Transport of Niosomal Aminexil through Whole Abdominal Skin of Rats

Introduction:  Androgenetic alopecia (AGA) is a common disease in both male and female genders which affect millions of people worldwide. Minoxidil and Aminexil can improve the blood supply of hair follicles by different mechanisms. Here, we report for the first time, the preparation and physicochemical evaluation of aminexil niosomes. Methods and Results:  We developed new noisome encapsulated aminexil formulation composed of sorbitan esters (Span™), their ethoxylated derivatives (Tween™) with cholesterol by lipid film hydration method. Four molar ratio were used. The suspension was centrifuged and the absorbance of the supernatant analyzed by UV spectrophotometer at the λ max. The morphological studies of niosomes of aminexil have been done by using transmission electronic microscope (TEM). Size distribution were evaluated by Malvern size analyzer. Release rate of niosomal aminexil was evaluated by Franz diffusion cell through abdominal skin of rat. Results showed that the prepared niosomes has good physical stability depicted as unchanged size distribution curves during six month storage formulation composed of the highest encapsulation. The formulation prepared was stable at room temperature. Slow and biphasic release profile of aminexil was also shown which could be contributed to slow diffusion of aminexil through lipid bilayer. Conclusions: It can be concluded that niosomes can be used as stable carriers for topical delivery of aminexil

Simultaneous Voltammetric Determination of Ascorbic Acid, Hydroquinone, Kojic Acid, and Arbutin in Pharmaceutical Samples; a New Approach for Quantitative Determination of Niosomal Formulations Loading Efficiency

Introduction: Arbutin (ABU) inhibits tyrosinase and thus prevents the formation of melanin, therefore, it used as a skin-lightening agent. Ascorbic acid (AA) used in therapeutical fields such as improving immunity, skin disorders, amelioration of injuries and burns. Hydroquinone (HQ) as one of the important skin-bleaching agents used to lighten areas of darkened skin such as freckles, melasma, age spots, and acne scars. Moreover, owing to ability of Kojic acid (KA) in preventing melanin formation, it used in whitening products because of this ability to limit melanin production. Due to the importance of quantitative determination of the four above mention drugs loading efficiency in niosomal formulations, a great attempt was made in the current work to provide a promising sensor using voltammetric techniques.   Methods and Results: BMITB/NiO/NPs/MCPE was prepared by mixing 0.2 g of 1-butyl-3-methylimidazoliumtetrafluoroborate (BMITB) as a binder, 0.8 g of paraffin, 0.1 g of NiO nanoparticles and 0.9 g of graphite powder. The electro-oxidation signals of ABU, KA, AA, and HQ were increased at the surface of modified sensor compared to the bare electrode. The obtained result shows that, at pH 7.0 phosphate buffer (0.1 M), the catalytic oxidation signals exhibited a wide linear range with a satisfactory low detection limit. Conclusions: The proposed sensor revealed good electrocatalytic activity towards ABU, KA, AA, and HQ. The proposed modified carbon paste electrode (BMITB/NiO/NPs/MCPE) was applied successfully for simultaneous analysis of trace amount of four above mention drugs in niosome carrier real samples

Kojic acid and hydroquinone non-ionic surfactant vesicles for topical application

Introduction: Pigmentation disorders are common skin diseases caused by a wide range of etiologic factors such as pregnancy, sunshine and some drugs, for example minocycline etc. Vesicle-entrapped anti-hyperpigmentation agents can protect the therapeutic compounds from environmental destructive causes (light, oxygen and …) and they also provide a sustained release condition in the skin application of these medications. Hereby, we present the initial report, on the basis of our knowledge, on a niosomal preparation with two active pharmaceutical agents. . Methods and Results: Kojic acid (KA) and hydroquinone (HQ) were chosen as typical depigmentation agents. Many niosomal formulations were prepared by film hydration method in which co-encapsulation or separate entrapment of these compounds were evaluated. Span (20, 40, 60 or 80), Tween (20, 40, 60 or 80) and cholesterol were the main bilayer formation compounds and deionized water, normal saline and phosphate buffer were utilized as hydration media. A few formulations resulted in formation of stable multilamellar vesicles (MLVs) with high encapsulation efficiency of active agents. Therefore, we used direct mixing method for niosome formation which showed appropriate formulation properties with average volume diameter less than 10 µm, high encapsulation efficiency and high protection ability for HQ against oxidation depicted as no color change was detected during the long term storage in open door jars. Release studies on prepared formulations showed a sustained drug delivery profiles for all vesicular formulations. Conclusions: Obtained results promised a new and appropriate drug delivery system for KA and HQ. Clinical trials with permitted ethical requirements should be done for application of these niosomes in topical niosomal gel, cream or lotion formulations

Determination of hydroquinone in food and pharmaceutical samples using a voltammetric based sensor employing NiO nanoparticle and ionic liquids

A sensitive modified carbon paste electrode (MCPE) employing NiO nanoparticle (NiO/NPs) and 1-butyl-3- methylimidazolium tetrafluoroborate (BMITFB) ionic liquid was used for trace level analysis of hydroquinone (HQ) in aqueous solution. Compared to bare electrode, the electro-oxidation signal of HQ was greatly improved. The obtained result shows that, the electro-oxidation signal was increased to about 2.5 times at the surface of (NiO/NPs/BMITFB/MCPE) compared to CPE. The linear response range and detection limit were found to be 0.1–500 μM and 0.05 μM by square wave voltammetry (SWV), respectively. NiO/NPs/BMITFB/MCPE was effectively applied for the determination of HQ in real samples such as Liposomes carrier containing HQ and water sample

Marketed New Drug Delivery Systems for Opioid Agonists/Antagonists ‎Administration: A Rapid Overview

Novel drug delivery systems for controlled-release of opioid agonists as a long time painkillers or opioid antagonists for opium, heroin, and alcohol addiction are under development or in clinical use today. In this article, the field of “new drug delivery systems” is momentarily reviewed from the viewpoint of the marketed opioid agonists/antagonists dosage forms today

Formulation of Rivastigmine Niosomes for Alzheimer Disease

Introduction: Alzheimer is a brain dysfunctional disease which could destroy the cognition and learning capabilities of the patient. Rivastigmine is an acetylcholine esterase inhibitor which can improve brain function in both Alzheimer and Parkinson's diseases. Hereby, we prepared niosomal formulations of rivastigmine for better penetration of this drug to brain. Methods and Results: Sorbitan esters (Span 20, 40, 60 and 80), their water-soluble derivatives (Tween 20, 40, 60 and 80) and cholesterol were used for preparation of niosomes by film hydration method. Deionized water was used as hydration medium. Volume diameter, drug release profile, rivastigmine encapsulation efficiency and vesicular stability were evaluated. All used surfactant combinations formed round and tubular multilamellar vesicles (MLVs). Single mode size distribution, high encapsulation efficiency (more than 70%), good stability of vesicles depicted as unchanged size and finally, diffusion-based release profiles were shown for many of niosomal formulations. Conclusions: Incorporation of rivastigmine into bilayer assemblies of niosomes compromises a good candidate for new drug delivery system which further studied in animal models will prove or reject its applicability in human

Preparation and Physicochemical Evaluation of Cochleate-based Carriers for Insulin

Introduction: Cochleates are  cylindrical lipid structures that are more stable against oxidation and temperature than liposomes.  Our research is formulation of  cochleates for oral delivery of insulin as a model protein drug. Protein drugs are softer from environmental degradation and poor oral absorption; therefore any carrier system for their oral delivery must have protection against enzymes and absorption  enhancing ability. Methods and Results: In this study, liposomes with different proportion of lipids (DPPC and DMPC) and cholesterol were prepared by film hydration method and converted to cochleates by hydrogel method with CaCl2 and MgCl2. Microscopically observation of structures was carried out by phase-contrast microscope and Scanning Electron Microscope (SEM). Physicochemical characteristics of these structures were evaluated by measuring size distribution  using with  laser light scattering technique, entrapment efficiency percentage, investigation of release profile, and stability of selected cochleates. HPLC method  was used for analytical evaluation of entrapped and released insulin.Best formulation of liposomes contains 70% of lipid and 30% of cholesterol. According to microscopic size distribution, cochleates with CaCl2 bridges were better. The size of vesicles was less than 6 µm. Insulin entrapment efficiency of cochleates with DPPC was more than DMPC type. Between 60-70% of encochleated insulin released after 2-4 hours in a buffer with pH 6.8. Conclusions:The results shows that cochleates can be suitable oral delivery systems for insulin

Highly sensitive and efficient voltammetric determination of ascorbic acid in food and pharmaceutical samples from aqueous solutions based on nanostructure carbon paste electrode as a sensor

A square wave voltammetric method for the trace analysis of ascorbic acid was developed in this study. Carbon paste electrode was modified with NiO nanoparticle and 1-butyl-3-methylimidazolium tetrafluoroborate as a binder. Electro-oxidation behavior of ascorbic acid on the modified electrode was studied, which indicated that the nanostructure modified electrode could efficiently promote electrocatalytic oxidation of ascorbic acid. A fast, selective, high sensitive and simple electrochemical strategy was then developed for trace analysis of ascorbic acid using the constructed electrode. The catalytic oxidation signal exhibited a wide linear range from 0.08 to 380.0 μM toward the concentration of ascorbic acid with a sensitivity of 0.0158 μA/μM, and the limit of detection was as low as 0.04 μM. The suggested sensor was also used for quantitative determination of ascorbic acid in food and pharmaceutical samples

Formulation and Physicochemical Characterization of Magnetic Nanoparticles Containing Brimonidine for Ophthalmic Drug Delivery

Introduction: Recently, magnetic nanoparticles (MNPs) drew a great attention for application in drug delivery systems. Due to their biocompatibility and non-toxic properties, they have potential to create versatile drug delivery systems. Brimonidine (a relatively selective alpha-2 adrenergic receptor agonist) has a significant effect on lowering intraocular pressure in glaucoma. In this study MNPs were coated with alginate and chitosan and loaded by brimonidine to prepare a drug delivery system applicable in glaucoma treatment. Methods and Results: Brimonidine, sodium alginate and MNPs have been prepared as a dispersion. Chitosan solution was added dropwise to the previous dispersion. The dispersion was centrifuged and the absorbance of the supernatant analyzed by UV spectrophotometer at the λmax of 246 nm. The final dispersion was freeze-dried. The morphological studies of chitosan alginate MNPs(C-A-MNPs) have been done by using transmission electronic microscope (TEM). The release rate of brimonidine tartrate was evaluated by Franz diffusion cell through cellophane membrane. Results showed that more than 93% of the brimonidine tartrate was loaded on the C-A-MNPs. The formulation prepared was stable at room temperature protected from light. Release study showed that less than 40% of the brimonidine was released after 2 hours compared to simple formulation of brimonidine solution which showed more than 80% release after 2 hours. This finding showed sustained release in C-A-MNPs formulation. Kinetic of drug release from C-A-MNPs was slower than blank and followed zero order. The stability of formulation was more than 2 years. Conclusions: It can be concluded that loading of brimonidine on C-S-MNPs may decrease the frequency of administration and increase the efficacy of the product

Biosynthesis of Srco3 nanostructures with honey as a green capping agent and reductant: photodynamic therapy

Objective (s): SrCO3 nanoparticles could be used as new biomedical sources in magnetic resonance imaging as a promising noninvasive imaging modality for the preoperative staging of breast cancer and monitoring of tumor response to therapy. The present study aimed to synthesize SrCO3 nanostructures using microwave irradiation in the presence of honey as a green capping agent and reductant. Materials and Methods: The optical properties of SrCO3 nanostructures were investigated using ultraviolet-visible (UV-Vis) spectroscopy. Sr(NO3)2.6H2O and NaOH were applied as the starting reagents. Fructose (32.56-38.2%) and glucose (28.54-31.3%), which were the main carbohydrates found in honey, were not only involved in stabilization, but they also acted as the reducing agents in the production of SrCO3 nanostructures. The produced nanostructures were characterized using X-ray diffraction analysis, Fourier transform infrared spectroscopy, scanning electron microscopy, and transmission electron microscopy.Results: Method of synthesis and chemical reagents were observed to affect the structural parameters, crystallite size, product size, morphology, and antioxidant activity. Conclusion: According to the results, honey could be used as a green capping agent and reductant for the synthesis of SrCO3 nanostructures as a novel structure to co-deliver therapeutic agents using photo-thermal agents. Moreover, honey has significant potential for diagnostic and therapeutic purposes in the future