomena results in poor enantioseparations.

Rapid high performance liquid chromatographic method for determination of clarithromycin in human plasma using amperometric detection: application in pharmacokinetic and bioequivalence studies.

A rapid, sensitive and reproducible HPLC method using amperometric detector was developed and validated for the analysis of clarithromycin in human plasma. The separation was achieved on a monolithic silica column (MZ- C8 125×4.0 mm) using acetonitrile-methanol-potassium dihydrogen phosphate buffer (40:6:54,v/v), with pH of 7.

Development of a combined solution formulation of atropine sulfate and obidoxime chloride for autoinjector and evaluation of its stability.

Atropine (AT) and oximes, alone or in combination, have been proven greatly valuable therapeutics in the treatment of organophosphates intoxications. An injectable mixture of AT and obidoxime (OB) was formulated for the administration by automatic self-injector. The aqueous single dose solution contained 275 mg obidoxime chloride and 2.

Improvement of electrophoretic enantioseparation of amlodipine by polybrene.

In chiral and non-chiral electrophoretic resolution of basic drugs, adsorption of analytes to negatively charged capillary wall could lead to poor repeatability of migration time and peak area. In addition, chiral resolutions of basic drugs are commonly performed in low pH buffers. Therefore, longer analysis time due to suppression of electroosmotic flow (EOF) is another dilemma.

Rapid high-performance liquid chromatographic method for determination of adefovir in plasma using UV detection: application to pharmacokinetic studies.

A rapid, sensitive and reproducible HPLC method was developed and validated for the analysis of adefovir (CAS 106941-25-7) in human plasma. The separation was achieved on a monolithic silica column (Chromolith Performance RP-18e, 100 x 4.6 mm) using acetonitrile-ammonium dihydrogen phosphate buffer (6:94, v/v), pH 5.

Sensitive and rapid HPLC method for determination of memantine in human plasma using OPA derivatization and fluorescence detection: application to pharmacokinetic studies.

A rapid, sensitive and reproducible HPLC method was developed and validated for the analysis of memantine in human plasma after derivatization with o-phthaldialdehyde (OPA) and fluorescence detection. Amantadine was used as internal standard. The derivatized memantine and amantadine were eluted in less than 10 min with no interference from endogenous plasma peaks.

Synthesis and characterization of methotrexate polyethylene glycol esters as a drug delivery system.

Methotrexate (MTX) is one of the most common anticancer drugs used for chemotherapy so far. However some problems such as high toxicity and short plasma half-life, have limited its use. To overcome these limitations, conjugation with polymers such as polyethylene glycol (PEG) is one the efficient approaches which has been attempted in recent years.

A rapid high-performance liquid chromatographic method for the determination of pantoprazole in plasma using UV detection. Application in pharmacokinetic studies.

A rapid, sensitive and reproducible HPLC method was developed and validated for the analysis of pantoprazole (CAS 102625-70-7) in human plasma. The separation was achieved on a monolithic silica column using acetonitrile-potassium dihydrogen phosphate buffer (25:75,v/v), pH 3.0, as the mobile phase at a flow rate of 1.

Simultaneous determination of amoxicillin and clavulanic acid in human plasma by isocratic reversed-phase HPLC using UV detection.

A simple, rapid and sensitive isocratic reversed phase HPLC method with UV detection using internal standard has been developed and validated for simultaneous determination of amoxicillin and clavulanic acid in human plasma. The assay enables the measurement of amoxicillin and clavulanic acid for therapeutic drug monitoring with a minimum quantification limit of 15 and 30 ng ml(-1), respectively. The method involves simple, one-step extraction procedure and analytical recovery was complete.