The main disadvantage of transdermal drug delivery is the poor penetration of most compounds into the human skin. The main barrier of the skin is located within its uppermost layer, the stratum corneum (SC). Several approaches have been developed to weaken this skin barrier. One of the approaches for increasing the skin penetration of drugs and many cosmetic chemicals is the use of vesicular systems, such as, liposomes and ethosomes. Ethosomes are phospholipid-based elastic nanovesicles containing a high content of ethanol (20-45%). Ethanol is known as an efficient permeation enhancer and has been added in the vesicular systems to prepare elastic nanovesicles. It can interact with the polar head group region of the lipid molecules, resulting in the reduction of the melting point of the stratum corneum lipid, thereby increasing lipid fluidity and cell membrane permeability. The high flexibility of vesicular membranes from the added ethanol permits the elastic vesicles to squeeze themselves through the pores, which are much smaller than their diameters. Ethosomal systems are much more efficient in delivering substances to the skin in the terms of quantity and depth, than either conventional liposomes or hydroalcoholic solutions. The scope of this small review is to introduce the novel concept of ethosomes and to describe some approaches and mechanisms of stimulating topical and transdermal products with ethosomes.

Microsponges are polymeric delivery systems composed of porous microspheres. They are tiny sponge-like spherical particles with a large porous surface. Moreover, they may enhance stability, reduce side effects and modify drug release favorably. Microsponge technology has many favorable characteristics, which make it a versatile drug delivery vehicle. Microsponge Systems are based on microscopic, polymer-based microspheres that can suspend or entrap a wide variety of substances, and can then be incorporated into a formulated product such as a gel, cream, liquid or powder. The outer surface is typically porous, allowing a sustained flow of substances out of the sphere. Microsponges are porous, polymeric microspheres that are used mostly for topical use and have recently been used for oral administration. Microsponges are designed to deliver a pharmaceutical active ingredient efficiently at the minimum dose and also to enhance stability, reduce side effects, and modify drug release.

The ocular insert represents a significant advancement in the therapy of eye disease. Ocular inserts are defined as sterile, thin, multilayered, drug-impregnated, solid or semisolid consistency devices placed into the cul-de-sac or conjuctival sac, whose size and shape are especially designed for ophthalmic application. They are composed of a polymeric support that may or may not contain a drug. The drug can later be incorporated as dispersion or a solution in the polymeric support. They offer several advantages as increased ocular residence and sustained release of medication into the eye. The insert includes a body portion sized to position within a lachrymal canaliculus of the eyelid. The inserts are classified according to their solubility as insoluble, soluble, or bioerodible inserts. The release of drug from the insert depends upon the diffusion, osmosis, and bioerosion of the drug, and this article is an attempt to present a brief about this newer drug delivery system.

Male hypogonadism is a condition in which the body does not produce enough of the testosterone hormone; the hormone that plays a key role in masculine growth and development during puberty. There is a clear need to increase the awareness of hypogonadism throughout the medical profession, especially in primary care physicians who are usually the first port of call for the patient. Hypogonadism can significantly reduce the quality of life and has resulted in the loss of livelihood and separation of couples, leading to divorce. It is also important for doctors to recognize that testosterone is not just a sex hormone. There is an important research being published to demonstrate that testosterone may have key actions on metabolism, on the vasculature, and on brain function, in addition to its well-known effects on bone and body composition. This article has been used as an introduction for the need to develop sensitive and reliable assays for sex hormones and for symptoms and treatment of hypogonadism.

Various regulatory authorities such as the International Conference on Harmonization (ICH), the United States Food and Drug administration (FDA), and the Canadian Drug and Health Agency (CDHA) are emphasizing on the purity requirements and the identification of impurities in Active Pharmaceutical Ingredients (APIs). The various sources of impurity in pharmaceutical products are - reagents, heavy metals, ligands, catalysts, other materials like filter aids, charcoal, and the like, degraded end products obtained during \ after manufacturing of bulk drugs from hydrolysis, photolytic cleavage, oxidative degradation, decarboxylation, enantiomeric impurity, and so on. The different pharmacopoeias such as the British Pharmacopoeia, United State Pharmacopoeia, and Indian Pharmacopoeia are slowly incorporating limits to allowable levels of impurities present in APIs or formulations. Various methods are used to isolate and characterize impurities in pharmaceuticals, such as, capillary electrophoresis, electron paramagnetic resonance, gas-liquid chromatography, gravimetric analysis, high performance liquid chromatography, solid-phase extraction methods, liquid-liquid extraction method, Ultraviolet Spectrometry, infrared spectroscopy, supercritical fluid extraction column chromatography, mass spectrometry, Nuclear magnetic resonance (NMR) spectroscopy, and RAMAN spectroscopy. Among all hyphenated techniques, the most exploited techniques for impurity profiling of drugs are Liquid Chromatography (LC)-Mass Spectroscopy (MS), LC-NMR, LC-NMR-MS, GC-MS, and LC-MS. This reveals the need and scope of impurity profiling of drugs in pharmaceutical research.

Nymphaea stellata Willd. (Syn. Nymphaea nouchali Burman f.) (Nymphaeaceae) is an important and well-known medicinal plant, widely used in the Ayurveda and Siddha systems of medicines for the treatment of diabetes, inflammation, liver disorders, urinary disorders, menorrhagia, blenorrhagia, menstruation problem, as an aphrodisiac, and as a bitter tonic. There seems to be an agreement between the traditional use and experimental observations, such as, hepatoprotective, anti-inflammatory, and particularly antidiabetic activity. Nymphayol, a steroid isolated from the flowers has been scientifically proved to be responsible for the traditionally claimed antidiabetic activity; it reverses the damaged endocrine tissue and stimulates secretion of insulin in the β-cells. However, taking into account the magnitude of its traditional uses, the studies conducted are still negligible. This review is an attempt to provide the pharmaceutical prospective of Nymphaea stellata.

In the present study, novel Schiff bases were synthesized by condensation of 3-amino-2-methyl quinazolin-4-(3H)-ones with different aromatic aldehydes. The 3-amino-2-methyl quinazolin-4-(3H)-one was synthesized from anthranilic acid via the 2-methyl benzoxazin-4-one. The chemical structures of the synthesized compounds were confirmed by means of Infrared (IR), ¹ H-NMR, ¹³ C-NMR, Mass spectral, and Elemental analysis. These compounds were screened for anti-bacterial (Staphylococcus aureus ATCC 9144, Staphylococcus epidermidis ATCC 155, Micrococcus luteus ATCC 4698, Bacillus cereus ATCC 11778, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 2853, and Klebsiella pneumoniae ATCC 11298)) and anti-fungal (Aspergillus niger ATCC 9029 and Aspergillus fumigatus ATCC 46645) activities, using the paper disk diffusion technique. The minimum inhibitory concentrations (MIC) of the compounds were also determined by the agar streak dilution method. Most of the synthesized compounds exhibited significant anti-bacterial and anti-fungal activities. Among the synthesized compounds, 3-(4-hydroxy benzylideneamino)-2-methyl quinazolin-4(3H)-one 4g and 4c was found to exhibit the highest anti-bacterial activity and 3-(4-hydroxy-3-methoxy benzylideneamino)-2-methyl quinazolin-4(3H)-one 4k exhibited the highest anti-fungal activity.

Cefuroxime Axetil (Poorly water soluble drug), when prepared as solid dispersion showed improved solubility and dissolution. Therefore, the main purpose of this investigation was to increase the solubility and dissolution rate of Cefuroxime Axetil by the preparation of its solid dispersion with urea, using the solvent evaporation method. Physical mixtures and solid dispersions of Cefuroxime Axetil were prepared by using urea as a water-soluble carrier in various proportions (1:1, 1:2, 1:3, 1:4, 1:5, 1:6, and 1:7 by weight), by employing the solvent evaporation method. The drug release profile was studied and it was found that the dissolution rate and the dissolution parameters of the drug from the physical mixture as well as solid dispersion were higher than those of the intact drug. The Fourier Transform Infrared (FTIR) spectra revealed no chemical incompatibility between the drug and urea. Drug-polymer interactions were investigated using differential scanning calorimetry (DSC) and Powder X-Ray Diffraction (PXRD).

The aqueous and ethanolic extracts of C. grandis (Family: Leguminosae) were evaluated for antidiabetic activity by a glucose tolerance test, in normal rats and alloxan-induced diabetic rats. The aqueous and ethanolic extracts showed that they significantly lowered the blood glucose levels to normal in the glucose tolerance test. In alloxan-induced diabetic rats the maximum reduction in blood glucose was observed after three hours, at a dose level of 150 mg/kg of body weight. The percentage of protection given by the aqueous and ethanolic extracts was 32.72 and 46.42%, respectively. In the long-term treatment of alloxan-induced diabetic rats, the degree of protection was determined by measuring the blood glucose, cholesterol, and triglycerides on the tenth day. Both the extracts showed a significant antidiabetic activity comparable to that of glibenclamide. These results showed that the Cassia grandis possessed significant antidiabetic activity.

Hydrogel nanoparticles have gained attention in recent years as they demonstrate the features and characters of hydrogels and nanoparticles at the same time. In the present study chitosan and carrageenan have been used, as hydrogel nanoparticles of mercaptopurine are developed using natural, biodegradable, and biocompatible polymers like chitosan and carrageenan. As these polymers are hydrophilic in nature, the particles will have a long life span in systemic circulation. Hydrogel nanoparticles with mercaptopurine is form an antileukemia drug by the counter polymer gelation method. Fourier-Transform Infrared (FT-IR) studies have shown a compatibility of polymers with the drug. The diameter of hydrogel nanoparticles was about 370 - 800 nm with a positive zeta potential of 26 - 30 mV. The hydrogel nanoparticles were almost spherical in shape, as revealed by scanning electron microscopy (SEM). Drug loading varied from 9 to 17%. Mercaptopurine released from the nanoparticles at the end of the twenty-fourth hour was about 69.48 - 76.52% at pH 7.4. The drug release from the formulation was following zero order kinetics, which was evident from the release kinetic studies and the mechanism of drug release was anomalous diffusion, which indicated that the drug release was controlled by more than one process.

The present study was undertaken to evaluate the mucilage isolated from Spinacia oleracea L. leaves, commonly named spinach (family: Amaranthaceae) as an innovative suspending agent. Zinc oxide suspensions (20% w/v) were prepared using the mucilage of S. oleracea L. leaves as a suspending agent, and it was evaluated for its stability by using parameters like, sedimentation profile, degree of flocculation, and redispersibility. The effect of the tested mucilage on the suspension was compared with various commonly used suspending agents, such as, tragacanth, bentonite, and sodium carboxymethyl cellulose (NaCMC) at concentrations of 0.5, 1.0, and 2.0% w/v. The results obtained indicated that the mucilage of S. oleracea L. leaves could be used as a suspending agent, and the performance was found to be superior to both tragacanth and bentonite.

In the present study, a series of novel Schiff bases of isatin [5a-5l] were synthesized by condensation of imesatin with different aromatic aldehydes. The imesatins were synthesized by the reaction of isatin with p-phenylenediamine. The chemical structures of the synthesized compounds were confirmed by means of Infrared (IR), Mass spectroscopy, and Elemental analysis. These compounds were screened for the analgesic activity by the tail-immersion method at a dose of 200 mg/kg body weight. Among the tested compounds 3-(4-(4-hydroxy-3-methoxylbenzylideneamino) phenylimino) indoline-2-one (5i) exhibited better analgesic activity when compared to standard pentazocine. From the above-mentioned results it may be concluded that compounds containing electron-donating groups exhibit better analgesic activity than the electron-withdrawing groups.

Ultraviolet (UV), first derivative, second derivative, and AUC-spectrophotometric methods for the determination of letrozole in pharmaceutical formulations have been developed. For UV-spectrophotometry, the standard solutions were measured at 240.0 nm. The linearity ranges were found to be 0.25-20.0 μgml⁻¹ in methanol and the regression equation was A=1.20×10⁻¹ C+2.22×10⁻² (r ² =0.9994). For the first derivative spectrophotometry, the response (dA/dλ) of standard solutions was measured at 224.0 nm. The calibration curve was constructed by plotting dA/dλ values against concentrations 0.25-20.0 μgml⁻¹ , of letrozole. The regression equation of the linear calibration graph was calculated as D ₁ =3.89×10⁻³ C+1.85×10⁻⁴ (r ² =0.9987). For the second derivative spectrophotometry, the response (d ² A/dλ² ) of standard solutions was measured at 241.0 nm. The calibration curve was constructed by plotting d ² A/dλ² values against concentrations 0.5-20.0 μgml⁻¹ of letrozole standards in methanol. The regression equation of the linear calibration graph was calculated as D ₂ =-1.59×10⁻³ C -4.66×10⁻⁴ (r ² =0.9985). The AUC-spectrophotometric method was based on the calculation of Area under Curve (AUC), for analysis of letrozole in the wavelength range of 235.0-245.0 nm. The calibration curve was constructed by plotting AUC values against concentrations 0.25-20.0 μgml⁻¹ , of letrozole. The regression equation of the linear calibration graph was calculated as AUC=1.132C+0.2153 (r ² =0.9994). The methods were validated by following the analytical performance parameters suggested by the International Conference on Harmonization (ICH). All validation parameters were within the acceptable range. The developed methods were successfully applied to estimate the amount of letrozole in pharmaceutical formulations.

A rapid, precise, specific, and accurate Electrospray Ionisation Tandem Mass Spectrometry (ESI-MS / MS) method has been developed and subsequently validated, for the determination of pregabalin (PB) in human plasma. Gabapentin (GB) was used as the internal standard. PB and GB were extracted from the plasma using a combination of deproteinization, using 0.1% formic acid and liquid-liquid extraction, using methylene chloride. PB and GB were separated using the Hypurity advance column (50 mm × 4.6 mm, 5 μm) and mobile phase, consisting of methanol : 0.1% formic acid (80:20 v / v). PB was determined by using ESI-MS / MS in positive ion mode, with the help of the API 2000 spectrophotometer, operated in a multiple reaction monitoring mode. The parent-to-product ion combination of m / z 160.2→55.1 and 172.2→95.0 was used to quantify PB and GB, respectively. The assay was validated in the concentration range of 99.79 - 4019.90 ng / mL for PB. The limit of quantification (LOQ) was identifiable and reproducible at 99.79 ng / mL. The method has been successfully applied to study the pharmacokinetics of PB in healthy male volunteers.

Rational drug use is a function of prescription practices having medical, social, and economic implications. A household level cross-sectional study was undertaken to determine the prescribing practices and extent of rational therapy in the rural area of 24 pgs (s) South district. Following multistage stratified random sampling, 250 households were selected for the study from 24 pgs South, West Bengal, India. Medical care received by morbid persons was noted as per prescription details, wherever available. The results indicate that of the total of 485 morbid episodes, 302 were treated at some healthcare facility and prescriptions were available for 137 (45.36%) only. Injection use was seen in 9.49% of the prescriptions. In all, 29.20% prescriptions contained at least one antibiotic. This observation was more or less the same among the private and public practitioners (34%). The average number of drugs found was 3.153 per prescription. Overall 63.51% prescriptions were found to be irrational. The prescribing practices and use of drugs have been found to be truly unsatisfactory.