Current Drug Therapy - Volume 15, Issue 1, 2020

Background: Adiponectin, a well-known adipokine plays a number of regulatory actions in human body metabolism. Decreased levels of adiponectin have been reported in type 2 diabetes mellitus, cardiovascular diseases, metabolic syndrome and hypertension. Coenzyme Q10 (Co Q10) is a fat-soluble antioxidant substance which has been reported to be effective in several metabolic disturbances such as insulin resistance and inflammation. Objective: Present systematic review and meta-analysis were performed to assess the effects of CoQ10 supplementation on adiponectin serum level. Methods: A comprehensive search was performed in electronic databases including EMBASE, Google scholar, and PubMed up to January 2018. A meta-analysis of eligible studies was performed using random effects model to estimate pooled effect size of CoQ10 supplementation on adiponectin. Results: A total of 209 subjects were recruited from 5 eligible studies. Meta-analysis did not suggest any significant effect of CoQ10 supplementation on adiponectin serum level (0.240 mg/dl, 95%CI: -0.216, 0.696, P= 0.303), without significant heterogeneity between included studies (I2= 40.9%, p= 0.149). Conclusion: Although present meta-analysis did not indicate any significant effects of CoQ10 supplementation on serum adiponectin levels but future long-term dose-response trials are needed before any firm conclusion.

Background: The therapeutic potency and efficacy of drugs can be affected by a patient’s dietary habit. The food composition and their nutritional value interact with drugs that lead to alteration of the therapeutic response of drugs in patients. Objective: This present review is an attempt to illustrate clinical reports of food-drug interaction. Further, it also highlights specific interaction mechanism(s) and the safety thereof. Methods: Through the search engine “Scopus”; literature on recent advances in food and drug interactions includes almost all therapeutic categories such as antimicrobials, antiviral, antifungal, antihistamines, anticoagulants, non-steroidal anti-inflammatory drugs, and drugs acting on the central nervous system and cardiovascular system. Results: Preclinical and clinical studies that have been conducted by various researchers affirm significant drug-food interactions across the various therapeutic categories of drugs. Preclinical studies have documented the effects of food, milk products, alcohols, fruit and vegetables on the drug absorption, metabolizing enzymes and drug transporters. The clinical studies on fruits/vegetables and drugs interactions report significant alteration in therapeutic response. Conclusion: Based on the preclinical and clinical reports, it can be concluded that the interaction of food with drug(s) significantly alters their therapeutic potential. The inputs from clinical practitioners to elucidate potential risk of food-drug interaction need to be intensified in order to prevent adverse clinical consequences.

Background: The recent trend of herbal drug delivery has been focused on developing novel drug delivery carriers to address problems related to solubility, oral bioavailability, skin permeation and stability. The phyto-phospholipid complex (phytosomes®) technology has been used to overcome the problems associated with many conventional herbal extracts. Aim: The present work aimed to formulate phospholipid-complex of the flavanoid Hesperidin to enhance its dissolution leading to enhanced oral bioavailability. Method: The complex was prepared by refluxing various molar ratios of hesperidin and PC followed by solvent evaporation. The prepared complexes were evaluated for saturation solubility, partition co-efficient and drug content. The free drug and phospholipid complexes were analyzed in DSC. Surface morphology of the prepared complexes was viewed using SEM images. Selected formulations were subjected to in vitro drug release study. Antioxidant effect was examined by free radical scavenging method. Results: Solubility and partition coefficient of the prepared complexes were improved in comparison to free drug. Based on the results of solubility, partition coefficient and drug content, formulation F2 was selected as an optimized batch. DSC thermograms confirmed the formation of phospholipid complex. Free Hesperidin and Hesperidin-phospholipid complex (F2) showed 46.9 % and 78.20 % of drug release, respectively, at seven hours phosphate buffer (pH 7.4). The optimized formulation showed concentration-dependent anti-oxidant property. Conclusion: Results of the present study suggested that the phospholipid complex of Hesperidin possesses the antioxidant potential and may be of potential use for improving the dissolution of hesperidin and hence oral bioavailability.

Background: The clinical application of Brinzolamide, a drug used in the treatment of glaucoma is limited due its poor aqueous solubility. Microemulsion based ocular delivery can be an effective means to improve its solubility and in turn the bioavailability. Objective: The main objective of the present work was optimization and characterization of Brinzolamide loaded microemulsion for the treatment of glaucoma. Method: The solubility of Brinzolamide in various oils and surfactants was checked in order to identify components of microemulsion. Pseudo-ternary phase diagram using Prosim software was plotted to identify microemulsion existence area. D-optimal mixture design was used for optimization of microemulsion. The optimized formulation consisted of Isopropyl myristate, Tween-80 and Transcutol-P as surfactant and co-surfactant respectively, and water. The chosen critical responses were droplet size, zeta potential, nepheloturbidimetric unit, and viscosity. Results: The selected optimal composition shows favorable features, such as droplet size (41.69 nm), Zeta potential (-9.496 mV), Viscosity (170.8 cps), Transparency (1.483 NTU) and pH (7.646) that are suitable for ocular delivery. Moreover, a prolonged drug release (78.08 % within 7 hour) was found in in-vitro experiments. By and large the formulation was found to be safe and nonirritant as proven by the ocular irritation study. Conclusion: Our study illustrated potential of Brinzolamide loaded microemulsion for ocular delivery for the treatment of glaucoma.

Background: Anti-reflux formulation is one of the popular formulations across the globe in the pharmaceutical industry used specifically for the management of gastro-oesophageal reflux disease. But, this formulation is less explored with respect to research. Anti-reflux formulation has challenges to show its antacid functionality, which could have synergies in the management of refluxes in gastro-oesophageal reflux disease. Alkalizing agents act as antacid and improve the acid neutralization capacity in the anti-reflux formulation, and can be used appropriately as they affect raft strength beyond certain (optimum) limits. Objective: The objective of this work is to investigate the significance of alkalizing agent in sodium alginate based on oral liquid anti-reflux suspension for the management of Gastro-oesophageal Reflux Disease (GERD). Methods: In the present study, the formulation was prepared using sodium alginate along with different alkalizing agents like calcium carbonate and sodium bicarbonate at different levels. The formulation was further studied for in-vitro characterization like pH, viscosity, Acid Neutralization Capacity (ANC), thickness, formation speed, flotation, and raft strength. Results: The formulation with a higher level of calcium carbonate as the alkalizing agent showed a positive effect on the acid neutralization capacity (20.83mEq) and raft strength (16.95g) as well. Whereas, the formulation with a higher level of sodium bi-carbonate (4.01%) showed improved acid neutralization (22.31mEq) but showed a negative effect on raft strengths (10.08g). Conclusion: Based on the study, the optimum levels include 5% sodium alginate, 1.6% calcium carbonate and 2.67% sodium bicarbonate to achieve good liquid suspension formulation possessing good acid neutralization capacity as well as raft strength.

Objectives: Dexmedetomidine, the alpha 2 agonist sedative and an analgesic agent may be beneficial in sedation for endoscopic intervention. Our aim was to compare the use of dexmedetomidine versus the traditional use of propofol as a sedative agent for colonoscopies. Methods: This study included 100 patients presenting for elective colonoscopy under sedation with random and equal allocation of patients into two groups; group P, in which patients received propofol in a loading dose of 1.5 mg/kg and maintenance dose of 0.5 mg/kg/hr, and group D, in which patients received dexmedetomidine at a loading dose of 1ug/kg and maintenance dose of 0.5 ug/kg/hr. In addition to the demographic data, time to recovery, time of discharge, and endoscopist rating were measured. Also, the hemodynamic parameters were recorded, and also the incidence of postoperative complications. Results: The basic patients' characteristics, time to recovery, and time of discharge were comparable between the two groups. Moreover, the endoscopist did not significantly report more convenient procedure with one group over the other. Also, there was no significant difference in hemodynamic parameters or in the incidence of complications between the two studied groups. However the use of dexmedetomidine decreased the incidence of hypoxemia. Conclusion: The use of dexmedetomidine seems to have a similar effect to the use of propofol as a sedative agent for lower GIT endoscopy with the positive effect of dexmedetomidine in decreasing the incidence of perioperative hypoxemia.

Objective: The objective of this study was to entrap water-insoluble drug itraconazole into polymer to form drug entrapped nanoparticles by using simple formulation strategy and characterize them for various in vitro properties. Method: Itraconazole (ITZ) encapsulated Eudragit E 100 nanoparticles (IEENs) were formulated by emulsification solvent evaporation technique. Results: Developed IEENs were evaluated for entrapment efficiency, particle size, polydispersity index, and drug release profile. It was clear that drug polymer ratio along with homogenization speed are the factors affecting droplet size of an emulsion. Evaluation was done by HPLC at 263nm. DSC, XRD studies were carried out. The in vitro antifungal study of nanoparticles suggested that they are more effective in inhibiting growth of Candida albicans. Conclusion: The results from this study suggest the potential use of IEENs to provide a possible way of improving solubility and thus oral absorption of Itraconazole. Thus the study concluded that IEENs have potential to effectively treat the fungal infection.

Background: Anthracyclines are widely used chemotherapeutic agents in several cancers. Since its use, survival improved significantly among cancer patients and has been reported to be up to 80%. However, anthracyclines possess several cardiac, renal and hematological toxicities which limit their use in practice. Cardiotoxicity is still the most important and dose-limiting side effect of anthracycline treatment. Here we aimed to investigate the frequency of anthracyclineinduced cardiomyopathy in pediatric malignancies in Khuzestan Province, Iran. Methods: A total of 112 patients were enrolled in the present study. Patients were allocated to the case or control group based on receiving anthracycline. Echocardiographic examinations were performed by a cardiologist. Electrocardiograms were also recorded. Results: We showed that cancer patients who underwent anthracycline treatment showed cardiomyopathy as defined by lower LVEF (Left Ventricular Ejection Fraction) among patients (p = 0.041). Abnormal LVEF was reported with a frequency of about 9.5% in patients (p = 0.026). However, LVFS (Left Ventricular Fraction Shortening), QRS voltage and QT interval did not differ significantly between treatment and control groups. Our data analysis revealed that this difference is mainly related to high cumulative dose since high cumulative dose of anthracycline (>300 mg/m2) leads to lower LVEF and LVFS and higher QRS voltage in comparison with lower cumulative dose (<300 mg/m2) and control group; but there was no significant difference between low dose and control group. Different age groups and type of malignancy including hematological and solid tumors did not show any significant differences for echocardiographic and electrocardiograms parameters. Conclusion: In our study, lower LVEF among patients who received anthracyclines were mainly related to a high cumulative dose of anthracyclines, which emphasizes the effect of cumulative dose for cardiotoxic effects. Larger studies are needed to investigate possible other risk factors for cardiotoxicity.