Stability of Compounded Topical Nifedipine in Cream, Gel, and Ointment Bases.

The objective of this study was to investigate the stability of compounded nifedipine cream in gel and ointment formulations dispensed in white plastic and glass amber jars. Extemporaneously compounded nifedipine cream (Glaxal Base), gel (K-Y Jelly), and ointment (Aquaphor) in white plastic and glass amber jars were stored at 4°C, 23°C, and 40°C. We determined potency on days 0, 7, 14, 30, 60, and 90, and subsequently assigned beyond-use-dates based on United States Pharmacopeia recommendations, organoleptic properties, and pH changes.

Drug-release Assessment of Compounded Topical Nifedipine and Diltiazem in Commonly Used Bases for Wound Healing.

The objective of this study was to determine release profiles of extemporaneously compounded nifedipine and diltiazem in commonly used bases in pharmacy practice. Release of nifedipine 0.2%, 2%, and 10% (w/w) from Glaxal Base, K-Y Jelly, and Aquaphor Healing Ointment, and of diltiazem 2% (w/w) from GlaxalBase, hydroxyethyl cellulose-based gel, and white petrolatum was quantified using the Franz-cell diffusion system.

Stability of Compounded Diltiazem Hydrochloride in Cream, Ointment, and Gel Formulations for Topical Use.

Interest in the topical use of compounded diltiazem has increased. Published information on the stability of such products is scarce. The objective of this study was to investigate the stability of diltiazem hydrochloride compounded in cream (Glaxal Base), ointment (white petrolatum), and hydroxyethyl cellulose-based gel over 90 days at room (23°C), refrigerator (4°C), and elevated (40°C) temperatures, stored in white plastic and glass amber containers.

Hemodynamic Assessment and In vivo Catabolism of Adenosine 5'-triphosphate in Doxorubicin or Isoproterenol-induced Cardiovascular Toxicity.

Objective: Previous studies have shown that catabolism of adenosine 5'-triphosphate (ATP) in systemic blood is a potential surrogate biomarker for cardiovascular toxicity. We compared the acute toxicity of high doses of doxorubicin (DOX) and isoproterenol (ISO) on hemodynamics and ATP catabolism in the systemic circulation.

Methods: sprague Dawley (SD) rats (n = 8 - 11) were each given either a single dose of 30 mg/kg ISO, or a twice-daily dose of 10 mg/kg of DOX or 4 doses of normal saline (control) by subcutaneous injection.

Compounded Topical Amitriptyline for Neuropathic Pain: In Vitro Release from Compounding Bases and Potential Correlation with Clinical Efficacy.

Background: Topical amitriptyline has been described as having mixed clinical efficacy for neuropathic pain. A few case reports using higher concentrations of this compound found clinical benefit, but many of these studies did not describe the components used in formulating the amitriptyline preparations.

Objective: To generate reproducible clinical measures of the characteristics of amitriptyline diffusion from selected compounding bases, to support a scientific approach to base selection when compounding this drug for neuropathic pain.

Compounded Topical Gabapentin for Neuropathic Pain: Does Choice of Base Affect Efficacy?

The objective of this study was to investigate the effect of Lipoderm Cream, VersaBase Gel, and Emollient Cream on the release and permeation of gabapentin formulated for neuropathic pain. Gabapentin of different strengths (1%, 5%, and 10%) was compounded with the bases, diffusion of the drug from thebases, and permeation through artificial skin model studied with Franz diffusionsystem. Steady-state flux, cumulative permeation, and lag times were calculated,and release mechanisms modelled with first order, second-order, Higuchi, Korsmeyer-Peppas, and Hixon-Crowell kinetic models.

Compounded gabapentin for neuropathic pain: Stability and beyond-use date (BUD) in some commonly used bases.

Objectives: To investigate the stability and beyond-use date (BUD) of topical gabapentin in 3 commonly used bases.

Methods: Lipoderm cream, Versabase gel, and Emollient cream were used to compound gabapentin (10%). The products were stored in Ecolojars, kept at 25°C, 4°C, and 40°C, and samples were collected on different days (days 0, 14, 28, and 90).

Stability Assessment of Topical Amitriptyline Extemporaneously Compounded with Lipoderm Base, PLO Gel Mediflo 30, and Emollient Cream.

Extemporaneous topical compounds for neuropathic pain offers an alternative or adjunct approach to existing therapies for patients. Assigning evidence-based beyond-use dating prior to dispensing topical medications is a legal requirement by pharmacy governing bodies. The purpose of this study was to utilize a validated stability-indicating high-performance liquid chromatography assay to determine beyond-use dating of topical amitriptyline in three different bases (Lipoderm Base, PLO Gel Mediflo 30, Emollient Cream) at three different temperatures [room temperature (25°C), refrigeration (4°C), and high temperature (40°C)].

Adenosine and Adenosine 5'-triphosphate Catabolism in Systemic Blood as a Potential Biomarker for Doxorubicin Cardiotoxicity in an Experimental Rat Model in vivo.

Background: Previous studies have shown that metabolism of adenosine 5'-triphosphate (ATP) in systemic blood is a potential surrogate biomarker for cardiovascular toxicity.

Objective: To investigate the acute effect of high dose of doxorubicin (DOX) on adenosine and ATP catabolism in systemic blood in vivo.

Method: Sprague Dawley (SD) rats were each given either 10 mg/kg of DOX (n = 8) or normal saline (1 mL/kg, n = 11) twice daily for 4 doses by subcutaneous (sc) injection.

Models for the study of nasal and sinus physiology in health and disease: A review of the literature.

Objective: Chronic sinusitis is a very common yet poorly understood medical condition with significant morbidity. Hence, it remains an entity that is difficult to treat with unsatisfactory outcomes of current management options. This necessitates research into the etiology and pathophysiology of the condition to enhance our knowledge and the therapeutic options.

An evaluation of the cold chain technology in South-East, Nigeria using Immunogenicity study on the measles vaccines.

Introduction: Vaccines are biological products and their efficacy is affected by storage conditions. They are vital in promoting public health. Failures in immunization programmes often times are blamed on disruption in vaccine cold-chain.

Improving the Efficiency of Respiratory Drug Delivery: A Review of Current Treatment Trends and Future Strategies for Asthma and Chronic Obstructive Pulmonary Disease.

Asthma and chronic obstructive pulmonary disease (COPD) are heterogeneous airway diseases associated with significant morbidity and mortality. Pharmacological treatment is delivered primarily through the inhalation route using various devices. Optimal disease control is highly dependent upon patient adherence.

Organic cation rhodamines for screening organic cation transporters in early stages of drug development.

The aim of this study was to investigate the suitability of rhodamine-123, rhodamine-6G and rhodamine B as non-radioactive probes for characterizing organic cation transporters in respiratory cells. Fluorescent characteristics of the compounds were validated under standard in vitro drug transport conditions (buffers, pH, and light). Uptake/transport kinetics and intracellular accumulation of the compounds were investigated.

Challenges in nasal drug absorption: how far have we come?

The nasal route is commonly used for local delivery of drugs to treat inflammatory conditions. It is also an attractive route for systemic delivery of some drugs. Irrespective of intended use, administered drugs must permeate the epithelial or olfactory membrane to be effective.

Effect of Cardiovascular Injury on Catabolism of Adenosine and Adenosine 5-'Triphosphate in Systemic Blood in a Freely Moving Rat Model In Vivo.

Background: Previous studies have shown that catabolism of adenosine 5'-triphosphate (ATP) in red blood cell (RBC) may be a key factor for cardiovascular protection and maintaining cardiovascular homeostasis.

Objective: To investigate the effect of cardiovascular injury on adenosine and ATP catabolism in systemic blood using a freely moving rat model in vivo.

Method: After acclimatized to the experimental environment, Sprague Dawley (SD) rats were each given either isoproterenol (30 mg/kg) or saline (1 mL/kg) by subcutaneous (sc) injection.

Thyroid hormone (levothyroxine) replacement via the respiratory route by inhalation: in vitro exploratory studies.

Objectives: To conduct proof of principle studies that will enable development of noninvasive (respiratory) delivery systems for levothyroxine (T4).

Methods: Preformulation (solubility, stability), formulation and biopharmaceutical (in vitro absorption, transport, gene expression) studies were conducted. Calu-3 cell line was used for permeation studies.

Drug transporters in the nasal epithelium: an overview of strategies in targeted drug delivery.

In this article, we discussed the expression of some ABC (e.g., P-glycoprortein, MRP and CFTR) and SLC (e.

Preliminary studies on validation of calu-3 cell line as a model for screening respiratory mucosa irritation and toxicity.

There is need to develop reproducible methods and experimental models for screening mucosal irritation and toxicity for drugs and pharmaceutical excipients. The aim of this study was to validate Calu-3 cell line as a model for screening respiratory irritation and toxicity of drugs and excipients. Eighteen test compounds were selected according to their irritation potential and European Centre for the Validation of Alternative Methods (ECVAM) guidelines.

Drug-eluting nasal implants: formulation, characterization, clinical applications and challenges.

Chronic inflammation and infection of the nasal sinuses, also referred to as Chronic Rhinosinusitis (CRS), severely affects patients' quality of life. Adhesions, ostial stenosis, infection and inflammation relapses complicate chronic sinusitis treatment strategies. Drug-eluting stents, packings or implants have been suggested as reasonable alternatives for addressing these concerns.

Cytoprotective potential of anti-ischemic drugs against chemotherapy-induced cardiotoxicity in H9c2 myoblast cell line.

To investigate potential prevention or attenuation of anti- cancer drug induced cardiotoxicity using anti-ischemic drugs, a rat myoblast (H9c2) cell line was used as our in vitro cardiac model. Irinotecan and doxorubicin were found to be cytotoxic for the H9c2 cell line with IC50 of 30.69 ± 6.

Organic cation transporters in human nasal primary culture: expression and functional activity.

Background: The majority of drugs cross epithelial cells by either passive diffusion or via carrier-mediated drug transporters. The aim of this study was to investigate the transport characteristics, protein expression and localization of organic cation transporters in human nasal epithelium.

Methods & Results: The expression, localization and transport characteristics of the transporters were investigated using permeation, PCR and immunohistochemistry.

Optimization of human nasal epithelium primary culture conditions for optimal proton oligopeptide and organic cation transporters expression in vitro.

Aim: To investigate the effect of key tissue culture conditions on cell growth, gene expression and functional uptake of peptide and organic cation transporter substrates in the human nasal epithelium (HNE).

Methods: HNE were cultured on different growth surfaces (polystyrene plastic, collagen film, and hydrated collagen gel) and were maintained with three popular nasal tissue culture media supplements [DMEM/F12 supplemented with Ultroser(®) G (2%), FBS (10%) and NuSerum(®) (10%)], respectively. The expression of gene transcripts for organic cation and peptide transporters were screened using qPCR and substrate uptake studies.

Characterization of Calu-3 cell monolayers as a model of bronchial epithelial transport: organic cation interaction studies.

Background: To fully exploit organic cation transporters for targeted drug delivery in the lung, the use of a readily available and well-characterized tissue culture model and cheap easily detectable substrates is indispensable.

Objectives: To investigate the suitability of Calu-3 as tissue model for characterizing organic cation permeation across the bronchial cells using a fluorescent dye, 4-(4-(Dimethylamino)styryl)-N-methylpyridinium iodide (4-DI-1-ASP).

Methods: Substrate uptake, inhibition, and transport were performed to establish active transport mechanism.

Proton-coupled oligopeptide transporter (POT) family expression in human nasal epithelium and their drug transport potential.

The molecular and functional expression of peptide transporters (PEPT1 and PEPT2, PHT1, PHT2) in human nasal epithelium was investigated. Quantitative/reverse transcriptase polymerase chain reaction (qPCR/RT-PCR), Western blotting and indirect immuno-histochemistry were used to investigate the functional gene and protein expression for the transporters. Uptake and transport studies were performed using metabolically stable peptides [β-alanyl-L-lysyl-Nε-7-amino-4-methyl-coumarin-3-acetic acid (β-Ala-Lys-AMCA) and β-alanyl-L-histidine (carnosine)].

Differential expression of organic cation transporters in normal and polyps human nasal epithelium: implications for in vitro drug delivery studies.

The aim of this study was to compare the expression of organic cation transporters (OCTs) in normal and polyps nasal epithelium. Primary cell cultures of human nasal epithelium (polyps and normal tissues) were compared by investigating the uptake of a fluorescent organic cation, [4-dimethylaminostyryl-N-methylpyridinium (4-Di-1-ASP)]. The effect of concentration, temperature, pH and competing inhibitors were investigated.